Redkar R G;Peshattiwar V V;Sathaye S
020659 Redkar R G;Peshattiwar V V;Sathaye S (Pharmaceutical Sciences and Technology Dep, Institute of Chemical Technology (ICT), Nathalal Parekh Marg, Matunga-East, Mumbai-400 019 - 141 - , Email: sadhanasathaye@hotmail.com) : Neuroprotective effects of Ocimum sanctum, Linn. extract of MPTP-induced oxidative and nitrosative stress marker in male mouse brain. Int J pharm Sci Res 2017, 8(4), 1694-700.
The present study focuses on the 'antioxidant approach' as a therapeutic intervention for Parkinson's disease (PD). It deals with understanding of the effects of Ocimum sanctum extract on oxidative and nitrosative stress biomarkers, responsible for neurodegeneration. The standardized hydromethanolic extract of O.sanctum, Linn (Os HM) at the dose of 50, 100 and 200 mg/kg were evaluated for their neuroprotective effects against MPTP induced Parkinsonism. Single divided doses of MPTP were used for induction of parkinsonism in male mice. L-DOPA rich and free fractions of Mucuna pruriens and Bromocriptine were considered as positive standards. The antioxidant effect and thus the neuroprotective potential was estimated based upon the levels of protein oxidation products, endogenous enzymatic and non-enzymatic antioxidant pool of glutathione, nitric oxide, superoxide dismutase and catalase. The results revealed that Os HM extract, particularly at the doses of 100 and 200 mg/kg, significantly depleted the protein carbonyl content, restored the decreased levels of GSH. Os HM prevented the observed compensatory response with superoxide dismutase levels against MPTP treatment. It also significantly reduced the MPTP-induced nitric oxide therefore the nitrosative stress levels. Thus, the study demonstrated that Os HM can correct the disrupted homeostasis and redox imbalances due to excess reactive oxygen and nitrogen species generated by the neurotoxin MPTP.
27 ref
Rawoof M D;Rajnarayana K;Ajitha M
020658 Rawoof M D;Rajnarayana K;Ajitha M (NO, Jawaharlal Nehru Technological Univ, Kukatpally, Hyderabad-500 072, Email: rawoofsucp@gmail.com) : Design and evaluation of colon targeted dosage from containing mesalazine using pH dependent polymers. Int J pharm Sci Drug Res 2017, 9(6), 308-14.
Colonic drug delivery has gained importance not just for the delivery of the drugs for the treatment of local diseases associated with the colon like Crohn's disease, ulcerative colitis and irritable bowel syndrome but also for the potential it holds for the systemic delivery of proteins and therapeutic peptides. The aim of the study was to develop colon targeted tablets of Mesalazine by wet granulation method using 33 response surface method with design of experiment software and HPMC K4M, Eudragit RL100, Ethyl cellulose and PVP K-30 used as pH dependent polymers. All the formulations (F1 to F27) were evaluated for the physicochemical parameters and were subjected to in vitro drug release studies. The amount of Mesalazine released from tablets at different time intervals was estimated by UV spectrophotometer. The formulation F26 released 98.16% of Mesalazine after 24 h. The results of the study showed that formulation F26 is the best formulation based on the evaluation parameters which provides targeting of Mesalazine for local action in the colon owing to its minimal release of the drug in the first 4 h. The pH dependent tablet system is a promising vehicle for preventing rapid hydrolysis in gastric environment and improving oral bioavailability of Mesalazine for the treatment of disease at colon region.
6 illus, 8 tables, 17 ref
Rathod N;Patel A I;Prajapati R;Patel N K; Patel A B;Vyas A J
020657 Rathod N;Patel A I;Prajapati R;Patel N K; Patel A B;Vyas A J (Quality Assurance Dep, B.K Mody Govt. Pharmacy College, ear polytechnique campus, Aji dam, Rajkot) : Analytical method development and validation of stability indicating method and related substance by using RP-HPLC of drug substance. Pharma Sci Monit 2017, 8(2), 409-19.
Analytical method for the determination of related substances in various drug substance was developed in reversed phase high performance liquid chromatography. The stability indicating capability of method was established by force degradation studies and method demonstrated successful separation of drug its related substance and degradation products. A simple, economic, selective, precise, and stability-indicating HPLC method has been developed and validated for analysis ofdrug substance.The method wasvalidated as per the International Conference on Harmonization guidelines covers all the performance characteristics of validation like accuracy, precision, specificity, linearity, range and limit of detection, limit of quantification.
8 ref
Rao A S;Rao A P;Dadhich A S;Rao M K
020656 Rao A S;Rao A P;Dadhich A S;Rao M K (NO, , Quality Control Dep, Bheemili, Visakhapatnam-531 162) : Simultaneous determination of atorvastatin, ezetimibe and fenofibrate in tablets by planar chromatography with conformation by electrospray ionization mass spectrometry. Int J Res Pharm Chem 2017, 7(1), 51-9.
A new high-throughput high-performance thin-layer chromatographic- mass spectrometry (HPTLC-MS) method was developed to separate and quantify atorvastatin (AT), ezetamibe (EZ) and fenofibrate (FN) in solid pharmaceutical formulations. Separation was performed on silica gel 60F254 plates using a saturated mixture of toluene: chloroform: ethyl acetate: acetic acid (5.0:3.0:1.6:0.4 v/v) as mobile phase. After chromatography, densitometric detection was carried out by measuring the UV-absorbance at 254 nm for AT, EZ and FN. The Rf values were (0.46±0.01), (0.57±0.01) and (0.84±0.01) for AT, EZ and FN respectively. The method exhibited good linearity over a dynamic range of 50-350 ng/band for AT, 50-350 ng/band for EZ and 1000-5000 ng/band for FN. Recoveries were between 98.98% and 101.26% at three different concentration levels with an intermediate precision (RSD) of the three compounds ranging from 0.3% to 1.5%. The repeatability (RSD) of all the substances was between 0.2% and 1.6%. The validated lowest limit of detection (LOD) was 3.69 ng /band, 18.31 ng /band and 12.22 ng /band whereas lowest limit of quantification (LOQ) - 140 - was 37.49 ng /band, 61.05 ng /band and 40.67 ng /band for AT, EZ and FN respectively. MS confirmation was accomplished by ion trap mass spectrometry in positive electrospray ionization full scan mode for EZ and FN and in negative mode for AT. The HPTLC-MS facilitated the separation and determination of the compounds understudy in one analytical run with reduced analysis cost, good chromatographic selectivity and proves to be a reliable alternative for routine analysis of pharmaceutical formulations.
5 illus, 3 tables, 33 ref
Ramirez-Camejo L A;Garcia-Alicea M; Maldonado-Morales G;Bayman P
020655 Ramirez-Camejo L A;Garcia-Alicea M; Maldonado-Morales G;Bayman P (Centro de Biologia Molecular y Celular de Enfermedades, Instituto de Investigaciones Cientificas y Servicios de Alta Tecnologi, Ciudad del Saber, Apartado 0843-01103, Panama, Republica de Panama, Email: ramirezcamejo@gmail.com) : Probiotics may protect Drosophila from infection by Aspergillus flavus. Int J pharm Sci Res 2017, 8(4), 1624-32.
Probiotics have been used to protect hosts from pathogens of gastrointestinal and reproductive systems, but their ability to protect against systemic pathogens is largely unexplored. In this study we ask whether orally administered bacteria and yeasts can protect Drosophila melanogaster against the opportunistic fungal pathogen Aspergillus flavus. Flies were fed an artificial diet mixed with live microorganisms for one day prior to infection with A. flavus, and mortality was recorded every day for 8 days. Seven microorganisms were tested; of these, Bacillus cereus (ATCC 13061), Candida inconspicua, Issatchenkia hanoiensis, and Klebsiella sp. significantly decreased mortality of flies subsequently infected with A. flavus compared to controls infected with A. flavus alone. Heat-killed microorganisms did not protect flies, suggesting that the probiotic effect observed was not caused by improved nutrition. D. melanogaster is a good model organism to study microbial interactions with hosts and test the effects of potential probiotics against pathogens.
47 ref
Rajput R;Kaur R;Singh M
020654 Rajput R;Kaur R;Singh M (Biotechnology Dep, Jaypee Institute of Information Technology, A-10, Sector - 62, Noida-201 307, Email: manishasingh1295@gmail.com) : In vitro cytotoxicity evaluation of escitalopram loaded nanoparticles after exposure to neuroblastoma cell lines. Int J pharm Sci Res 2017, 8(6), 2600-6.
The aim of the present studies is to evaluate the cytotoxic effects of newly formulated polymeric nanoparticles (ETP NP's) of Escitalopram oxalate (ETP) on NB41A3 cell lines. They were made by ionic gelation method with particle size range between 60 - 115nm, showing spherical morphology. Moreover, zeta potential of the same was recorded as -1.89 ± 0.052 mV and its permeability release showed 98.45 ± 1.82% in 24 hour. The cytotoxicity evaluation of the optimized formulation (A3) included qualitative method of cell morphology (microscopic and DAPI staining evaluation) and quantitative colorimetric assays like - neutral red (NRU), MTT and LDH. The results suggested that, in presence of ETP, there was a remarkable decrease in cell count whereas; ETP NP's showed lesser cytotoxicity. performed. Further, in NRU membrane integrity was assessed and it showed 95.2 ± 0.83% and 72.2 ± 0.56% of cell viability in ETP NP's and ETP pure respectively. However, MTT assay summed up the cell viability up to 93.6 ± 0.68% in ETP NP's in comparison to 88.2 - 139 - ± 0.35% of ETP pure and LDH assay results for both, ETP NP's (5.105 unit/ml) and ETP pure (5.779 units/ml) suggested that the cell viability is more dose and incubation time dependent. These results confirms the efficacy and non toxicity of formulated ETP NP's and thus, it can be further applied to in vivo model to study its various pharmacokinetic and pharmacodynamic parameters to establish its therapeutic potentials completely.
