020559   Dubey G;Chaurasiya A (NO, Suresh Gyan Vihar Univ, Jaipur, Rajasthan) : Pharmacognostic and phytochemical screening of the aerial parts of Tephorsia purpurea (Linn.) Pers (Fabaceae). Int J Pharm Life Sci 2016, 7(6), 5099-106.

Tephorsia purpurea commonly known in Sanskrit as Sharapunkha, a highly branched, sub erect and herbaceous perennial herb. Herb is found in tropical regions and bear white to purplish flowers. According to Ayurveda, the name of "Sarwa wranvishapaka" means, property to heal all type of wounds. Whole plant and its various parts are useful as ayurvedic medicines. Medicinal uses of drug are tonic, Laxative, diuretic, bronchitis, bilious febrile attack, boils, pimples, diarrhea, gonorrhea, rheumatisim, and cures disease of heart, spleen and blood. The plant has not been explored scientifically for its pharmacological or for pharmacognostical details. Therefore, the study of morpho-anatomical characters and phytochemical analysis of Tephorsia purpurea was undertaken to establish the pharmacognostic and phytochemical details about the plant. Various parameters such as morphology, microscopy and phytochemical profiles of the aerial parts of the plant were studied and the salient diagnostic features are documented.

2 illus, 3 tables, 25 ref

020558   Dodake P;Pal M (Botany and Biotechnology Dep, Sadhu Vaswani College, Bhopal, Madhya Pradesh, Email: drmalikapal@gmail.com) : In vitro callus induction in pharmacologically significant herb: eclipta alba. Flora Fauna 2017, 23(1), 119-23.

A competent protocol was developed for in vitro plant regeneration and multiplication through callus culture of Eclipta alba. Perfect medium for callus establishment through nodal tissue was observed in 2,4-D supplemented media. The callus formed was creamish yellow in colour, showed a growth period of three to four weeks. A moderate quality callus was obtained with different gradients of BAP supplemented medium. A white to creamy callus with rapid growth was observed in the medium supplemented with NAA. Callus was subjected for multiple shoot induction.

1 illus, 6 ref

020557   Dhir S;Saffi K A;Kamalpuria N;Mishra D (NO, Indore Institute of Pharmacy, Indore, Madhya Pradesh, Email: savitadhir74@gmail.com) : Overview of In situ gelling system. Int J Pharm Life Sci 2016, 7(8), 5135-56.

Conventional liquid formulation for drug delivery shows low bioavailability because of rapid gastric emptying time from stomach/ duodenum or rapid precorneal drug loss from eye etc. Hence to improve the bioavailability of drug, In situ forming polymeric drug delivery system could be a better option. Intially they are in sol form before administered in the body, but once administered; undergo gelation in situ to form a gel. The controlled release of drug molecules via In situ forming system has a number of advantages, such as ease of administration, less complicated fabrication, less stressful manufacturing condition for sensitive drug molecules. The constant drug release may be achieved via various polymers (gellan gum, alginates, pectin, xyloglucans, PEO-PPO-PEO, poly (acrylic acid), poly (N-isopropyl acrylamide), chitosan) obeys Fick's law of diffusion which can be better explained by "egg box model". The possible mechanism from which above polymers forms In situ gel are: solvent exchange, UV- irradiation, pH change, osmotic pressure change, ionic cross linkage and temperature changes. These polymeric formulations possibly are administered by oral, rectal, ocular, vaginal, injectable and intraperitoneal routes. This article deals with the detail review of polymeric systems, their evaluation, biomedical applications, mechanism of polymer gelation, factor affecting polymers gelation, commercial formulation and their limitations.

5 illus, 3 tables, 142 ref

020556   De A;Nath S;Das A K;Bandyopadhyay S K; Banerjee M C;Mandal T K (NO, BCDA College of Pharmacy and Technology, Hridaypur, Barasat, Kolkata, Email: amartyap.col30@rediffmail.com) : Effects of Glycosmis pentaphylla leaf powder against chronic arsenicosis in rats. Int J pharm Sci Res 2017, 8(5), 2287-97.

The present study was undertaken to evaluate the effects of Glycosmis pentaphylla (GP) leaf powder against sodium arsenite (NaAsO2) induced toxicosis in adult albino rats. Forty eight albino rats having body weight 150-200 gm of either sex were randomly divided (equally) into four groups viz., I₀, I₁, I₂, I₃. Sodium arsenite was administered at 4mg/kg body weight daily in drinking water for 90 days to all rats of groups I₁, I₂ and I₃. The rats of group I₂ - 93 - and I₃ were orally treated with leaf powder of G. pentaphylla at 500mg/kg and 250mg/kg (1/10th of and 1/20th of LD₅₀) daily from 91st day to 120th day. Distilled water was given to rats of I₀ for 120 days and rats of I₁ for 91st day to 120th day. Blood samples were collected at different days for analysis of haemogram, biochemical parameters like ALT, AST, BUN and CRT. Tissue samples were collected to study activity of SOD, MDA, GSH, catalase and histopathology was conducted after completion of experiment. The results reveal that the G. pentaphylla leaf powder may mitigate the arsenicosis in rats at dose dependent manner and in future may be used to reduce or to prevent arsenic toxicity in human.

34 ref

020555   Dattani B J;Patel N k;Patel A B;Vyas A J; Patel A I (Quality Assurance Dep, B. K. Mody Government Pharmacy College, Polytechnic campus, Near Aji dam, Rajkot-360 003) : Development and validation of stability indicating HPLC method for estimation of pargeverine hydrochloride in pharmaceutical dosage form. Pharma Sci Monit 2017, 8(2), 10-23.

A simple, sensitive and specific stability indicating high performance liquid chromatographic (HPLC) method for the estimation of Pargeverine Hydrochloride was developed and validated. Pargeverine Hydrochloride was separated and quantified using stainless steel column (25 cm <126> 4.0 mm) packed with end-capped octadecylsilyl silica gel for chromatography (5 μm) (Nucleosil C18 is suitable) OR Equivalent, using a mixture of Acetonitrile: Methanol: 1% Ammonium Acetate pH 4.5 (40:40:20v/v/v) and at a flow rate of 1.0 ml/min. Quantification was achieved with an UV detector at 252 nm over the concentration range of 7.5.45 μg/ml. The applied HPLC method allowed the separation and quantification of Pargeverine Hydrochloride with good linearity (r²=0.999) in the studied concentration range. The method was validated as per the International Conference on Harmonization (ICH) guidelines. Pargeverine Hydrochloride stock solution was subjected to different stress conditions. The degraded product peaks were well resolved from the pure drug peak with significant difference in their retention time values. Stressed samples were assayed using developed HPLC method. Statistical analysis of the data showed that the method is precise, accurate, reproducible, and selective for the analysis of Pargeverine Hydrochloride. The method was successfully applied to the estimation of Pargeverine Hydrochloride in Oral Solution dosage form.

18 ref

020554   Damle M C;Bandal P;Kale S;Rao S (Quality Assurance Dep, AISSMS College of Pharmacy, Kennedy Road, Near R.T.O, Pune-411 001) : HPTLC estmation and antibactrial effect of methanolic extract of S. nux vomica seeds under accelerated storage codition. Pharma Sci Monit 2017, 8(2), 69-76.

Strychnos nux vomica seeds (L.) (Loganaceae) commonly known as "Kuchla" is widely used in Ayurveda.The main active constituents present in S.nux vomica seeds are Strychnine and Brucine. S.nux vomica seed is official in Ayurvedic pharmacopeia of India. The HPTLC method involves estimation of Strychnine and Brucine from S.nux vomica seeds extract exposed to accelerated storage condition for a period of 6 months. The antibacterial activity of Methanolic extract of dried seeds of S.nux vomica seed was determined by broth method against Gram- Positive bacterial strain (Staphylococcus aureus) and - 92 - Gram-negative bacterial strain (Escherichia coli). For HPTLC method, the active markers STR, BRU and extract was spotted on the plates precoated with silica gel 60 F₂₅₄ and developed using toluene: ethyl acetate: triethyl amine (8.5:0.5:2v/v/v) as mobile phase. Densitometry analysis was carried out at 215 nm. The method showed high sensitivity with good linearity over the concentration range of 500-2500ng/band. The peak for Strychnine and Brucine were observed at Rf of 0.23 ±0.02 and 0.14±0.02 resp. The aim of our study was to observe the effect of accelerated storage on assay of pure markers and markers in the extract. The analysis was carried out at 1,2,3,6 months study as per ICH guidelines for stability testing of drug at storage condition of 40°C ± 2°C/75% RH ± 5% RH.

13 ref

020553   Condurso C;Cincotta F;Tripodi G;Verzera A (Chemical Dep, Messina Univ, Biological, Pharmaceutical and Environmental Sciences, Messina, Italy, Email: fabcincotta@unime.it) : Bioactive volatiles in sicilian (South Italy) saffron: safranal and its related compounds. J essential Oil Res 2017, 29(3), 221-7.

Sicilian saffron is cultivated mainly in the province of Enna, although cultivation is spreading slowly throughout the region. Volatile constituents which are fundamental for saffron aroma were determined. A large number of volatile compounds were identified using HS-SPME and GC-MS. Safranal, safranal isomer, isophorones, α-cyclocitral, and β-cyclocitral were also quantified. A high amount of safranal resulted in the samples; moreover, of interest was the amount of safranal isomer and a-isophorone. The results allowed to consider Sicilian saffron of high commercial quality. It is an important source of bioactive compounds for the amount of safranal and related compounds, which are important for its aroma and relevant to human health too.

1 illus, 2 tables, 34 ref

020552   Choudhury D;Gairola B;Roy D;Sikidar P (Pharmacology Dep, Silchar Medical College and Hospital, P.O. Ghongoor-788 014, Email: drdevarsi@gmail.com) : Evaluation of analgesic activity of aqueous extract of Aloe vera [AEAV] in albino wistar rats. Int J pharm Sci Res 2017, 8(4), 1850-7.

Aloe vera has been used since ages to manage a number of diseases causing pain, inflammation and fever. However, its effectiveness has not been scientifically certified. NSAIDs & Opioid are used continuously for the pain management. Alternative analgesics are needed to escape from the serious adverse effects of NSAIDs. Our study demonstrated significant analgesic activity of Aloe vera at doses of 200 mg/kg and 500 mg/kg. The study was carried out using Wistar Albino rats (150-200gm). Soxhlets apparatus was used to prepare the aqueous extract of Aloe vera [AEAV]. The animals were divided into 4 groups (n=6) receiving different treatments. Hot plate method, acetic acid induced writhing method and tail flick tests were used. The results were subjected to statistical analysis by using one way ANOVA followed by Dunnett's test. Analgesic effect of high dose of AEAV at 500 mg/kg was similar with the standard drug indomethacin. The extract (200 & 500 mg/kg) exhibited a dose-dependent inhibition of writhing and also showed a significant (P <60> 0.001) inhibition in the hot plate method. The results indicate that the analgesic effect of AEAV is mediated both by central and peripheral mechanism.

17 ref

020551   Chemate S Z;Bothe Prinyka S (Pharmaeutics Dep, PDVVPF's College of Pharmacy, Vilad Ghat, Ahmednagar, Maharashtra) : Formulation and evaluation of losartan potassium Bi-layer buccal tablet using mucoadhesive polymer. Int J pharm Sci Res 2017, 8(6), 2624-30.

In the present study, an attempt was made to design and evaluate mucoadhesive bilayer tablet of losartan potassium (angiotensin II receptor antagonist), in order to overcome bioavailability problems, to reduce dose dependent side effects and frequency of administration. The losartan potassium mucoadhesive buccal tablet were prepared by wet granulation method using chitosan as a mucoadhesive polymer to prolong the drug release and to avoid first pass metabolism. The prepared Mucoadhesive buccal tablets were evaluated by pre and post compression parameter. Precompression test like bulk density, tap density, angle of repose and post compression test include thickness, hardness, friability, weight variation, drug content, disintegration time, wetting time, surface pH, in-vitro drug release and ex-vivo mucoadhesive time. The drug excipients compatability was evaluated by DSC studies.

6 illus, 4 tables, 21 ref

020550   Chauhan D;Koradia H (Pharmaceutics and Pharmaceutical technology Dep, L.M. College of Pharmacy, Ahmedabad, Gujarat-380 009) : Formulation, development and evaluation of immediate release tablet of loperamide HCl. Pharma Sci Monit 2017, 8(2), 435-47.

The aim of the research work was to prepare Immediate Release tablet of Loperamide HCl in order to provide quick relieve to the patient suffering from chronic diarrhoea. Preliminary trials were carried out for the selection of diluent, super disintegrant and solubilizing agent. FTIR study revealed drug- excipients compatibility.The calibration curve was obtained for LoperamideHCl in methanol and 0.1N HCl. The Immediate release tablets were prepared using direct compression method. The Immediate Release tablet with 8 mg of sodium starch glycolate and 20 mg of PEG 6000showed 97.78±0.05% release in 60 min in 0.1 N HCl.The developed Immediate Release tablet of LoperamideHCl will be helpful in curing chronic diarrhoea with improved patient compliance.

19 ref

020549   Chaudhari P R;Gajera V;Shah D P (Pharmacology Dep, Shree Naranjibhai Lalbhai Patel College of Pharmacy, Umrakh, Bardoli) : Evaluation of antiulcer activity of aqueous extract of Albizzia lebbeck Benth. leaves in rats. Pharma Sci Monit 2017, 8(2), 674-96.

Objective was to evaluate the Antiulcer activity of aqueous extract of Albizzia lebbeck Benth. leaves against Ethanol and Cysteamine HCL. induced Peptic Ulcer in rats. Antiulcer assays were performed using the protocols of ulcer induced by Ethanol and Cysteamine HCL. The aqueous extract of Albizzia lebbeck. Benth leaves were administered at doses 200 and 400 mg/kg.Omeprazole (20 mg/kg) was used as standard drug. Various parameters like ulcer index, SOD, MDA and CAT were also determined. Preliminary phytochemical investigation revealed the presence of Alkaloids, Saponins, Tannin, Phenolic compound and flavanoids. Pretreatment with omeprazole reduced the ulceration in - 90 - ethanol and Cysteamine HCL induced models. AQAL at dose of 200 and 400 mg/kg inhibited ulcer formation in both models. However it was less compare to omeprazole. Oxidative stress marker (MDA) levels were found to be (11.45±0.241 mmole /gm of gastric tissue x 10^-4) in the ethanol control group, which decreased to (10.04 ± 0.098 mmole /gm of gastric tissue x 10^-4), (9.493±0.318 mmole/gm of gastric tissue x 10^-4) in the AQAL group 200 mg/kg and 400 mg/kg respectively. Antioxidant parameters SOD and CAT activity were reduced significantly in the ethanol and Cysteamine HCL induced ulcerated group. Oral pretreatment with AQAL (200 and 400 mg/kg) significantly increased the SOD and CAT levels in both models. The histopathological study of the stomach and duodenum tissue also supported the above results. Overall data from our experimental studies suggest that aqueous extract of Albizzia lebbeck Benth. Leaves possess significant antiulcer activity and these actions of AQAL can be attributed to the phyto constituents like flavonoids, saponins tannins present in it.

21 ref

020548   Chatterjee A;Singh N;Abraham J (Microbial Biotechnology Laboratory, School of Biosciences and Technology, VIT Univ, Vellore-632 014, Email: jayanthi.abraham@gmail.com) : Mycoremediation of textile dyes using Talaromyces funiculosum JAMS1. Int J pharm Sci Res 2017, 8(5), 2082-9.