5 illus, 26 ref
Rajput M;Patel N;Chotaliya U;Patel A;Patel A; Vyas A
020653 Rajput M;Patel N;Chotaliya U;Patel A;Patel A; Vyas A (Quality Assurance Dep, B. K. Mody Government Pharmacy College, Polytechnic campus, Near Aji dam, Rajkot-360 003) : Determination of genotoxic impurity and chromatographic method. Pharma Sci Monit 2017, 8(2), 24-31.
Impurity occurs essentially in all drug substance and drug product. Impurities have the potential to cause adverse effect. Hence, there is a need to ensure the level of impurity which is administered to human for safety. Therefore, impurity profiling is of prime importance. Routine impurity analysis in pharmaceuticals generally requires identification at levels of 0.05 percent to 0.2 percent depending on the daily dose. However, genotoxic impurities can be difficult to detect due to their presence at low ppm levels. This review focuses on the regulations and analytical technologies used to detect and quantitate impurities (genotoxic) in pharmaceuticals. Genotoxicity describes the property of chemical agents that damages the genetic information within a cell causing mutations, that may lead to cancer. The data set usually available for genotoxic impurities is quite variable and is the main factor that dictates the process used for the assessment of acceptable limits. In the absence of data usually implementation of a generally applicable approach Threshold of Toxicological Concern (TTC) is proposed. This review focuses on assessment and control of DNA reactive impurities by implementing ICH M7 guideline. Analytical methods are suggested on how to determine genotoxic impurity.
11 ref
Raj A;Bhati P;Bhadekar R
020652 Raj A;Bhati P;Bhadekar R (Microbial Biotechnology Dep, Rajiv Gandhi Institute of IT and Biotechnology, Bharati Vidyapeeth Dee, Pune - Satara Road, Katraj, Pune-411 046, Email: neeta.bhadekar@gmail.com) : Effect of lactic acid bacteria on biofilm formation by Streptococcus mutans: An in vitro study. Int J pharm Sci Res 2017, 8(6), 2533-8.
Dental biofilms are majorly developed by Streptococcus mutans, a cariogenic microorganism and are one of the major effects of glucosyltransferases (Gtf) produced by it. This study was conducted to determine the antagonistic potential of probiotic bacteria against S. mutans biofilm formation. We studied the anti-biofilm formation ability of three Lactobacillus species viz L. rhamnosus, L. acidophilus and L. plantarum. Inhibition of biofilm formation was checked on a cell culture cluster. The samples with robust inhibitory activity were selected to check their effect on Gtf activity by estimating the changes in the amount of glucan synthesized, the Gtf catalyzed reaction product. The results showed that, the cell free broth of L. plantarum and L. acidophilus has significant inhibitory and displacement activity on biofilm formation by the cariogenic organism when employed individually and in combination. Further, the interference (80% reduction) in glucan synthesis observed by - 138 - applying these lactic acid bacteria (LAB) samples suggested their possible role in inhibition of glucosyltransferase (insoluble) [Gtf-I]. In conclusion, our studies demonstrated repressive activities of two LAB species, on the expression of S. mutans virulence genes to reduce its biofilm formation which may be associated with Gtf-I enzyme. Thus the observations would help to develop a potent strategy to combat dental plaque.
6 illus, 31 ref
Rai S Y;Prajapati Y;Patni P
020651 Rai S Y;Prajapati Y;Patni P (Quality Assurance Dep, A-One college of Pharmacy, Enasan, Ahemedabad, Gujarat) : Development and validation of RP-HPLC and UV spectroscopy methods for simultaneous estimation of sofosbuvir and ledipasvir in their combined tablet dosage from. Pharma Sci Monit 2017, 8(2), 369-88.
The present research work describes a simple, accurate, precise and effective UV-Vis Spectroscopic and RP-HPLC method for simultaneous estimation of Sofosbuvir and Ledipasvir. Spectrophotometric methods for simultaneous estimation are developed & validated using QAbsorbance ratio and dual wavelength method. In Q-Absorbance ratio method Sofosbuvir and Ledipasvir showed an iso-absorptive point at 241nm, the second wavelength used was 260nm, which was λmax of Sofosbuvir. In dual wavelength method Sofosbuvir was measured at 252 nm and 310.70 while Ledipasvir was measured at 332 nm and 310.70 nm. A reverse phase high performance chromatographic method was developed for simultaneous estimation of Sofosbuvir and Ledipasvir in their combined dosage. The separation was achieved by BDS Hypersil C18 column (150 X 4.6 mm, 5 μm) column, and ACN : 0.1% TFA in the proportion of 32:68%v/v as mobile phase, at a flow rate of 1 ml/min. Detection was carried out at 245 nm.
20 ref
Radha M;Parthiban P;Aseervadamma M
020650 Radha M;Parthiban P;Aseervadamma M (NO, Nova College of Pharmaceutical Education and Research, Jupudi, Vijayawada-521 456) : New method development and validation for the simultaneous estimation of capecitabine and gemcitabine by using RP-HPLC in a bulk and pharmaceutical dosage forms. Pharma Sci Monit 2017, 8(2), 645-53.
A rapid and precise reverse phase high performance liquid chromatographic method has been - 137 - developed for the validated of Capecitabine and Gemcitabine, in its pure form as well as in tablet dosage form. Chromatography was carried out on an Altima C18 (4.6 x 150 mm, 5 μm) column using a mixture of Acetonitrile, Methanol and Phosphate buffer pH 4.6 (10:25:65 v/v) as the mobile phase at a flow rate of 1.0 mL/min, the detection was carried out at 234 nm. The retention time of the Capecitabine and Gemcitabine was 2.088, 6.068 ± 0.02 min respectively. The method produce linear responses in the concentration range of 25-125 <109g/mL of Capecitabine and 10-50 <109>g/mL of Gemcitabine. The method precision for the determination of assay was below 2.0% RSD. The method is useful in the quality control of bulk and pharmaceutical formulations.
13 ref
Proy-Vega B;Martinez Blazquez A;Solis Garcia Del Pozo J;Nava E;Jordan J
020649 Proy-Vega B;Martinez Blazquez A;Solis Garcia Del Pozo J;Nava E;Jordan J (Pharmacy Dep, La Mancha-Centro Hospital, Avenida de la Constitucion n
Pharmacovigilance compiles and analyzes spontaneous adverse drug reactions (ADRs) notifications reports on pharmacovigilance databases. Benzodiazepines have been related to skin and subcutaneous tissue disorders ADRs (SSTD-ADRs); tetrazepam was withdrawn in 2013 because of these ADRs. We intended to locate possible associations between cutaneous ADRs and benzodiazepines marketed in USA; for that, we calculated Data mining algorithms (PRR, ROR, IC and EBGM) on benzodiazepines spontaneous notifications reported to the American pharmacovigilance database. ROR yielded signals for eight drugs; PRR and IC for four, and EBGM only one. Clobazam originated a signal for "Stevens-Johnson syndrome" and "Blister"; midazolam for "Toxic epidermal necrolysis", "DRESS syndrome" and "Erythema"; quazepam for "Erythema multiform" and "Drug eruption"; and tetrazepam "Dermatitis bullous", "Toxic skin eruption", "Rash maculopapular" and "Rash erythematous". Tetrazepam exhibited signals by all Data mining algorithms calculated. Quazepam, clobazam and midazolam, by 3 algorithms (PRR, ROR and IC). Our results provide new data that come to increase the limited comparative data published on the sensibility of algorithms. However, larger studies providing new clinical evaluation on these associations will be required.
1 illus, 6 tables, 35 ref
Pratiwi S U T;Hertiani T
020648 Pratiwi S U T;Hertiani T (Pharmaceutical Biology Dep, Faculty of Pharmacy, Gadjah Mada Univ, Sekip Utara, Yogyakarta 55281, Indonesia, Email: sylvia_pratiwi@ugm.ac.id) : Efficacy of massoia oil in combination with some indonesian medicinal plants oils as anti-biofilm agent towards candida albicans. Int J pharm Sci Res 2017, 8(5), 2013-25.
Microbial resistance to antibiotics is often caused by biofilm formation of the microbial pathogen. One strategy used to combat this recalcitrance mechanism is by using the combination of antimicrobial drugs. Essential oils have - 136 - evoked interest as sources of natural products and represent an alternative approach in combating microbial pathogen. The aim of the present work was to investigate the possible synergistic activity of Massoia aromatica oil in combination with Cinnamomum burmanii, Ocimum basilicum, Citrus hystrix and Piper betle oils against Candida albicans biofilm. Biofilm formation inhibition assay and biofilmdegradation assay of essential oils were determined using microtiter broth method. The Fractional inhibitory concentration indices (FICI) of essential oils in combinations were calculated from the checkerboard assay. The synergistic activity was found in combination of M. aromatica oil with all the essential oil tested in inhibit the formation of intermediate stage of C. albicans bio-film. The interaction of M. aromatica oil with all the essential oil tested in inhibit the formation of mature stage of C. albicans biofilm were varied from synergistic to neutral, however, the activity of essential oils combination in breaking down the established biofilm were found to be less active. The results obtained clearly indicate that combinations of these oils are potential for enhancing their anti biofilm properties. This research could contribute to the development of new strategies to prevent and treat C. albicans biofilm infections.