The present study was planned with the aim to remove various dye decolorization using fungal strains. The fungi was isolated from soil samples collected from waste disposal areas and agricultural fields. Nine isolates were initially selected for testing their decolorization potential in the liquid medium. Three most effective strains were used to study the decolorization of four different dyes i.e Reactive Red, Navy Blue HER, Reactive Magenta B and Orange 3R. The strain belonging to Talaromyces funiculosum (M2F) was found to be the most potent strain. More than 70% decolorization was observed under optimal incubation conditions of temperature and pH. Overall, the dye decolorization was maximum at 250 mg/L dye concentrations at pH 5-6 under continuous shaking conditions. The culture conditions like pH, temperature, inoculum size and NaCl concentrations were also found effective in decolorization efficacy of the fungal strain which was studied using Response surface methodology (RSM) with Minitab 16 software. Qualitative and quantitative assays for determining the production of lignolytic enzymes such as laccases and peroxidises by the fungal strains were studied and a comparison of degraded and undegraded forms of the dye were done by using analytical techniques like FTIR, UV Vis spectroscopy and GCMS.

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020547   Chakraborty S;Bhattacharjee P (Food Technology and Biochemical Engineering Dep, Jadavpur Univ, Kolkata-700 032, Email: pb@ftbe.jdvu.ac.in) : Supercritical carbon dioxide extraction of melatonin from Brassica campestris: in vitro antioxidant, hypocholesterolemic and hypoglycaemic activities of the extracts. Int J pharm Sci Res 2017, 8(6), 2486-95.

Brassica campestris Linn. (yellow mustard), a common Indian condiment, possesses melatonin as an important antioxidant. Optimization of supercritical carbon dioxide extraction (SC-CO₂) process parameters was conducted to obtain an extract having the best combination of yield of melatonin and maximum in vitro hypoglycaemic and hypocholesterolemic activities, along with a desirable balance of ω6 to ω3 fatty acids. A full factorial design and response surface methodology were employed for process optimization. Melatonin content of the extracts was obtained by high performance liquid chromatography and by liquid chromatography-mass spectrometry. The optimized extraction conditions were obtained at 300 bar, 50 °C for 120 min. This extract exhibited highest content of melatonin (660.72±41.05 ng/g of dry mustard powder), maximum in - 89 - vitro hypocholesterolemic (60.11±3.89%) and hypoglycaemic (59.70±2.67μg/ml) activities and possessed minimum ω6 to ω3 (1.29) ratio with minimum erucic acid content (2.00±0.20 g/100g of fatty acid). The electron paramagnetic resonance spectroscopy of the extract (0.10±0.001 g/ml) showed 72.10±4.01% scavenging activity of DPPH radicals, establishing its strong antioxidant potency. A new Chrastil equation was developed to compute solubility of melatonin in SC-CO₂ under different extraction conditions. The SC-CO2 extract of yellow mustard seeds could have promising use as a natural source of melatonin as well as of balanced ω6 to ω3 fatty acids.

3 illus, 4 tables, 17 ref

020546   Bijauliya R K;Jain S K;Alok S;Dixit V K;Singh V K;Singh M (Institute of Pharmacy, Bundelkhand Univ, Jhansi-284 128, Email: rkpharma3791@gmail.com) : Macroscopical, microscopical and physico-chemical studies on leaves of Dalbergia sissoo Linn. (fabaceae). Int J pharm Sci Res 2017, 8(4), 1865-73.

This is to rationalize the macroscopial, anatomical and physico-chemical studies on leaves of plant Dalbergia sissoo Linn. (Fabaceae). The crude ethanolic extract of leaves of Dalbergia sissoo Linn. (Fabaceae) was using physico-chemical parameters, fluorescence analysis, and preliminary phytochemical investigation (TLC, HPTLC, column chromatography). An attempt has been made to highlight this folk herbal medicine through present study which will assist in the identification of fresh as well as dried crude samples of leaves anatomically and physiochemically. TLC fingerprint profiling and fluorescence analysis of powdered leaves were also carried out and the salient qualitative and quantitative parameters are reported. The present study will provide referential information for correct identification and help in checking adulteration in market samples used in the preparation of various herbal medicines. The present observation will also be helpful in macroscopical, microscopical and physiochemical studies on leaves of Dalbergia sissoo Linn.(Fabaceae).

12 ref

020545   Bijauliya R K;Alok S;Singh M;Mishra S B (Pharmacognosy Dep, Bundelkhand Univ, Jhansi-284 128, Email: rkpharma3791@gmail.com) : Morphology, phytochemistry and pharmacology of Syzygium cumini (Linn.)-An overview. Int J pharm Sci Res 2017, 8(6), 2360-71.

Syzygium cumini (L.) is a - 88 - widely used medicinal plant for the treatment of various ailments. The plant contains anthocyanins, glucoside, ellagic acid, isoquercetin, kaempferol, and myricetin as its chief active constituents. These active cons isoquercetin, kaempferol tituents impart multiple pharmacological activities to the plant which includes antidiabetic, anticancer, antioxidant, antibacterial, antifungal and antidiarrhoeal activity. The present review presents specific information on botany, phytochemical constituents, traditional uses and pharmacological actions of S. cumini (L.). Further applications of Syzygium cumini (L.) in the field of novel drug delivery has been also elaborated in the review. Apart from its application in the treatment of various diseases there is need to explore chemical and toxicity concern of S. cumini (L.).

7 illus, 84 ref

020544   Bhayani S;Chavda J R;Dudhrejiya A (Pharmaceutical Sciences Dep, Saurashtra Univ, Rajkot-360 005) : Development and validation of first order derivative spectrophotometric method for simultaneous estimation of cefpodoxime proxetil and levofloxacin hemihydrate in combined tablet dosage form.. Pharma Sci Monit 2017, 8(2), 520-6.

A Simple, accurate, precise and sensitive first order derivative spectrophotometric method was developed and validated for the determination of cefpodoxime proxetil and levofloxacin hemihydrate in combine tablet dosage forms. First order derivative spectrophotometric method is adopted to eliminate spectral interference. Cefpodoxime proxetil and levofloxacin hemihydrate have λ_max at 237 nm and 300 nm respectively in methanol in water solvent. The method was found to be linear and obeys beer's law in concentration range of 5 - 30 μg/ml for both cefpodoxime proxetil and levofloxacin hemihydrate. The developed method was validated as per ICH guidelines.

13 ref

020543   Bhatnagar P;Vyas D;Sinha S K;Gajbhiye A (Chemistry Dep, Sir Padampat Singhania Univ, Bhatewar, Udaipur-313 601, Email: prasoon.bhatnagar@spsu.ac.in) : HPLC method for estimation of drug release of entacapone in entacapone, levodopa and carbidopa tablets. Int J pharm Sci Res 2017, 8(4), 1734-43.

Today's generic drugs manufacturing industry need robust analytical methods for analysis of generic drug products to provide best quality pharmaceutical formulation. Entacapone, Levodopa and Carbidopa tablets is such a product which is used for the treatment of Parkinson's disease. This paper presents a robust HPLC method that has been developed for estimation of % drug release of Entacapone in this multi component drug formulation. HPLC column used for separation was Cosmosil 5PE-MS 150mm x 4.6 mm with 5 micron particle size. Combination of phosphate buffer pH 2.5, acetonitrile and methanol was used for mobile phase in isocratic mode with UV detection at 280 nm. The method was validated to ensure suitability of the method for quantitative determination of % drug release of Entacapone in presence of Levodopa and Carbidopa in this triple drug combination pharmaceutical formulation. Proposed method was found to be specific, precise, robust, accurate and linear in range 0.066 to 0.33 mg/mL of Entacapone.

17 ref

020542   Bhat Z A;Gani R;Zargar M I (Pharmaceutical Sciences Dep, Pharmacognosy Div, Kashmir Univ, Hazratbal, Srinagar-190 006) : GC-MS analysis, antibacterial and antifungal activity of essential oil of Bunium persicum from Kashmir, India. Int J Res Pharm Chem 2017, 7(1), 39-44.