33 ref
Prasad S S;Pathak R R;Vijpeyee S K;Bhavsar V H
020647 Prasad S S;Pathak R R;Vijpeyee S K;Bhavsar V H (Pharmacology Dep, GMERS Medical College, Himmatnagar-383 001, Email: shambhuprasad94@yahoo.com) : Effect of ginger-juice (Zingiber officinale roscoe) on lithium-induced locomotor activity in rat. Int J pharm Sci Res 2017, 8(4), 1826-9.
Ginger has shown to benefit in muscular pain due to eccentric exercise and in osteoarthritis but a later review denied these properties due to uncertainties. To ascertain the reality, this study was proposed. (A) Albino rats (n=6-12) were administered G.J at single dose (4 ml/rat, p.o) as single administration (acute) and chronic treatment 4ml/rat p.o over period of 7 days. Following this assessment was done. Effect of treatment with G.J acutely and chronically (7 days) administered, was assessed. Parameter used during assessment was head twitches. Chronic treatment of ginger-juice induced the head twitches significantly. Acute treatment with ginger-juice did not affect this activity. Chronic treatment increased the number of head twitches induced by lithium. Lithium induced head twitches were enhanced after chronic administration of ginger-juice.
9 ref
Prajapati K V;Sheth N R;Dudhrejiya A V
020646 Prajapati K V;Sheth N R;Dudhrejiya A V (Pharmaceutical Sciences Dep, Saurashtra Univ, Rajkot-360 005) : Antidiabetic activity of chloroform fraction of methanolic extract of fruits of Cucumis callosus cogn. Pharma Sci Monit 2017, 8(2), 527-38.
Cucumis callosus Cogn. (Cucurbitaceae) fruit is used in the traditional medicine for the treatment of diabetes. Based on a number of reports on the blood glucose reduction and other complications associated with some curbitaceae plants, antidiabetic effect of Cucumis callosus fruit was investigated. To investigate the antidiabetic action of chloroform fraction of methanolic extract of fruits of Cucumis callosus Cogn. in alloxan induced diabetic rats. The antidiabetic activity of chloroform fraction of Cucumis callosus fruit was evaluated by using normal and alloxan induced diabetic rats. The chronic effect of chloroform fraction was evaluated by administering to normal and alloxan induced diabetic rats at dose of 10 and 20 mg/kg p.o per day for 14 days. Blood glucose levels were monitored at specific interval and different biochemical parameters were also carried out. The statistical data indicated the significant decrease in blood glucose, total cholesterol, serum triglycerides, serum LDL, serum VLDL, serum SGOT and SGPT levels and serum urea level, whereas HDL cholesterol was significantly increased when treated with the fraction.Chloroform fraction of the fruits of Cucumis callosus also showed significant antioxidant potential. The phytochemical screening revealed the presence of flavonoids, steroidal triterpenoids(cucurbitacins) and glycocides. The chloroform fraction of Cucumis callosus has had beneficial effects in reducing elevated blood glucose level and lipid profile of alloxan induced diabetic rats. The results of the study for the first time show that the plant possesses antidiabetic activity, confirming the traditional claims. Future research should focus on the identification and the antidiabetic activity of the constituents from this plant.
35 ref
Prabha G R B;Nagulu M
020645 Prabha G R B;Nagulu M (NO, Mewar Univ, NH-79, Gangrar, Chhitorgarh-312 901, Email: ramyapharmd66@gmail.com) : Pharmacokinetic drug- drug interactions between albuterol with beta blockers timolol. Int J pharm Sci Drug Res 2017, 9(6), 323-6.
The study was aimed to conduct to evaluate any possible pharmacokinetic interactions between albuterol and timolol. Study was conducted in Male Wistar rats; animals were divided in to three groups, Group I received albuterol alone in single dose / day in healthy rats. Group 2 received timolol alone in single dose / day in healthy rats. Group 3 received albuterol and timolol concomitant administration in healthy rats as a single dose / day. The treatment was given on day one and day 8 both alone albuterol and timolol concomitantly used both the drugs. There was no significant difference in both cmax, tmax and AUC0-t and AUCo-inf of albuterol alone and combination of timolol on day 1 and day 8 respectively. Based on the results obtained from kinetic study it is evident that the single dose of albuterol and timolol individually and concomitantly treated shows no statistically significant interactions in its pharmacokinetic parameters.
4 illus, 4 tables, 13 ref
Poornima P;Abbulu K;Mukkanti K
020644 Poornima P;Abbulu K;Mukkanti K (NO, Jawaharlal Nehru Technological Univ, Kukatpally, Hyderabad-500 072, Email: pamupoornima@gmail.com) : Formulation and in-vitro evaluation of gastro-retentive floating tablets containing quetiapine fumarate. Int J pharm Sci Drug Res 2017, 9(6), 315-22.
The study was focused on Gastro-retentive tablets of Quetiapine fumarate using hydrophilic polymers HPMC K 250 PH PRM, HPMC K 750 PH PRM and HPMC K 1500 pH PRM as release retarding agents. WSR 301 was chosen as resin, Sodium bicarbonate was used as effervescent agents. FTIR studies revealed that there is no interaction between the drug and polymers used for the formulation. The tablets were prepared by direct compression method and the release rate was found to decrease with proportional increase in the ratio of polymer to drug. Quetiapine fumarate has good water solubility and is absorbed well from stomach and therefore is a very good drug to be formulated into gastro retentive floating dosage form. In-vitro release profile of Quetiapine fumarate and marketed product when compared, the optimized formulation F19 showed drug release of 98.65% within 24 h whereas 96.78% of the drug was released from the marketed product within 1h. The major mechanism of drug release follows zero order kinetics and non fickian transport by coupled diffusion and erosion. Such a formulation of Quetiapine fumarate with extended drug release over 24 hours probably is the best formulation for the treatment of Schizophrenia with only one oral tablet a day thus minimizing the side effects with low drug dose. The optimized formulation remained stable when subjected to accelerated stability studies.
19 illus, 8 tables, 20 ref
Platel K;Srinivasan K
020643 Platel K;Srinivasan K (Biochemistry Dep, CSIR - Central Food Technological Research Institute, Mysore-570 020, Email: ksri.cftri@gmail.com) : Nutritional profile of chekurmanis (Sauropus androgynus), a less explored green leafy vegetable. Indian J Nutr Diet 2017, 54(3), 243-52.
Chekurmanis (Sauropus androgynus) belonging to Euphorbiaceae, is a perennial shrub, growing wildly in Southeast Asia. The leaves of chekurmanis are highly nutritious, being a very rich source of micronutrients and protein. In this study, chekurmanis leaves were evaluated for protein and micronutrient content at different stages of maturity. Maturity of the leaves did not alter the rich content of protein which remained around 22.0 g/100 g. Total dietary fibre content of the leaves ranged between 34 and 36% at different stages of maturity. Fully matured leaves contained a significantly higher amount of calcium, as compared to the tender leaves. The iron content of these leaves ranged from 3.89 to 4.50 mg/100 g, while the zinc content of the same was between 1.26 and 1.48 mg/100 g. The bioaccessibility of iron and zinc was significantly higher in the tender leaves. The tender and partially mature leaves of chekurmanis contained 74 and 69 mg/100 g of niacin, respectively. The β-carotene content of the leaves ranged from 7400 to 9250 μg/100 g, while that of vitamin E ranged between 17.6 to 15.6 mg/100 g. Chekurmanis leaves contain an alkaloid, the content of which was significantly higher in mature leaves (1740 mg/ 100 g) as compared to tender leaves (1439 mg/100 g). The alkaloid content of chekurmanis leaves was significantly reduced upon pressure - 134 - cooking. This is the first report on the nutrient content of chekurmanis leaves at different stages of maturity, as also on the bioaccessibility of minerals.
6 tables, 10 ref
Pise H N;Jadhav S S
020642 Pise H N;Jadhav S S (Pharmacology Dep, SRTR Govt. Medical College, Ambajogai, Beed, Maharashtra, Email: drharshalpise@gmail.com) : Evaluation of analgesic and antipyretic activity of Nigella sativa: an experimental study. Natn J Physiol Pharm Pharmac 2016, 6(4), 291-5.
Objectives were to investigate the analgesic and antipyretic activity of N. sativa seed fixed oil and compare it with control and aspirin. Albino Wistar rats of either sex weighing 180-200 g and Swiss mice weighing 25-30 g were used. The study was conducted after approval from the Institutional Animal Ethics Committee. The tail flick method in rats described by D'Amour and Smith and acetic acid-induced writhing in mice were used for evaluation of analgesic activity and baker's yeast-induced pyrexia method was used to evaluate antipyretic activity. In tail flick method of analgesia, N. sativa showed analgesic activity, which was comparable with aspirin. In acetic acid-induced writhing model of analgesia, the action of N. sativa was significantly greater than the control group, and it was comparable with aspirin. In baker's yeast-induced pyrexia method, N. sativa group did not show any significant reduction in the rectal temperature at any hour interval. The changes in the rectal temperature in N. sativa group were comparable with control group (p
4 tables, 16 ref
Phatak R S;Matule S M
020641 Phatak R S;Matule S M (NO, Krishna Institute of Medical Sciences Deemed Univ, NH-4, Near Dhebewadi Road, Malkapur-415 539, Email: phatak.rohan1983@gmail.com) : Ameliorated activity of Murraya koenigii leaves chloroform extract (MKCE) against lead induced hepatic dysfunctions in mice. Int J pharm Sci Res 2017, 8(6), 2619-23.