This work was carried out to evaluate chemical composition, antibacterial and antifungal activity of Bunium persicum essential oil. The oil was extracted by hydrodistillation which was analysed through GC-MS. The antibacterial and antifungal activity was evaluated by Agar well diffusion method and Minimum inhibitory concentration (MIC) was evaluated by Agar dilution method. P cymene, Gamma terpinene and cumic aldehyde were the major constituents present in the oil. The oil showed significant antibacterial and antifungal activity.

5 illus, 5 - 87 -

020541   Batoro J;Ekowati G (Biology Dep, Faculty of Mathematics and Natural Sciences, Brawijaya Univ, Jl. Veteran Malang, East Java, Indonesia, Email: jati_batoro@yahoo.co.id) : Ethnobotanical tobacco (Nicotiana tabacum L.) in Indonesia. a review. Adv Life Sci 2017, 7(2), 26-9.

Tobacco plants (Nicotiana tabacum L.) have important role to supports economical local people, development, agricultural and absorbing labors in Indonesia. How to suppress nicotine content that includes as harmful components in the study of high biotechnology. The collected data were supported bases references and survey. Tobacco uses are having an excellent significance in supporting socio-cultural ties, especially indigeous ancestors in strengthening the unity of society in Indonesia. Thus, tobacco product also has negative effects for human's health. So that, it is requires right solution to solve the problem toward that tobacco product.

1 table, 14 ref

020540   Ayari H;Bricca G (NO, Universite Lyon1, INSERM, ERI22, EA 4173, Lyon, France, Email: hananeayari@yahoo.fr) : Microarray based identification reveals arterial angiotensin system expression in human. Int J pharm Sci Res 2017, 8(6), 2452-7.

Authors studied by microarray analysis the tissue angiotensin system organization. Also elucidated the expression of chymase, cathepsins D, G and angiotensin-converting enzyme (ACE), potentially involved in intraparietal angiotensin II formation and atheroma. mRNA gene expression was measured by an Affymetrix Gene Chip Human Gene 1.0 ST arrays (Affymetrix, Santa Clara, CA, USA) using RNA prepared from 68 specimens of endarteriectomy from 34 patients. The studied mRNAs could be measured in all patients. ACE mRNA was increased 1.2 fold (p=1.21E-07) in atheroma. A 1.4 fold increase in cathepsin D mRNA (p=2.53E-07) was observed in atheroma plaque. Concerning chymase and cathepsin G, 1.22 and 1.24 fold change (p=0.001) were observed respectively. Angiotensin type 1 receptor (AT1R) mRNA was decreased 0.7 fold (p=2.74E-06) in atheroma compared to intact tissue. All components required for angiotensin II formation are expressed locally in the arterial wall. The genes expression showed clear changes in ATH compared to MIT by enhancing the involvement of genes associated with Ang II production. Over expression of ACE and cathepsin D may lead to angiotensin II overproduction and contribute, to the lower amount of AT1R in atheroma. Although further evidence is needed, our results support previous data.

1 illus, 2 tables, 25 ref

020539   Aver G M;Mottin V H M;Kreutz O C;Suyenaga E S (NO, Universidade Feevale, ERS-239, 2755, Vila Nova, 93525-000, Novo Hamburgo-RS, Brazil) : Genesis of pharmaceuticals: from prontosil rubrum to antipsychotics-a history of sulfa drugs from the perspective of medicinal chemistry. Int J Res Pharm Chem 2017, 7(3), 306-19.

Based on research conducted on dye Prontosil Rubrum, it was possible to obtain the first synthetic bacteriostatic, the sulfas, which present sulfanilamide as its pharmacophore. This prototype made possible to obtain pharmaceuticals of different pharmacological classes, such as diuretics, hypoglycemiants, anti-inflammatories, antipsychotics, anti-leprosy drugs and antiadrenergics. This paper intends to report, through a bibliographic review, the structural alterations that characterize the different therapeutic classes of sulfanilamide derivatives, through chemical structure versus pharmacological activity relationship analysis. As a result, it was observed that some chemical groups are essential to define the pharmacological action. Diuretic drugs derived from sulfanilamide present groups of benzothiazide, thiadiazole and associated to sulfamoylbenzoic acid in their chemical structure. As for hypoglycemiants, they present the group sulfonylurea in their chemical structure. In the chemical structure of oxicams, there is cyclization of the pharmacophore, - 86 - 4-hydroxy-2-methyl-1,2-benzothiazine-3-carboxamide-1,1-dioxide. The coxibs present in their chemical structures two aromatic rings linked by a furan or trifluoromethyl pyrazole ring, the antipsychotics show the group N-(pyrrolidin-2-yl)-sulfonylbenzamide. Thus, it is clear that through knowledge of Medicinal Chemistry, and only one prototype, it was possible to obtain several important drugs for therapeutic throughout history.

25 illus, 35 ref

020538   Ansary A A;Uddin I;Khan M I (Biochemical Sciences Div, National Chemical Laboratory, Dr. Homi Bhabha Road, Pune-411 008, Email: nmansary@gmail.com) : Biomimetic synthesis of CdSe nanoparticles with potential bioimaging applications. Int J pharm Sci Res 2017, 8(6), 2526-32.

This study presents in vitro biomimetic synthesis of CdSe nanoparticles using the enzyme, NADPH dependent-Nitrate reductase purified from fungus, Fusarium oxysporum. The synthesis of CdSe nanoparticles was accomplished in the presence of a synthetic peptide having amino acid sequence (γ-Glu-Cys-Glu-Cys)-Gly, which acted as binding molecule. The nanoparticles were synthesized in the size range of 3.9-9.0 nm was analysed using TEM. Further characterization of nanoparticles was done using techniques such as UV, PL, XPS, and FTIR. The as-synthesized CdSe nanoparticles were water dispersible containing free reactive amino groups. These CdSe nanoparticles were conjugated with bi-antennary and tri-antennary glycopeptides opening up the possibilities for their applications in bioimaging. These significant observations will help better understand the mechanism of biosynthesis of fluorescent nanoparticles using fungi. These findings promise an alternative strategy for an eco-friendly, economical, and large-scale synthesis of water dispersible CdSe nanoparticles. These CdSe nanoparticles have promising biomedical-imaging applications without a need for further functionalization.

5 illus, 24 ref

020537   Andika A;Mentari M P;Dewanti M C;Hertiani T; Pratiwi S U T (Pharmaceutical Biology Dep, Faculty of Pharmacy, Gadjah Mada Univ, Sekip Utara, Yogyakarta 55281, Indonesia, Email: sylvia_pratiwi@ugm.ac.id) : Essential oils effect in combination with antibiotics against Staphylococcus aureus ATCC 29213 biofilm susceptibility. Int J pharm Sci Res 2017, 8(4), 1606-12.

Staphylococcus aureus biofilm has been known as one inducing factor for the bacteria's resistance to various antibiotics. One strategy which may increase the efficacy of the antibiotic is by combining the antibiotic therapy with antiinfective from natural resources. This research was evaluating the potency of three known antiinfective essential oil derived from leaves of Piper betle L., Ocimum basilicum L. forma citratum Back and Cymbopogon citratus L., in a combination with antibiotics i.e. chloramphenicol, streptomycin, and erythromicin towards S. aureus ATCC 29213. The essential oils were obtained by steam-hydrodistillation of the fresh raw materials. Microdillution technique combined with colorimetric was used to determine the biofilm inhibition. Crystal violet was used for biofilm - 85 - staining of which the reading was performed on a microplate reader. Fractional Inhibitory Concentration Index (FICI) values was evaluated based on the comparison of % inhibitory obtained from the essential oils and the antibiotics in a single and in a combination. The essential oils alone has the PMIC50 (planktonic) values as follows, 0.2% (P. betel), 0,3% (C. citratus) and 0.84% v/v (O. basilicum). However, all essential oils has FICI values of <62> 2 indicates that instead of causing a synergistic effect, the essential oils seems to be antagonist to the antibiotics' biofilm formation inhibition activities.

26 ref

020536   Al-Khafaji Z;Al-Samaree M (Institute of Genetic Engineering and Biotechnology for Postgraduate St, Baghdad Univ, Iraq, Email: zahranasserk@gmail.com) : Design of synthetic antimicrobial peptides against resistant acinetobacter baumannii using computational approach. Int J pharm Sci Res 2017, 8(5), 2033-9.

Acinetobacter baumanniiis typically coccobacillus Gram-Negative bacterium, resists almost all antibiotics in use. Synthetic antimicrobial peptides (AMPs) against this bacterium were designed with the aid of computational software and databases to be with the accepted models. Antimicrobial peptides (AMPs) might be the candidate solution for the this problems. Four peptides designated MY1, MY2, MY3 and MY4 were synthesized with length 11-14 amino acids, they were rich in Arginine and Tryptophan. The MICs of the peptides against colistin sensitive A. baumannii were 2.4, 6.2, 6.9, 6.6 μg/ml (mean for 10 strains) respectively vs Mastoparan as control was 10.4 μg/ml, whereas the MICs of peptides against colistin resistant A. baumannii were 3.8, 6.2, 6.8, 6.4 μg/ml (mean for 10 strains) respectively vs Mastoparan 13.6 μg/ml. The designed peptides showed no hemolytic activity at effective MICs. The practical calculated Therapeutic Index were 141.7, 67.7, 60.9, 77.3 vs 7.7 for Mastoparan (Colistin sensitive strains) and for resistant strains were 89.5, 67.7, 61.8, 79.7 vs Mastoparan 5.9.

31 ref

020535   Abhishek Kumar;Tiwari B K (NO, NKBR College of Pharmacy and Research Centre, Meerut-250 004, Email: pharma.abhishek@yahoo.co.in) : Formulation and development of gastro-retentive floating drug delivery system of curcumin for stomach tumors and ulcer. Int J pharm Sci Res 2017, 8(5), 2149-60.

Objective was to prepare and evaluate floating tablet of curcumin for prolonged gastric residence time and increased drug bioavailability for the treatment of gastric problem. Floating tablet were prepared by wet granulation method using different ratios of Curcumin, Psyllium husk, HPMC K 15 M, HPMC K 100 M and Mangifera indica gum. The respective powders were blended thoroughly and a dump mass was prepared by adding the granulating agent. Dump mass was passed through sieve number 10 and dried in hot air oven at 50 °C for 30 mins. After drying, granules were further - 84 - passed through sieve number 22 to attain the uniformity in granules. Finally, optional additives like magnesium stearate and talc were added and finely blended for preparation of floating tablet. Floating drug delivery tablets were being formulated and the present study focused on the formulation of FDDS by using different polymes like phyllium husk, HPMC K 100 and HPMC K15 and to evaluate its efficacy in reducing ulcers caused by H.pylori. The Floating drug delivery tablets were characterized for their weight variation, hardness, friability, drug content determination, disintegration, in-vitro dissolution studies, IR, floating lag time, swelling studies and erosion studies. The developed curcumin floating tablet system is a promising floating drug delivery system for oral sustained administration of curcumin.

28 ref

020534   Abbas N;Naz M;Alyousef L;Ahmed E S;Begum A (Medicinal Chemistry Dep, Qassim Univ, College of Pharmacy, Qassim-54152, KSA, Email: nhd_abbas@rediffmail.com) : Comparative study of hepatoprotective effect produced by Cuminum cyminum, fruits of Phyllanthus emblicus and silymarin against cisplatin-induced hepatotoxicity. Int J pharm Sci Res 2017, 8(5), 2026-32.

Cisplatin is a cytotoxic drug which induced the hepatotoxicity in the albino mice when intra-peritoneally administered at the dose of 10mg/kg. Administration of cisplatin raised the level of LFT's enzymes and also reduced the level of antioxidant enzymes in the liver of the mice. Administration of Cuminum cyminum, Phyllanthus emblicus extract and silymarin remarkably showed the hepatoprotective effect in the albino mice. Administration of C. cyminum, P. emblica and silymarin decreased the level of ALT, AST, and ALP along with increasing the level of Total protein content. It also increased the level of antioxidant enzymes in the liver of mice showing its hepatoprotective activity. We found C. cyminum has a better hepatoprotective effect than P. emblica.

30 ref

019641   Zhou S;Liu B;Meng J (Automation Dep, Guangdong Univ of Technology, Guangzhou, People's Republic of China) : Quality evaluation of raw moutan cortex using the AHP and gray correlation-TOPSIS method. Pharmacog Mag 2017, 13(51), 528-33.

Raw Moutan cortex (RMC) is an important Chinese herbal medicine. Comprehensive and objective quality evaluation of Chinese herbal medicine has been one of the - 131 - most important issues in the modern herbs development. Objective was to evaluate and compare the quality of RMC using the weighted gray correlation- Technique for Order Preference by Similarity to an Ideal Solution (TOPSIS) method. The percentage composition of gallic acid, catechin, oxypaeoniflorin, paeoniflorin, quercetin, benzoylpaeoniflorin, paeonol in different batches of RMC was determined, and then adopting MATLAB programming to construct the gray correlation-TOPSIS assessment model for quality evaluation of RMC. The quality evaluation results of model evaluation and objective evaluation were consistent, reliable, and stable. The model of gray correlation-TOPSIS can be well applied to the quality evaluation of traditional Chinese medicine with multiple components and has broad prospect in application.

2 illus, 6 tables, 20 ref

019640   Zhou J;Sun Y Y;Sun M Y;Mao W A;Wang L;Zhang J;Zhang H (Dermatology Dep, Seventh People's Hospital of Shanghai Univ of TCM, Shanghai 200137, China) : Prim-O-glucosylcimifugin attenuates lipopolysaccharide- induced inflammatory response in RAW 264.7 macrophages. Pharmacog Mag 2017, 13(51), 378-84.

Radix Saposhnikoviae (RS) exerts anti-inflammatory, analgesic, antipyretic, antioxidation effects and has been used in traditional Chinese medicine to treat common colds, headache, and rheumatoid arthritis. Prim-O-glucosylcimifugin (POG) is the highest content chromone and one of the major active constituents in RS. The study was aimed to explore the anti-inflammation effects of POG in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. Cell viability was detected by Cell Counting Kit-8 assay. Production of nitric oxide (NO), tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), and IL-6 was assessed by enzyme-linked immunosorbent assay. Real-time polymerase chain reaction and Western blot were performed to analyze mRNA and protein levels, respectively. During the whole experiment, 15, 50, and 100 μg/mL of POG had no cytotoxicity on RAW 264.7 cells. POG dose-dependently inhibited the production of NO, TNF-α, IL-1β, and IL-6 that were induced by LPS. POG treatment downregulated the mRNA and protein expression inducible NO synthase (iNOS) and cyclooxygenase 2 (COX-2) in LPS-activated RAW 264.7 macrophages in a concentration-dependent manner. Furthermore, LPS-induced JAK2/STAT3 activation was prevented in RAW 264.7 macrophages by POG treatment. STAT3 overexpression significantly reversed the effects of POG on LPS-activated RAW 264.7 macrophages. These results demonstrate that POG exerts anti-inflammatory effects through the inhibition of iNOS and COX-2 expression by inhibiting the phosphorylation of JAK2/STAT3.

5 illus, 32 ref

019639   Zhang H;Wang X;Li R;Sun X;Sun S;Li Q;Xu C (College of Food and Biological Engineering, Zhengzhou University of Light Industry, Zhengzhou, Henan, P.R. China) : Preparation and bioactivity of exopolysaccharide from an endophytic fungus Chaetomium sp. of the medicinal plant gynostemma pentaphylla. Pharmacog Mag 2017, 13(51), 477-82.