Lead is a well-known hepatotoxic and all-pervading heavy metal. Ingestion of lead induces structural dysfunctions, physiological distortion and biochemical impairment in the liver. The present study was aimed to ascertain the ameliorated effect of chloroform extract of Murraya leaves against the deleterious effects of lead on hepatic function parameters. Murraya koenigii Chloroform Extract (MKCE) was prepared by maceration. Male albino Swiss mice were divided into three groups of six each. Group I (Control group) served as normal diet and water ad libitum as control group, Group II (lead treated group) received intraperitoneal injection of lead acetate (15mg/kg) daily once whereas Group III (MKCE with lead-treated group) received MKCE (50 mg/kg) and injection of lead acetate intraperitoneally (15mg/kg) daily once time. Experimental study continued for consecutive 7 days. On the 8th day, liver were desiccated from all animals; homogenized to collect supernatant into vials. Serum ALT, AST, ALP, TB, TP and ALB levels were estimated. Significant rise in levels of ALT, AST, ALP, TB were observed along with decreased level of TP and ALB in lead-intoxicated mice. Hepatic enzyme levels were significantly reduced (p
1 table, 29 ref
Pervaiz A;Malik B;Rashid N
020640 Pervaiz A;Malik B;Rashid N (Institute of Biochemistry and Biotechnology, Punjab Univ, Lahore, Pakistan, Email: barizah.ibb@pu.edu.pk) : Enhancing soluble gene expression of α-amylase Bacillus licheniformis and purification of recombinant protein. Adv Life Sci 2017, 7(1), 5-10.
Alpha-amylase is an endoglucan hydrolase that catalyzes the cleavage of a(1-4) glycosidic linkage between glucose residues of polysaccharides. α-amylase involved in starch degradation plays a wide role in the starch industry. Also, it has many applications in other industries as it is being employed in detergent industry, food industry, paper industry, pharmaceuticals and sugar industry. This enzyme shows optimized activity at 40-100°C and a pH of 6.5. α-amylase is a metalloenzyme and Ca+2 ions play an important role in its thermostability and activity. Recombinant α-amylase, from Bacillus licheniformis strain ATCC 27811, was produced in Escherichia coli. Enzyme expression was optimized and intracellular protein expression in soluble form was found with 306 total units of enzyme activity. The enzyme was heat treated at 70°C and it showed its thermostability. The enzyme was purified using the single step purification technique of Ni+2 affinity column chromatography.
7 illus, 1 table, 20 ref
Pawar Y D;Chaudhari K L;Chaudhrari P D
020639 Pawar Y D;Chaudhari K L;Chaudhrari P D (Pharmaceutics Dep, SCES's, Indira College of Pharmacy, 89/2A, Tathawade, Pune, Maharashtra, Email: yogeshdpawar@rediffmail.com) : Development and optimization of spray dried amorphous ternary system of celecoxib using design of experiments. Int J pharm Sci Res 2017, 8(5), 2233-42.
One of the major challenges in pharmaceutical development is the poor dissolution performance of drugs. Celecoxib (CLX) is a poorly water soluble drug with its bioavailability being limited by its poor dissolution. In this study spray drying method was employed to prepare CLX: PVP K30:HPB (hydroxypropyl β-cyclodextrin) amorphous ternary system (ATS). Statistical experimental design was employed to investigate the combined effect of two experimental factors, i.e., % of polyvinayl pyrrolidone (PVP) K30 and % of HPB on saturation solubility (SS), dissolution efficiency (DE) and mean dissolution time (MDT), considered as the responses to be optimized. Design of experiment was used in the context of quality by design, which requires a multivariate approach for understanding the multifactorial relationships among experimental factors. Central composite design allowed for defining a design space. Desirability function was used to attain simultaneous optimization of all responses. The desired goals were achieved for SS, DE and MDT. Experimental values obtained from the optimized formulations were very close to the predicted values, thus confirming the validity of - 132 - the generated mathematical model. These results demonstrated the effectiveness of the proposed jointed use of PVP K30 and HPB, as well as the usefulness of the multivariate approach for the preparation of ATS. Validated optimum ATS were characterized by DSC, XRD, SEM and particle size analysis. Characterization results confirmed the formation of amorphous ternary system with average particle size 727.9±260.6nm.
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Paul A D;Samatha P;Manasa S;Munemma R;Supriya D
020638 Paul A D;Samatha P;Manasa S;Munemma R;Supriya D (SVU College of Pharmaceutical Sciences, SV Univ, Tirupati-517 502, Email: deevan4@gmail.com) : Modeling the oral cavity with mucoadhesive drug delivery systems - a potential alternative to conventional therapy. Int J pharm Sci Drug Res 2017, 9(6), 299-307.
Oral mucosal drug delivery system is widely applicable as novel site for administration of drug and controlled release action by preventing first pass metabolism and enzymatic degradation due to GI microbial flora. The oral cavity represents a challenging area to develop an effective drug delivery modelling. This arises due to the various inherent functions of the oral cavity (eating, swallowing, speaking, chewing), as well as the presence of the fluid that is involved in all these activities, saliva. This fluid is continually secreted into and then removed from the mouth. Oral Mucosa drug delivery system provides local and systemic action. The delivery of drugs through the buccal mucosa has attracted much research interest over the past two decades and numerous approaches, both conventional and complex, have been developed in an attempt to deliver a variety of pharmaceutical compounds via the buccal route. To outline the progress in the in vitro and in vivo modeling of Mucosal drug delivery and provide a critical review of currently used methods. The purpose of this review is to represent the modeling of oral cavity with Mucoadhesive drug delivery systems and clarify the potential alternative to conventional therapy.
^iia7 illus, 1 table, 40 ref
Patil Y;Patil S;Pawar S P
020637 Patil Y;Patil S;Pawar S P ((Quality Assurance) P.S.G.V.P. Mandal Dep, College of Pharmacy, Shahada, Nandurbar, Maharashtra) : Review on solubility enhancement of poorly soluble drug by solid dispersion method. Pharma Sci Monit 2017, 8(2), 99-109.
Solubility is the phenomenon of dissolution of solid in the liquid phase to give a homogenous system. Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be show. Poorly water soluble drug often require high doses in order to reach therapeutic plasma concentration after oral administration. Low aqueous solubility is the major problem - 131 - encountered with formulation development of new entities. Currently only 8%of new drug candidates have both high solubility and permeability. Because of solubility problem of many drug the bioavailability of then gets affected and hence solubility enhancement become necessary. It is now possible that to increase the solubility of poorly soluble drugs with help of various techniques such as physical method and chemical method.
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Patil N;Tadvi S A;Pawar S P
020636 Patil N;Tadvi S A;Pawar S P (NO, P. S. G. V. P. Mandal's College of Pharmacy, Shahada (MH)) : Review on self emulsifying drug delivery system. Pharma Sci Monit 2017, 8(1), 115-36.
Solubility of orally administered drug is major challenge of pharmaceutical industry as nearly 35-40% of newly launched drugs possess low aqueous solubility which leads to their poor dissolution and low bioavailability, resulting in high intra & inter subject variability & lack of dose proportionality. This can be increased by different methods like salt formation, solid dispersion and complex formation. Self-Emulsifying Drug Delivery System (SEDDS) is gaining popularity for improving the solubility of lipophilic drugs. SEDDS are defined as isotropic mixtures of one or more hydrophilic solvents and co-solvents/surfactants that have a unique ability of forming fine oil-in-water (o/w) micro emulsions upon mild agitation followed by dilution in aqueous media, such as GI fluids. Present review provides an updated account of advancements in SEDDS with regard to its composition, evaluation, different dosage forms and newer techniques to convert liquid SEDDS to solid and also various applications.
2 illus, 9 tables, 47 ref
Patil K;Patil N;Tadvi S A;Pawar S P
020635 Patil K;Patil N;Tadvi S A;Pawar S P (NO, P. S. G. V. P. Mandal's College of Pharmacy, Shahada(MH)) : Medicated lollipop containing fexofenadine HCL for pediatric. Pharma Sci Monit 2017, 8(2), 448-60.
There are several dosage forms in the market, there is a need for more dosage form which acts effectively and locally as well as systematically. The benefits of the present research work is increased retention time of the dosage form in oral cavity and increased bioavailability, reduction in gastric irritation by passing first pass metabolism. Lollipops are flavored medicated dosage form intended to be sucked and held in the mouth or pharynx containing one or more medicaments usually in the sweetened base. Medicated lollipop is designed to improve patient compliance, acceptability. The lollipops were prepared by heating and congealing method using methylcellulose, citric acid as polymer. Drug Fexofenadine Hcl is an antihistaminnics drug which contains very bitter taste drug. For patient acceptability we need to improve the taste of the drug by different saccharides like sucrose, dextrose. Pourability,Texture,and Elasticity is improved by different plasticizers like glycerin. It was found that the formulation containing methyl cellulose,and combination of sacharides like dextrose,sucrose showed better drug release and it was more stable, unlike the other formulations.