Many exopolysaccharides from the endophytes in medicinal plants possess various potential bioactivities. The endophytic fungus JY25 was isolated from the leave of the Chinese medicinal plant Gynostemma pentaphylla and identified as Chaetomium sp. by its phylogenetic and physiological analysis. One exopolysaccharide (EPS) fraction was isolated from the fermentation broth by ethanol precipitation and - 130 - purified by gel filtration chromatography on Sepharose CL-6B. The molecular characteristics were examined by GC-MS, FT-IR, and multiangle laser light scattering (MALLS). The monosaccharide composition analysis indicated that the purified EPS was mainly composed of glucose, mannose, arabinose, and galactose with the molecular ratio of 78.29: 8.99: 8.64: 4.08. FT-IR spectral analysis of the purified EPS revealed prominent characteristic groups, such as carbonyl bond, pyranose ring, and so on. The weight-average molar mass and the polydispersity ratio of the EPS were revealed to be 1.961x10⁴ g/mol and 1.838, respectively. Furthermore, thermo gravimetric analysis (TGA) indicated that the degradation temperature of the purified EPS was 305°C. The purified EPS from the endophytic fungus Chaetomium sp. displayed antioxidant and antiproliferative activities. The results demonstrated that the EPS could be used as a healthful food and material source in pharmaceutical industries.

7 illus, 2 tables, 29 ref

019638   Zhang H L;Zhang H (Bone and Joint Dep, The First Affiliated Hospital of PLA General Hospital, Fucheng Road, H, ) : Withaferin-a induces apoptosis in osteosarcoma U2OS cell line via generation of ROS and disruption of mitochondrial membrane potential. Pharmacog Mag 2017, 13(51), 523-7.

Withaferin-A (WF-A) is a well-known dietary compound isolated from Withania sominifera. It has tremendous pharmacological potential and has been shown to exhibit antiproliferative activity against several types of cancerous cells. Currently, the main focus of anti-cancer therapeutic development is to identify apoptosis inducing drug-like molecules. Osteosarcoma is a rare type of osteocancer, affecting human. The present study therefore focused on the evaluation of antitumor potential of WF-A against several osteosarcoma cell lines. MTT assay was used to evaluate WF-A against osteosarcoma cell lines and to calculate the IC₅₀. DAPI staining was used to confirm the apoptosis inducing potential of WF-A. Mitochondrial membrane potential, reactive oxygen species (ROS) assay, and Western blotting were used to confirm the basis of apoptosis. The results revealed that that WF-A exhibited strong antiproliferative activity against all the cells lines, with IC₅₀ ranging from 0.32 to 7.6 μM. The lowest IC₅₀ (0.32 μM) was observed against U2OS cell line and therefore it was selected for further analysis. DAPI staining indicated that WF-A exhibited antiproliferative activity via induction of apoptosis. Moreover, WF-A induced ROS-mediated reduction in mitochondrial membrane potential Δψm) in a dose-dependent manner and activation of caspase-3 in osteosarcoma cells. We propose that WF-A may prove a potent therapeutic agent for inducing apoptosis in osteosarcoma cell lines via generation of ROS and disruption of mitochondrial membrane potential. Abbreviations used: WA: Withaferin A; ROS: Reactive oxygen species; OS: Osteosarcoma; MMP: Mitochondrial membrane potential.

3 illus, 1 table, 36 ref

019637   Zeng Z;Li X;Zhang S;Huang D (NO, State Key Laboratory of Ecological Applied Technology in Forest Area o, Changsha 410004 China) : Characterization of nano bamboo charcoal drug delivery system for Eucommia ulmoides extract and its anticancer effectin vitro. Pharmacog Mag 2017, 13(51), 498-503.

Nano bamboo charcoal is being widely used as sustained release carrier for chemicals for its high specific surface area, sound biocompatibility, and nontoxicity; however, there have been no reports on nano bamboo charcoal as sustained release carrier for traditional Chinese medicine (TCM). Objectives was to study the effect of nano bamboo charcoal in absorbing and sustained releasing Eucommia ulmoides extract (EUE) and to verify the in vitro anticancer effect of the sustained release liquid, so as to provide a theoretical basis for the development and utilization of nano bamboo charcoal as TCM sustained-release preparation. The adsorption capacity for the nano bamboo charcoal on EUE was measured by Langmuir model, and the release experiment was carried out under intestinal fluid condition. Characteristic changes for the nano bamboo charcoal nano-drug delivery system with and without adsorption of E. ulmoides were evaluated by scanning electron microscopy, Fourier transform infrared spectroscopy, thermogravimetric analysis, and specific surface area. In addition, the anticancer effect from this novel bamboo charcoal E. ulmoides delivery system was evaluated against a human colon cancer cell line (HCT116). It was found that nano bamboo charcoal exhibits - 129 - good adsorption capacity (up to 462.96 mg/g at 37°). The cumulative release rate for EUE from this nano bamboo charcoal delivery system was 70.67%, and specific surface area for the nano bamboo charcoal decreased from 820.32 m²/g to 443.80 m²/g after EUE was loaded. An in vitro anticancer study showed that the inhibition rate for E. ulmoides against HCT116 cancer cells was 23.07%, for this novel bamboo charcoal nano-drug delivery system. This study provides a novel strategy for the delivery of traditional Chinese medicine using bamboo charcoal nano-drug delivery system.

5 illus, 2 tables, 16 ref

019636   Yoo S R;Jeong S J;Lee N R;Shin H K;Seo C S (K-herb Research Center, Korea Institute of Oriental Medicine, Daejeon, Korea) : Quantification analysis and in vitro anti-inflammatory effects of 20-hydroxyecdysone, momordin ic, and oleanolic acid from the fructus of Kochia scoparia. Pharmacog Mag 2017, 13(51), 339-44.

The fructus of Kochia scoparia Schrader (Chenopodiaceae) is a traditional herbal medicine that has been used for treating gonorrhea and dermatitis. We investigated the anti-inflammatory activities of three marker compounds, including 20-hydroxyecdysone, momordin Ic, and oleanolic acid, from the fructus of K. scoparia. The simultaneous analysis of three components was performed using high-performance liquid chromatography and high-performance thin-layer chromatography. We evaluated the anti-inflammatory effects of the nine marker compounds by determining their anti-inflammatory activities in the murine macrophage cell line RAW 264.7. Among three marker compounds, momordin Ic, but not 20-hydroxyecdysone and oleanolic acid, had inhibitory effects on the production of inflammatory cytokines tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6) in LPS-treated RAW264.7 macrophages. The effects of three marker compounds on prostaglandin E₂(PGE₂) were also evaluated. All three compounds significantly reduced PGE₂ production in LPS-treated cells. We suggest that momordin Ic is the most potent phytochemical of the fructus of K. scoparia as an anti-inflammatory agent. HPLC: High-performance liquid chromatography; TNF-α: Tumor necrosis factor alpha; IL-6: Interleukin-6; PGE²: Pro-inflammatory mediator prostaglandin E₂; LPS: Lipopolysaccharide.

7 illus, 26 ref

019635   Yang B;Lee H B;Kim S;Park Y C;Kim K;Kim H (Pharmacology Div, School of Korean Medicine, Pusan National Univ, Gyeongnam, Korea) : Decoction of Dictamnus dasycarpus turcz. root bark ameliorates skin lesions and inhibits inflammatory reactions in mice with contact dermatitis. Pharmacog Mag 2017, 13(51), 483-7.

The root bark of Dictamnus dasycarpus Turcz. (Dictamni Radicis Cortex) has been widely used to treat skin diseases in Korea, and its anti-inflammatory efficacies were recently reported. The paper aims to investigate the inhibitory effects of decoction of Dictamni Radicis Cortex (DDRC) in mice with contact dermatitis (CD). We investigated the effects of DDRC on skin lesion characteristics such as crust, scales, incrustation and petechiae, the erythema and melanin indexes, skin thickness, histopathologic changes, and cytokine production in 1-fluoro-2,4-dinitrofluorobenzene (DNFB)-induced CD mice. Topical application of DDRC ameliorated crust, scales, incrustation, and induced by DNFB. In addition, DDRC lowered the erythema index significantly (P <60> 0.05). DDRC effectively inhibited enlargement of skin thickness (P <60> 0.05). Histopathologic observation showed that DDRC inhibited epidermal hyperplasia, hyperkeratosis, and spongiotic changes. Finally, DDRC decreased production levels of IFN-γ, TNF-α and IL-6 induced by repeated application of DNFB (P <60> 0.05). These data suggest that DDRC can be used in the treatment of inflammatory skin diseases including CD. Moreover, these results are closely related to the decreasing - 128 - production of TNF-α IFN-γ and IL-6 in inflamed tissues.

7 illus, 20 ref

019634   Yan H;Guo C;Shao Y;Ouyang Z (School of Pharmacy, Zhenjiang Univ, Zhenjiang, China) : Rapid detection of volatile oil in Mentha haplocalyx by near-infrared spectroscopy and chemometrics. Pharmacog Mag 2017, 13(51), 439-45.

Near-infrared spectroscopy combined with partial least squares regression (PLSR) and support vector machine (SVM) was applied for the rapid determination of chemical component of volatile oil content in Mentha haplocalyx. The effects of data pre-processing methods on the accuracy of the PLSR calibration models were investigated. The performance of the final model was evaluated according to the correlation coefficient (R) and root mean square error of prediction (RMSEP). For PLSR model, the best preprocessing method combination was first-order derivative, standard normal variate transformation (SNV), and mean centering, which had R_c² of 0.8805, R_p² of 0.8719, RMSEC of 0.091, and RMSEP of 0.097, respectively. The wave number variables linking to volatile oil are from 5500 to 4000 cm^-1 by analyzing the loading weights and variable importance in projection (VIP) scores. For SVM model, six LVs (less than seven LVs in PLSR model) were adopted in model, and the result was better than PLSR model. The R_c² and R_p² were 0.9232 and 0.9202, respectively, with RMSEC and RMSEP of 0.084 and 0.082, respectively, which indicated that the predicted values were accurate and reliable. This work demonstrated that near infrared reflectance spectroscopy with chemometrics could be used to rapidly detect the main content volatile oil in M. haplocalyx.

9 illus, 2 tables, 23 ref

019633   Xu Z;Zhang M;Dou D;Tao X;Kang T (College of Pharmacy, Liaoning University of Traditional Chinese Medicine, No. 77, Shengming One Road, Dalian 116600, P.R. China) : Berberine depresses contraction of smooth muscle via inhibiting myosin light-chain kinase. Pharmacog Mag 2017, 13(51), 454-8.

Berberine is a natural isoquinoline alkaloid possessing various pharmacological effects, particularly apparent in the treatment of diarrhea, but the underlying mechanism remains unclear. Smooth muscle myosin light-chain kinase (MLCK) plays a crucial role in the smooth muscle relaxation-contraction events, and it is well known that berberine can effectively depress the contraction of smooth muscle. Hence, whether berberine could inhibit MLCK and then depress the smooth muscle contractility might be researched. The purpose of this study is to investigate the effects of berberine on MLCK. Based on this, the contractility of gastro-intestine, catalysis activity of MLCK, and molecular docking are going to be evaluated. The experiment of smooth muscle contraction was directly monitored the contractions of the isolated gastrointestine by frequency and amplitude at different concentration of berberine. The effects of berberine on MLCK were measured in the presence of Ca²⁺-calmodulin, using the activities of 20 kDa myosin light chain (MLC₂₀) phosphorylation, and myosin Mg²⁺-ATPase induced by MLCK. The docking study was conducted with expert software in the meantime. The phosphorylation of myosin and the Mg²⁺-ATPase activity is reduced in the presence of berberine. Moreover, berberine could inhibit the contractibility of isolated gastric intestine smooth muscle. Berberine could bind to the ATP binding site of MLCK through hydrophobic effect and hydrogen bonding according to the docking study. The present work gives a deep - 127 - insight into the molecular mechanism for the treatment of diarrhea with berberine, i.e., berberine could suppress the contractility of smooth muscle through binding to MLCK and depressing the catalysis activity of MLCK.

4 illus, 21 ref

019632   Wu A;Ye X;Huang Q;Dai W M;Zhang J M (Neurosurgery Dep, Second Affiliated Hospital of Zhejiang Univ, School of Medicine, Hangzhou 310009, P.R. China) : Anti-epileptic effects of valepotriate isolated from Valeriana jatamansi jones and its possible mechanisms. Pharmacog Mag 2017, 13(51), 512-16.

This work aimed to investigate the anti-epileptic effects of valepotriate isolated from Valeriana jatamansi Jones and studied its possible mechanisms. The anti-epileptic effects of valepotriate were studied using maximal electroshock-induced seizure (MES), pentylenetetrazole (PTZ)-induced epilepsy, and pentobarbital sodium-induced sleeping model in mice. The possible anti-epileptic mechanisms of valepotriate were investigated by analyzing the expressions of GABA_A, GABA_B, glutamic acid decarboxylase (GAD65), Bcl-2, and caspase-3 in the brain using Western blot assay. The results indicated that valepotriate showed significant anti-epileptic activity against MES- and PTZ-induced epilepsy at doses of 5, 10, and 20 mg/kg, and ED₅₀ values for MES- and PTZ-induced epilepsy were 7.84 and 7.19 mg/kg, respectively. Furthermore, valepotriate (10 and 20 mg/kg) can significantly prolong sleeping time and shorten the latency time on the pentobarbital sodium-induced sleeping time test. Furthermore, valepotriate (5, 10, and 20 mg/kg) could significantly up-regulate the expression of GABA_A, GAD65, and Bcl-2 and down-regulate the expression of caspase-3, but had no significant effect on the expression of GABA_B. The results indicated that valepotriate had anti-epileptic activity and the mechanisms might be associated with regulation of GABA and inhibition of neuronal apoptosis.

5 illus, 2 tables, 34 ref

019631   Wang Y;Gong G H;Xu Y N;Yu L J;Wei C X (NO, , No. 22 Holin He Street, Tongliao City, Inner Mongolia, P.R. China) : Sugemule-3 protects against isoprenaline-induced cardiotoxicity in vitro. Pharmacog Mag 2017, 13(51), 517-22.

Sugemule-3 (SD) is a traditional Chinese medicine with protective effect of myocardium. However, the underlying mechanisms of the effect had not been elucidated. In the present study, the serum of SD was prepared. A model of β-adrenergic agonist isoprenaline (ISO)-induced H9c2 cardiomyocytes injury was established in vitro. The changes in cell viability were examined to determine the available concentration of ISO and serum of SD. ELISA, terminal deoxynucleotidyl transferase-mediated dUTP nick end-labeling assay, and flow cytometry were used to detect the effect of serum of SD on oxidative stress and apoptosis. The expression levels of the mitochondria-dependent apoptotic pathway and mitogen-activated protein kinase signalling-related proteins were analyzed. Incubation with different dose of ISO (0.015, 0.01, 0.005, and 0.0025 mol/L) for 24 h caused dose-dependent loss of cell viability and 0.01 mol/L of ISO approximately reduced the cell viability to 50%. Pretreatment with 50 μ mol/L serum of SD effectively decreased the levels of ISO-induced cell toxicity. Serum of SD relived ISO-induced oxidative stress and apoptosis in H9c2 cardiomyocytes. A further mechanism study indicated that serum of SD inhibited the mitochondria-dependent apoptotic pathways and regulated the expression levels of Bcl-2 family. ISO activated ERK and P38, whereas serum of SD inhibited their activation. Serum of SD inhibits the ISO-induced activation of the mitochondria-dependent apoptotic pathway, oxidative stress, and ERK, P38 inactivation. Serum of SD is used for the treatment of ISO-induced cardiomyopathy.

8 illus, 33 ref

019630   Wang S;Bao Y R;Li T J;Yu T;Chang X;Yang G L; Meng X S (School of Pharmacy, Liaoning Univ of Traditional Chinese Medicine, Dalian-116600 China) : Mechanism of fructus aurantii flavonoids promoting gastrointestinal motility: from organic and inorganic endogenous substances combination point of view. Pharmacog Mag 2017, 13(51), 372-7.