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Patil H;Patil S;Pawar S
020634 Patil H;Patil S;Pawar S (NO, P.S.G.V.P.M's College of pharmacy, shahada,Dist-Nandurbar-425 409) : Review on solubility enhancement of poorly water soluble drug by solid dispersion techaniqe. Pharma Sci Monit 2017, 8(2), 110-8.
Solubility is the phenomenon of dissolution of solid in liquid to give homogenous system. Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. A success of formulation is depend on how efficiently it makes the drug available at the site of action. Therefore it is necessary to improve solubility of drug by some methods like co-solvency, salt formation, addition of solubilizing agent, micronization, complexation, solid dispersion. Many times it becomes challenging to formulate poorly water soluble drugs. In this review we concentrated on improvement of the solubility of poorly water soluble drugs by using various - 130 - methods.
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Patil H A;Tadvi S A;Pawar S P
020633 Patil H A;Tadvi S A;Pawar S P (NO, P.S.G.V.P. Mandal's College of Pharmacy, Shahada, Dist. Nandurbar-425 409) : Formulation and evaluation of floating matrix tablet of repaglinide. Pharma Sci Monit 2017, 8(2), 285-97.
The study involves preparation and evaluation of floating tablet of Repaglinide prolongation of gastric resident time. The tablets were prepared by direct compression method using polymer HPMC (K 100M, HPMC E15) & Xanthun gum. The tablets were evaluated for Angle of repose, Bulk density, Tapped density, Carr's index Hausner ratio. The prepared tablets were characterized by size & Shape, Hardness, Thickness, Friability, Weight variation and drug content respectively. In-vitro drug release studies were performed by using an USP dissolution test apparatus-II (Basket type) at 37 + 0.5 OC and 50 rpm speed. To study the release behavior were performed on the optimized formulation. The prepared tablet exhibited prolonged drug release (12 hr.) and remained buoyant for > 12 hr. The optimized formulation F7 was kept for short term stability study. The conditions for stability study were 40oc and relative humidity of 75% from the study; it was observed that there is no significant change in stability and drug release rate.
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Patil H A;Patil P S;Tadavi S A;Jain V H;Pawar S P
020632 Patil H A;Patil P S;Tadavi S A;Jain V H;Pawar S P (NO, PSGVPM's College of Pharmacy, Shahada, MH-India-425 409) : Review on "floating drug delivery system". Pharma Sci Monit 2017, 8(2), 55-68.
The purpose of writing this review on floating drug delivery systems (FDDS) was to compile the recent literature with special focus on the principal mechanism of floatation to achieve gastric retention. Drug delivery systems are those that float immediately upon contact with gastric fluids present - 129 - promising approaches for increasing the bioavailability of drugs with absorption windows in stomach or upper small intestine, unstable in the intestinal or colonic environment, and exhibit low solubility at high pH values. It is new drug delivery system maximize effectiveness and compliance. The Physiological problems like short gastric residence time and unpredictable gastric emptying time were overcome with the use of floating dosage forms which provide opportunity for both local and systemic effect. Floating drug delivery system enable prolonged and continuous input of the drug to the upper part of the gastro retention tract and improve the bioavailability of medication that is characterized by a narrow absorption window. This review article is in pursuit of giving detailed information on the pharmaceutical basis of their design, classification, advantages, in vitro and in vivo evaluation parameters, and application of floating systems, and applications of these systems. These systems are useful to several problems encountered during the development of a pharmaceutical dosage form and the future potential of FDDS. At attempt has been made in this review article to introduce the readers to current development in floating drug delivery system.
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Patel R A;Shah C N
020631 Patel R A;Shah C N (Pharmacy Dep, Shri Jagdishprasad Jhabarmal Tirewala Univ, Jhunjhunu, Rajasthan-333 001) : Method development and method validation of HPTLC for stability indicating and simultaneous estimation study of linagliptin and metformin in combination dosage form. Pharma Sci Monit 2017, 8(1), 63-74.
A new simple, precise, and accurate stability indicating high-performance thin-layer chromatography (HPTLC) method was developed and validated for simultaneous estimation of linagliptin and metformin active pharmaceutical ingredients and fixed dose combination. The separation was eluted on a Zodiac C18 column (250 mm x 4.6 mm; 5μ) using a mobile phase mixture of mixed phosphate buffer 6.5 and acetonitrile in a ratio of 50:50 v/v at a flow rate of 1.0 ml/min. The plates were developed to a distance of 8 cm at ambient temperature. The developed plates were scanned and quantified at their single wave length of 248 nm. The retention times were 1.070.1 min for Metformin and 4.630.1 min for Linagliptin. Linagliptin and metformin RF values were found as 0.70 and 0.17, respectively. The method was validated for precision, accuracy, specificity, and robustness. The linearity curves were obtained in the concentration range of 100-600 ng per spot by area with correlation coefficients of 0.999 and 0.99 for linagliptin and metformin, respectively. Limit of detection was found to be 5.09 and 7.24 ng per spot for linagliptin and metformin, respectively; lowest possible quantity to be quantified by the proposed method was found to be 15.72 and 26.39 ng per spot for linagliptin and metformin, respectively. The method was accurate, precise, specific and rapid found to be suitable for the quantitative analysis of the drug and dosage form.
2 illus, 5 tables, 28 ref
Patel M M;Doshi D B;Ghosh C
020630 Patel M M;Doshi D B;Ghosh C (Quality Assurance Dep, L. M. College of Pharmacy, Navrangpura, Ahmedabad-380 009) : Development and validation of UV methods for estimation of nimodipine in soft gelatin capsule. Pharma Sci Monit 2017, 8(2), 389-400.
Three simple, sensitive and economical UV spectrophotometric methods have been developed for the estimation of nimodipine in soft gelatin capsule. Methods were based on the zero order (Method A), first order derivative spectroscopy (Method B) and area under curve method (Method C). All proposed methods obeyed Beer's law in the concentration range of 4-20 μg/mL with correlation coefficient r= 0.9984 in Method A, r= 0.9960 in Method B and r=0.9989 in Method C. Accuracy of the method was confirmed by recovery studies and mean recovery was found to be 99.93-99.86% for Method A, 98.74-99.24% and 99.27-99.92% for Method B and 98.43-99.19% for Method C. The intraday and inter day precision were found to be within limits. The proposed methods have adequate specificity, sensitivity and reproducibility for quality control assay of nimodipine in soft gelatin capsule.
33 ref
Patel M M;Doshi D B;Ghosh C
020629 Patel M M;Doshi D B;Ghosh C (Quality Assurance Dep, L. M. College of Pharmacy, Navrangpura, Ahmedabad-380 009) : Development and validation of HPLC method for estimation of nimodipine in soft gelatin capsule. Pharma Sci Monit 2017, 8(2), 200-9.
Nimodipine is a calcium channel blocker, used in treatment of hypertension. A simple, precise, rapid and accurate isocratic reverse phase high performance liquid chromatography method was successfully developed and validated for estimation of nimodipine in soft gelatin capsule. Chromatographic separation was achieved on an Inertsil ODS-3V column (150 mm X 4.6 mm, 5 μm) using mobile phase containing methanol: tetrahydrofuran:water (30:20:50 v/v/v) at the flow rate 2.0 mL/min with UV detection at 235 nm. The column was kept at 40°C. A linear response was observed in the range of 60-180 μg/mL with correlation co-efficient of 0.9998. The mean percent recoveries of nimodipine in soft gelatin capsule were found to be in the range of 98.92- 100.31%. The intraday and inter day precision was found to be within limits. The proposed method has adequate specificity, sensitivity and reproducibility for quality control assay of nimodipine in soft gelatin capsule dosage form without any interference from excipients.
33 ref
Parmar U;Sheth N;Dhudhrejiya A
020628 Parmar U;Sheth N;Dhudhrejiya A (Pharmaceutical Sciences Dep, Saurashtra Univ, Rajkot-360 005) : Simultaneous estimation of ofloxacin and cefpodoxime proxetil in tablet dosage form by using liquid chromatography methods. Pharma Sci Monit 2017, 8(2), 573-82.
An accurate, sensitive and precise high-performance liquid chromatographic method has been developed for the estimation of Ofloxacin and Cefpodoxime proxetil in tablet dosage form. The method employed C18 (250mm
19 ref
Parmar D R;Vala B S
020627 Parmar D R;Vala B S (Pharmaceutical Chemistry Dep, L. M. College of Pharmacy, Navrangpura, Ahmedabad-380 009) : Design, synthesis and biological screening of some novel imidazole derivatives as H1 receptor antagonists. Pharma Sci Monit 2017, 8(2), 461-72.
Imidazole derivatives are associated with broad spectrum of biological activities.1, 2 In view Two series of compounds have been - 127 - designed as H1-receptor antagonists. Derivatives of two series, 5- (4-substituted-benzylidene) -3-((3,4-dimethoxy benzylidene)amino)-2-thioxoimidazolidin-4-one and 2-(1H-imidazol-1-yl)-N,N-diphenylalkylamide were synthesized. All the synthesized compounds were characterized by IR and Mass spectroscopy and one by 1H - NMR spectroscopy. All synthesized compounds were pharmacologically screened in vitro H1- antihistaminic activity using chicken ileum. Cetrizine is used as standard. The potent compounds were screened in-vivo for their sedation potential. Amongst all the compounds screened, compound 7b was found most potent in the series with IC50 value 0.186 μM. Potent compounds were screened in-vivo for their sedation potential showed less sedation potential than that by the standard drug.
10 ref
Parekh K K;Paun J S;Soniwala M M
020626 Parekh K K;Paun J S;Soniwala M M (Pharmaceutics Dep, Smt. C.V. Gajera Pharmacy Mahila College, Amreli, Gujarat, Email: khyatirparekh@gmail.com) : Formulation and evaluation of nanosuspension to improve solubility and dissolution of diacerein. Int J pharm Sci Res 2017, 8(4), 1643-53.
Diacerein is an Osteoarthritic drug that exhibited suboptimal oral bioavailability upon oral administration of conventional dosage form. Nanosuspension gaining more attention for improving oral bioavailability of such drugs. This study was aimed to enhance the solubility and dissolution of diacerein by preparing Nanosuspension. Diacerein Nanosuspension was prepared using combination of High Speed Homogenization (HSH) and Media Milling (MM), Poloxamer 407 (stabilizer) and ZrO2 beads (milling media). Various formulation and processing parameters were optimized in preliminary studies. Concentration of stabilizer and milling media were optimized for Cumulative percentage release (%CPR), saturation solubility (SS) and mean particle size (MPS) using 32full factorial design. Optimized batch was derived statistically using desirability function of Minitab17. Model was validated by formulating checkpoint batch. Accelerated stability study was carried out for optimized batch. Identification and compatibility study of drug and stabilizers were carried out using FTIR and DSC studies. Preliminary parameters were optimized by varying one parameter at a time, while keeping other constant by trial and error method. Optimized batch has 100%w/v milling media and 1%w/v of Poloxamer407. %CPR, SS and MPS were found to be 97.74%, 1.245mg/ml and 221.5nm respectively. Four hundred times enhancement in SS that of bulk drug and 97.74%CPR at 2min was observed after nanonization. It was concluded that Combination of HSH and MM technique can be successfully used for preparation of Diacerein Nanosuspension. Prepared nanosuspension significantly enhances solubility and in-vitro dissolution of Diacerein.
39 ref
Panigrahi A R;Guntuku G S;Krishna Kumar M
020625 Panigrahi A R;Guntuku G S;Krishna Kumar M (AU College of Pharmaceutical Sciences, Andhra Univ, Visakhapatnam, Andhra Pradesh) : Screening and identification of marine sponge associated fungus producing novel bioactive molecules. Int J Res Pharm Chem 2017, 7(1), 92-106.
The marine environment is a rich source of both biological and chemical diversity, which has been the source of unique chemical compounds with the potential for industrial development. In recent years, a significant number of novel metabolites with potent pharmacological properties have been discovered from the marine organisms. Several robust new compounds derived from marine natural products are now in clinical pipeline, with more clinical development. In our present study, we had collected the sponge samples from the Bay of Bengal. - 126 - From that we had isolated microorganisms, screened for activity, extracted the bioactive compound from the selected isolate and identified the isolate. Samples of different sponges are collected by removing a piece of the animal (sponge) and kept in sterile YEME broth in a screw capped tube and stored at low temperatures. We isolated microorganisms from various sponge samples by following screening procedures of which one sample was primarily selected for further studies. From the selected sample namely KSP 03 09 2010, morphological studies of the isolates 2F, 3F, 5F, 6F and 7F were performed and identified as fungal isolates. Phenotypic characterization of the fungal isolate 5F by IMTECH, Chandigarh revealed that it belongs to the genus Penicillium. Bioprocess parameters like production medium, sea water composition and incubation time for growth and production of secondary metabolites were optimized to get high yield of the bioactive. Bioautography of the crude extract of 5F revealed that our compound was a mixture of 2- 3 compounds.
31 illus, 6 tables, 47 ref
Panicker P S;Vigneshwaran L V;Bharathi M S
020624 Panicker P S;Vigneshwaran L V;Bharathi M S (pharmaceutics Dep, Ahalia school of pharmacy, Palakkad, kerala) : Formulation and evaluation of sintered matrix tablets of metformin hydrocloride. Pharma Sci Monit 2017, 8(1), 182-99.
Metformin hydrochloride, a water soluble drug,has a short half life of 4 to 5 hours and a limited window of absorption. This necessitates the formulation of this drug as a controlled release tablets so the present work was aimed to extend the release of metformin hydrochloride from matrix tablets by sintering technique. For this purpose polymers like eudragit L 10055and H P M C K 4M were used. These polymers were added to the active ingredient and other excipients. The formulation was then punched into tablets and kept in a dessicator for 1.5 hrs, 3 hrs, 4.5 hrs for sintering.The dessicator must be previously saturated with acetone vapours for 24 hrs. After sintering the tablets were removed from the dessicator, and dried at room temperature for 24 hrs to evaporate the adhering acetone and were finally dried in a vaccum dessicator at 30°C over fused calcium chloride for 24 hrs to remove the residual acetone from the tablets and stored in dessicator for further studies. The tablets were subjects to all evaluation tests of tablets. The results proved that tablets sintered for 4.5 hrs were harder and released drug at slower rate than those sintered for 3 hrs also eudragit L 100 55 was found to be better rate controlling polymer than HPMC K4M.
6 illus, 12 tables, 6 ref
Pandya R P;Sakhreliya B;Patani P
020623 Pandya R P;Sakhreliya B;Patani P (Quality Assurance Dep, A-One college of Pharmacy, Enasan, Ahemedabad, Gujarat) : Development and validation of RP-HPLC method for simultaneous estimation of teneligliptin hemipent ahydrobromide hydrate and metformin hydrochloride in their combined tablet dosage form. Pharma Sci Monit 2017, 8(2), 420-34.
A simple, rapid and precise reverse phase high performance liquid chromatographic method has been developed for simultaneous estimation of Teneligliptin hemipentahydrobromide hydrate and Metformin Hydrochloride in their combine tablet dosage form. Chromatography was performed on a Phenomenex luna ODS C18 (250 mm X 4.6 mm) 5 μm column using 0.025M Dipotassium hydrogen phosphate buffer: Acetonitrile (75:25 v/v) as a mobile phase. The detection was carried out at 238 nm with a flow rate of 1.0 mL/min. The retention times were 2.167 and 6.033 minutes for Metformin Hydrochloride and Teneligliptin hemipentahydrobromide hydrate, respectively. Proposed method was validated as per ICH guidelines for linearity, accuracy, precision, specificity and robustness for estimation of Teneligliptin hemipenta hydrobromide hydrate and Metformin Hydrochloride in their combined Tablet dosage form and results were found to be - 125 - satisfactory. The linearity of the method was excellent over a concentration range 5 to 15 μg/mL for Teneligliptin hemipenta hydr bromide hydrate and 125 to 375 μg/mL for Metformin Hydrochloride. The correlation coefficient was 0.997 and 0.999 for Teneligliptin hemipenta hydrobromide hydrate and Metformin Hydrochloride, respectively. The limit of detection was 0.771 μg/mL and 2.959 μg/mL for Teneligliptin hemipenta hydrobromide hydrate and Metformin Hydrochloride, respectively. The limit of quantitation was 2.336 μg/mL and 8.967 μg/mL for Teneligliptin hemipenta hydrobromide hydrate and Metformin Hydrochloride, respectively. The relative standard deviation values for repeatability, intraday precision and interday precision studies were less than 2% and % recovery was between 98% to 102% for both drugs. So the proposed method was found to be suitable as per ICH Guidelines Q2(R1) for the routine estimation of Teneligliptin hemipenta hydrobromide hydrate and Metformin Hydrochloride in their Combined Tablet dosage form.
9 ref
Pandian N;Chidambaram S
020622 Pandian N;Chidambaram S (Microbiology Dep, Valliammal College of Women, Chennai-600 102, Email: drcsoundhari@gmail.com) : Antimicrobial, cytotoxicity and anti cancer activity of silver nanoparticles from Glycyrrhiza glabra. Int J pharm Sci Res 2017, 8(4), 1633-41.
In this study, the plant Glycyrrhiza glabra was explored for the synthesis of silver nanoparticles (SNPs). The SNPs were characterised by ultra-violet-visible spectroscopy, FTIR analysis and scanning electron microscopy. SEM analysis revealed the formation of SNPs of average size of 46 nm with aqueous extract of G. glabra. The SNPs synthesised by aqueous extract of G. glabra showed strong antibacterial activity against Staphylococcus aureus and Pseudomonas aeruginosa and significant inhibition to other bacteria and few fungi tested. The SNPs also exhibited potential anti cancer activity. The SNPs was observed to be nontoxic from a concentration of 500 μg/ml in vero cell line. The results document SNPs can be synthesised using aqueous plant extracts for applications in the biomedical field.
19 ref
Pandey A K;Tripathi Y C
020621 Pandey A K;Tripathi Y C (Chemistry Div, Forest Research Institute, New Forest, Dehradun-248 006, Email: akpandey@icfre.org) : Biotechnological approach for medicinal plant conservation and enhanced production of secondary metabolites. Int J Pharmac 2017, 4(11), 352-62.
Growing awareness and interest towards traditional heath care system coupled with phenomenal increase in demand and trade of medicinal plant has caused severe threat to the very existence of medicinal plants, which can be gauged from the fact that a number of important medicinal - 124 - plants are becoming threatened or extinct and an increasing number of species are being substituted in herbal preparations. There is, therefore, a need to strike a balance between conservation and use. It is imperative to evolve viable strategies to conserve the surviving populations and their genetic resource of critically important species to avoid further loss. Further, spurt demand for herbal drugs has led to renewed interest in screening plants for novel biologically active compounds particularly to combat such ailments which have defied synthetics drugs. Herbal sector is under constant pressure to develop and deliver effective natural drugs. Phytochemical and pharmacological investigations have led to the isolation and characterization of a significant number of active molecules with versatile therapeutic efficacy. Biotechnology has emerged as the frontier tool for in-vitro production of pharmacologically active phytochemicals. The paper describes the potential and prospects of chemo-biotechnological approach to conservation of medicinal plants and enhanced production of phytopharmaceuticals.
^iia57 ref
Pamu S;Subrahmanyam C V S;Patnaik K S K R
020620 Pamu S;Subrahmanyam C V S;Patnaik K S K R (Pharmacy Dep, Univ College of Technology Osmania Univ, Hyderabad-500 004, Email: sandhyapasikanti@gmail.com) : Formulation and in vitro evaluation of gastroretentive floating drug delivery of valsartan using hot melt extrusion technique. Int J pharm Sci Res 2017, 8(4), 1813-19.
The aim of present study is to improve the aqueous solubility of valsartan by utilizing hot melt extrusion technique (HME). Hot melt extrudates were prepared by novel polymeric matrices such as HPMCAS and Plasdone S630 copovidone at different ratios. The solubility studies of extrudates, showed a significant improvement in aqueous solubility. Gastroretentive floating tablets of valsartan using its extrusion complex with plasdone S630 copovidone were formulated by, direct compression method. The tablets comprised of HPMC K4M, HPMC K15M, as release retarding polymers to control the drug release. Preliminary trials applied to optimize the drug release profile. A 10.5 fold increase in the solubility of valsartan was observed with valsartan: plasdone S630 copovidone complex in the ratio of 1:2. Trial batches of tablets showed best results for formulation F3 (20% HPMC K15M and pregelatinized starch 12%) released 99.41% of valsartan in 20 h, with desired floating lag time (18 sec) and constantly floated on dissolution medium for more than 24 h. Accelerated stability studies were conducted at 40±2 °C temperature and 75±5% RH to determine the effect of aging on the physical and chemical stability of the drug, the results showed no significant loss of activity of drug in the prepared formulations. From the study it was concluded that a gastroretentive floating drug delivery of poorly soluble valsartan can be formulated using hot melt extrusion technique.
14 ref
Pahal V;Arashdeep Kaur;Dadhich K S
020619 Pahal V;Arashdeep Kaur;Dadhich K S (Microbiology Dep, Dolphin Post Graduate College of Science and Agriculture, Chunni Kalan, F.G. Sahib, Punjab-140 406, Email: vikaspahal@gmail.com) : Effect of combination therapy using cow (Bos indicus) urine distillate and some indian medicinal plants against - 123 - selective pathogenic gram-negative bacteria. Int J pharm Sci Res 2017, 8(5), 2134-42.
Inconsequential use of broad-spectrum antibiotics results in the evolution of multiple drug resistant pathogenic gram-negative bacterial strains which is a global health threat and is responsible for high morbidity and mortality rates. This necessitated the search for new effective and safe treatment strategies. One such successful treatment strategy is combination therapy which comprises cow urine distillate and medicinal plants extract. In the present report, this combination therapy was used against five pathogenic gram-negative bacteria- S. typhimurium, K. pneumoniae, E. coli, E. aerogenes and V. cholerae. It was observed that combination therapy had more profound effect than the individual plant extract against all the bacterial strains at the specified level. Combination therapy with T. erecta plant extract was found to be the most effective which improved the antibacterial effect 2.54 times more against E. coli. Other plants extract also improved their antibacterial potential when used with CUD (R.A.I=1.28 to 2.54).
28 ref
Ojewumi M E;Banjo M G;Oresegun M O;Ogunbiyi T A;Ayoola A A;Awolu O O;Ojewumi E O
020618 Ojewumi M E;Banjo M G;Oresegun M O;Ogunbiyi T A;Ayoola A A;Awolu O O;Ojewumi E O (Chemical Engineering Dep, Covenant Univ, Km 10, Idiiroko Road, Canaan Land, P.M.B 1023, Sango-ota, Ogun-State, Nigeria, Email: modupe.ojemodupe.wumi@convenantuniversity.edu.ng) : Analytical investigation of the extract of lemon grass leaves in repelling mosquito. Int J pharm Sci Res 2017, 8(5), 2048-55.
The main objective of the work was to extract the active ingredient in Cymbopogon citratus leave and to formulate a mosquito repellent cream naturally obtained from medicinal plants instead of commonly available synthetic repellents and insecticides such as N-Diethyl-3methylbenzamide (DEET), which are carcinogenic and non eco-friendly. The formulation of cream have smooth texture with a pH 7.30 which is non-irritant and suitable for the skin. The efficacy of the extract of Lemon grass (Cymbopogon citratus) was investigated on mosquito in this research using different concentrations of the oil extract. The sample (cream) with the highest concentration of the active ingredient extracted was found to be most effective in repelling mosquitoes. Ethanol and Hexane were used to extract the essential oil and Gas chromatography-mass spectrophotometer (GC-MS) was used to analyse the constituents in the extracted active oil. The most abundant constituents observed in the hexane extract are cyclotetracosane (4.05%) and naphthalene (5.03%). Hexane proved to be a better solvent by giving a percentage yield of 7.8% of essential oil while ethanol a percentage of 2.9%.
24 ref
Ogunwa T H
020617 Ogunwa T H (Centre for Biocomputing and Drug Development, Adekunle Ajasin Univ, Akungba-Akoko, Ondo State, Nigeria, Email: tomisin.ogunwa@aaua.edu.ng) : Phytoconstituents obtained from tanzanian medicinal plants display a high potential to inhibit glucosamine-6-phosphate synthase as an antimicrobial target. J biol Engng Res Rev 2017, 4(1), 20-33.
Recent pharmacological research has focused attention on biological properties of bioactive compounds derived from medicinal plants. With the aid of in silico modeling and computational studies, the possible antimicrobial activity of phytoconstituents isolated from various Tanzanian medicinal plants was investigated. Out of the eighteen compounds selected and docked against a critical antimicrobial target, Glucosamine-6-phosphate synthase from Escherichia coli (E. Coli), eight (8) compounds including baphikinone, annonaine, rheediaxanthone B, isorheediaxanthone, forbexanthone, amaniensine, 12-hydroxy-des-D-garcigerrin A and baphikixanthone showed high binding affinity towards the enzyme. The molecular interaction, in - 122 - comparison with the reference compounds, fructose-6-phosphate and fluconazole revealed that the compounds favorably docked on the binding site and the enzyme-ligand complex possessed low binding energy value, implying that the compounds may be potent inhibitors of the enzyme. The binding energy values obtained ranged from -7.0 kcal/mol to -9.3 kcal/mol compared to -7.6 kcal/mol and -6.0 kcal/mol obtained for fluconazole and fructose-6-phosphate respectively. The compounds penetrated and appeared to completely blocked the active site and, engaged amino acid residues at the active site in strong hydrogen bonds. These residues include Val-399, Thre-352, Glu-488, Ser-349, Gln-348, Thre-302, Ala-602, Lys-603, and Ser-303 most of which are required for catalytic activity. Hydrophobic interaction also seemed to participate in stabilizing the enzyme-ligand complex. Overall, the binding affinity and configuration for the selected phytoconstituents were comparable to the control ligands. Hence, the compounds may competitively hinder the synthesis of glucosamine-6-phosphate that is required for bacterial and fungal cell wall production. The results obtained in this study validate the antimicrobial potential of the medicinal plant sources of the compounds and show that they possess the ability to inhibit glucosamine-6-phosphate synthase as a target while providing insights into the possible molecular interaction involved in the antimicrobial effects observed in earlier reported wet experiments.
3 illus, 4 tables, 58 ref
Nayak P;Kachroo M
020616 Nayak P;Kachroo M (Pharmaceutical Chemistry Dep, Al-Ameen College of Pharmacy, Bangalore, Karnataka, Email: prgy.nyk@gmail.com) : Comparative group-QSAR and molecular docking studies of 4 - thiazolidinone containing indolin-2-one moiety as vgefr inhibitors. Int J pharm Sci Res 2017, 8(4), 1796-805.
Vascular endothelial growth factor receptors (VEGFR) are kinase based receptors reported as a promising target in anti tumour therapy. VGEFR inhibitors are being investigated which can have important contribution in anti-angiogenic therapy for treatment of cancer. In the present study, an attempt has been made to develop a site-specific QSAR model in order to explore the definite sites of substitution of a series of 4-thiazolidinone derivatives having reported antitumor activity against h460 cell lines. Each molecule of the series was divided into seven fragments for varying substituent at the positions R1, R2, R3, R4, R5, R6 and R7 of the parent nucleus. GQSAR was performed using MLR, PCR, PLS and KNN methods of variable selection. Amongst these methods, PCR has come out with promising result as compared to other methods. A comparative docking study was performed to explore the particular sites of interactions within the binding cavity of VGEFR protein. (PDB id: 1Y6A). The important substitutions contributing towards the biological activity by interpreting the developed GQSAR equation using virtual studies were found out which are as follows. position R1 should be substituted with groups with low electro negativity and higher atomic mass, oxygen count at R5 should be increased which would act as hydrogen bond acceptors and total polar surface area at R7 has to be decreased by making substitutions of non polar groups to promote hydrophobic interactions.
32 ref
Narzari S;Sarmah J
020615 Narzari S;Sarmah J (Biotechnology Dep, Bodoland Univ, Kokrajhar-783 370, Email: jatinsarmahindia@gmail.com) : Spectroscopy and chromatography based study on mineral analysis, amino acid and fatty acid composition of Polistes olivaceus, and edible insect consumed in North East India. Indian J Nutr Diet 2017, 54(3), 302-15.
The study was aimed to analyze the mineral content, amino acid and fatty acid composition of Polistes olivaceus larvae consumed by different aboriginal tribes of North East India. Although the edible insect larvae has high market value in Assam and adjoining states of North East India, the nutritional analysis on it has not been done till now. Mineral elements including potassium, sodium, calcium, magnesium, phosphorus, zinc, iron and copper were detected by Atomic Absorption Spectroscopy. Amino acid composition and fatty acid profile were analysed by high performance liquid chromatography and gas chromatography mass spectrometry respectively to ascertain its potentiality to be included in food based strategies concerning human health. Iron and copper were the most abundant minerals and potassium, sodium and phosphorus were present in substantial amounts. Nineteen amino acids including all essential amino acids (43.87%) except isoleucine were detected in the sample. All essential amino - 121 - acids satisfied the recommended level (score
3 illus, 4 tables, 43 ref
Nandha Kumar N;Sourianatha Sundaram K; Sudhakar D;Kumar K K
020614 Nandha Kumar N;Sourianatha Sundaram K; Sudhakar D;Kumar K K (Fruit Crops Dep, Horticultural College and Research Institute, Tamil Nadu Agricultural, Coimbatore-641 003, Email: sooria@tnau.ac.in) : Improved method for inhibitor free nucleic acids from polyphenol rich leaves of Musa spp. Flora Fauna 2017, 23(1), 25-36.
Excessive presence of polysaccharides, polyphenol and secondary metabolites in banana plant affects the quality of DNA and it leads to difficult in isolating good quality of DNA. An optimized modified CTAB protocol for the isolation of high quality and quantity of DNA obtained from banana leaf tissues has been developed. In this protocol a slight increased salt (NaCl) concentration (2.0M) was used in the extraction buffer. Polyvinylpyrrolidone (PVP) and Octanol were used for the removal of polyphenols and polymerase chain reaction (PCR) inhibitors. Proteins like various enzymes were degraded by Proteinase K and removed by centrifugation from plant extract during the isolation process resulting in pure genomic DNA, ready to use in downstream applications including PCR, quantitative polymerase chain reaction (qPCR), ligation, restriction and sequencing. This protocol yielded a high molecular weight DNA isolated from polyphenols rich leaves of Musa spp which was free from contamination and colour. The average yields of total DNA from leaf ranged from 917.4 to 1860.9 ng/iL. This modified CTAB protocol reported here is less time consuming 4-5h, reproducible and can be used for a broad spectrum of plant species which have polyphenol and polysaccharide compounds.
6 illus, 1 table, 20 ref
Nalini C N;Abhinav P;Ramalakshmi N;Kiran Bhatt K;Sahini K
020613 Nalini C N;Abhinav P;Ramalakshmi N;Kiran Bhatt K;Sahini K (Pharmaceutical Analysis Dep, C. L. Baid Mehta College of Pharmacy, Jyothi Nagar, Old Mahabalipuram Road, Thoraipakkam, Chennai, Email: nalini_cn@yahoo.co.in) : Simultaneous estimation of eperisone hydrochloride and paracetamol in pharmaceutical dosage form by reverse phase HPLC and validation of the developed method. Rasayan J Chem 2017, 10(4), 1500-4.
Eperisone and paracetamol were estimated simultaneously and the developed method is validated.The principle depends on HPLC separation of the two drugs on the Phenomenex Column (150mmx4.6mm, 5μm) with a mobile phase containing Methanol: Ortho phosphoric acid (55: 45, v/v) and the flow rate being 1.0 mL/min. UV detection at 270 nm with a retention time of 2.84, 4.41 min for Eperisone hydrochloride and Paracetamol respectively. The calibration plots showed a good linear - 120 - relationship over the concentration range of 10.07-100.65μg/mL for Paracetamol, 10.08-100.83μg/mL for Eperisone hydrochloride. The method was validated for all the parameters according to International Council for Harmonisation guidelines. This method was found to be Statistically repeatable and selective for the simultaneous estimation of the two drugs in pharmaceutical dosage form. It can also be applied routine quality control of raw materials of the drugs.
2 illus, 7 tables, 15 ref
Nagam S P;Achanta G;Mandava N;Chalimadugu P; Kala S L J;Nadendla R R
020612 Nagam S P;Achanta G;Mandava N;Chalimadugu P; Kala S L J;Nadendla R R (Pharmaceutics Dep, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur, Andhra Pradesh) : Design and development of a weekly shot of injectable in-situ gel for an antipsychotic drug in the treatment of schizophrenia. Int J Res Pharm Chem 2017, 7(3), 221-31.
Injectable insitu forming depots comprise a specific class of polymeric delivery system that posess the advantages of straight forward even for sensitive molecules and ease of application as a liquid, which solidifies after application by phase separation. The paper introduces a novel type of injection temperature sensitive polymer based on insitu gel for IM delivery of Ziprasidone mesylate into systemic circulation. The drug has 100%bioavailability when administered through intra muscular route.and has less oral bioavailability when administered through the other routes inorder to increase the bioavailabilty it has been formulated in the form of injectable gel. The thermogelling polymer with different concentrations has been used for formation of insitu gel of Ziprasidone mesylate with polymer and propylene glycol as plasticizer and glutaraldehyde as cross linking agent for sustained release. The FTIR studies confirm the absence of interaction between dru g and polymer. The developed formulation were evaluated for various parameters like surface gelation temperature, drug content, spreadability, viscosity, invitro drug release studies. Among all the developed formulations F6 was found to be the best in terms of cumulative percent drug release of 98.6% along with zero order kinetics mechanism and the release of the drug lasts for seven days and fulfilled many requirements of once a week delivery system.
10 illus, 9 tables, 21 ref
Mya M M;Aung Z Z;Nwe C T;Oo A W;Htay T M; Thaung S;Maung Y N M
020611 Mya M M;Aung Z Z;Nwe C T;Oo A W;Htay T M; Thaung S;Maung Y N M (Medical Research Dep, Ministry of Health and Sport, Myanmar, No.5. Ziwaka Road, Dagon Township, Yangon Myanmar, Email: dr.mgmgmya@gmail.com) : Larvicidal, ovicidal and repellent effect of Citrus hystrix DC (kaffir lime) fruit, peel and internal materials extracts on Aedes aegypti mosquitoes. J biol Engng Res Rev 2017, 4(1), 34-43.
The present study aimed to evaluate the larvicidal, ovicidal and repellent activity of ethanol extracts of dry fruit, peels and internal fruit materials of Citrus hystrix DC against Aedes aegypti. Aedes aegypti larvae were collected from Than Byu Zayat Township Mon State and 50 each 3rd and 4th instar larvae were exposed for 24 hours in various concentrations of ethanol extracts of different parts of the Citrus hystrix fruit, done 5 replicates. The dry fruit and peels extracts resulted in significantly higher 100% mortality (P
4 illus, 2 tables, 67 ref
Muhaimin;Chaerunisaa A Y
020610 Muhaimin;Chaerunisaa A Y (Chemistry Dep, Faculty of Education, Jambi Univ, Jl. Jambi- Ma. Bulian Km 15. Kampus Pinang masak, Jambi - 36361, Indonesia, Email: muhaimin_73@yahoo.de ) : Polymer combination for parenteral drug delivery. Int J pharm Sci Res 2017, 8(5), 1993-2002.
The number of medical applications for natural or synthetic biomaterials continues to expand. One particularly interesting development concerns the use of injectable polymeric biomaterials. The forms in which the biomaterials are injected can vary from particulate matter, e.g., microspheres or irregularly shaped particles, to gels and cements that are injected in liquid form and which harden inside the body. Polymers have played an integral role in the advancement of drug delivery technology by providing controlled release of therapeutic agents in constant doses over long periods, cyclic dosage, and tunable release of both hydrophilic and hydrophobic drugs. The development of using polymer combination have attracted much attention because the biodegradation rate of the copolymer is easily controlled by altering its composition. In this review, the fundamental drug delivery systems from polymer blends including the origins and applications of polymer blend systems and polymer blend therapeutics are highlighted. The PCL microparticle-dispersed PLGA solution may be a good candidate as an injectable bulking agent. Using PCL-PLGA blend, the porous structure of the polymer blends dependent on the blend ratio under the same conditions other than the ratio. When blending PLGA with PEG, the in vitro release studies showed that the initial burst effect was dependent on the PLGA/PEG blend ratio. Moreover, the release rate increased in direct relation to PEG content. Blending PCL with poly(methacrylate) showed that the greater the poly(methacrylate) content, the less pronounced the burst effect and the more sustained the release effect. The latest developments in polymer blend capable of molecular recognition or directing intracellular delivery are surveyed to illustrate areas of research advancing the frontiers of drug delivery.
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