Fructus Aurantii (FA) derived from the dried, and unripe fruit of Citrus aurantium L. is one of the commonly used traditional Chinese medicines to treat gastrointestinal motility dysfunction diseases. According to the literature research, FA flavonoids (FAF) are important active ingredients of FA promoting gastrointestinal motility, but the exact material basis and mechanism of action are still not very clear. This experiment was designed to illustrate the - 125 - material basis of FAF promoting gastrointestinal motility and explore the mechanism of action from an organic and inorganic combination point of view. In this experiment, high-performance liquid chromatography (HPLC) method was used to analyze the composition and content of FAF. Based on the prominent prokinetic effect of FAF on mice, the mechanism of action was speculated through a combination of HPLC coupled with quadrupole time-of-flight mass spectrometry (HPLC-QTOF-MS) and inductively coupled plasma mass spectrometry (ICP-MS). With the method of HPLC, ten dominating components of FAF including neoeriocitrin, narirutin, rhoifolin, naringin, hesperidin, neohesperidin, neoponcirin, naringenin, hesperetin, and nobiletin accounting for more than 86% of FAF were identified. Combined HPLC-QTOF-MS with ICP-MS, the endogenous substances with difference in the blood of mice were analyzed, in which 4-dimethylallyltryptophan, corticosterone, phytosphingosine, sphinganine, LysoPC (20:4(5Z, 8Z, 11Z, 14Z)), LysoPC(18:2 (9Z, 12Z)), and Ca²⁺, Mg²⁺, Zn²⁺ metal ions had significant changes, involving tryptophan metabolism, corticosterone metabolism, sphingolipid metabolism, and other pathways. The results preliminarily elaborated the mechanism of FAF promoting gastrointestinal motility from an organic and inorganic point of view, which provide valuable information for researching and developing new multi-component Chinese medicine curing gastrointestinal underpower associated diseases.

5 illus, 1 table, 38 ref

019629   Veda Priya G;Mallikarjuna Rao T;Ganga Rao B (AU College of Pharmaceutical Science, Andhra Univ, Visakhapatnam-530 003, Email: gummadi.veda88@gmail.com) : Oxidative stress inhibitory aptitude of Saponaria officinalis and Zanthophyllum aramatum. Int J Sci Nat 2017, 8(1), 75-80.

The study was aimed to evaluate the antioxidant activity two traditional medicinal plants, Saponaria officinalis and Zanthophyllum aramatum. The root part of plants was used for preparation of extracts using maceration process. The extracts of plants were studied for free radical scavenging activity on 2, 2-diphenyl-1-picrylhydrazyl (DPPH), hydroxyl and superoxide free radicals and antioxidant capacity was studied using ferric thiocyanate (FTC) method. The selected plants' extracts showed the concentration dependent percentage inhibition on tested free radicals. The extracts showed the good scavenging activity on DPPH free radical and less on superoxide free radical. The ethyl acetate extract of Z. aramatum showed best activity and is comparable with standard drug ascorbic acid. The extracts showed the more activity at 400μg/100μL. The results of the FTC method also showed that the selected plants extracts have antioxidant capacity. The extracts of selected plants showed the lower absorbance compared to the control. The ethyl acetate extract of Z. aramatum reduced the amounts of peroxides from the linolenic acid oxidation with the percentage of 51.07 on 7th day of FTC method. The chloroform extract of Z. aramatum showed less free radical scavenging activity and less peroxide inhibition in FTC method. Finally, among two plants Z. aramatum have the more antioxidant capacity.

5 illus, 2 tables, 23 ref

019628   Tung N H;Uto T;Hai N T;Li G;Shoyama Y (Pharmacognosy Dep, Faculty of Pharmaceutical Sciences, Nagasaki International Univ, Sasebo, Nagasaki 859-3298, Japan) : Quassinoids from the root of Eurycoma longifolia and their antiprolifertive activity on human cancer cell lines. Pharmacog Mag 2017, 13(51), 459-62.

The roots of Eurycoma longifolia Jack have traditionally been used as an aphrodisiac tonic besides the other remedies for boils, fever, bleeding gums, and wound ulcer. Recently, the antiproliferative activity of E. longifolia has been reported and remained attractive to natural chemists. The objective of this study was to study on antiproliferative compounds from the root of E. longifolia. Column chromatography was used to separate individual compounds, - 124 - spectroscopic data including nuclear magnetic resonances and mass spectrometry were analyzed to determine the chemical structure of the isolates and for biological testing, antiproliferative activity of compounds was tested on seven human cancer cell lines (KATO III, HCT-15, Colo205, HepG2, PC-3, Jurkat, HL-60) by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide method. Nine quassinoids including a new C₁₉longilactone-type quassinoid glycoside were characterized from the roots of the title plant. Among them, the major quassinoid eurycomanone exhibited selectively potential antiproliferative activities on the leukemia cell lines (HL-60 and Jurkat) and had very low toxic effects on normal skin fibroblast cell line (NB1RGB). The current study reveals one new quassinoid glycoside and the potential active component (eurycomanone) from E. longifolia for the leukemia treatment.

3 illus, 2 tables, 17 ref

019627   Tomar V;Tonpay S D;Alok S (NO, , Pharmacology IPS Dep, Gwalior, Madhya Pradesh, Email: vivek.tmr81@gmail.com ) : Effect of ethanolic extract of leaves of Passiflora insarnata Linn. in streptozotocin-induced diabetes in rats. Int J pharm Sci Res 2016, 7(10), 4246-52.

The worldwide prevalence of diabetes mellitus (DM) has risen dramatically over the past two decades; based on current trends, more than 360 million individuals will be having diabetes by year 2030. The present study was designed to investigate the hypoglycemic of effect of ethanolic extract of leaves of Passiflora insarnata linn. in streptozotocin-induced diabetes in rat. The pharmacological investigation suggested that the ethanolic extract of the leaves was beneficial in controlling the blood glucose levels, improves the lipid metabolism and prevents diabetic complications from lipid peroxidation in experimental diabetic rats. From this study, it can be concluded that the ethanolic extract of the plant exhibited protective and ameliorative effects against streptozotocin induced pancreatic cytotoxicity and severe hyperglycaemia by enhancing the peripheral utilization of glucose, correcting the impaired liver glycolysis and limiting gluconeogenic formation and also repairing and rejuvenating the residual beta cell population. These effects may be due to the presence of phenolic compounds, flavonoids, and other phytochemical constituents, which could act synergistically or independently in modulating the activities of glycolytic and gluconeogenic enzymes.

16 ref

019626   Timalsina A;Ahmed M G;Acharya A (Pharmaceutics Dep, Sri Adichunchanagiri College of Pharmacy, B.G. Nagara, Email: mohammedgulzar1@gmail.com) : Formulation and comparative evaluation of olmesartan medoxomil tablets by solid dispersion and complexation techniques. J pharma Sci Tech 2016, 5(2), 87-91.

Olmesartan Medoxomil (OLM) is a selective AT1 subtype angiotensin-II receptor antagonist that is approved for the treatment of hypertension. It is having low aqueous solubility, so the present attempt is made to enhance the solubility of OLM by solid dispersion and complexation methods further - 123 - formulating them into tablets by direct compression method. Solid dispersion and inclusion complex were prepared following solventevaporation method using poloxamer 188 and β-cyclodextrin as a carrier.The prepared formulations were characterized for compatibility, drug content, saturation solubility and, dissolution studies. FT-IR study revealed no interaction between drug and excipients. Among all methods, solid dispersion (SD3) containing drug: poloxamer188 in the ratio of 1:3 showed rapid and higher drug release (85.36% within 45 min).The tabletsprepared using SD3 solid dispersion and C3 inclusion complex were evaluated for both precompression and postcompression parameters. All the data obtained from the precompression and postcompression parameters fulfill the official requirements of tablets. The % drug release from the F1 batch tablet is higher (84.28%) than the F2 batch tablets (77.78%) within 45 minutes.Stability studies of F1 batch tablets showed no significant change in formulation during study period. Thus, it can be concluded that the formulation was stable.

5 illus, 9 tables, 15 ref

019625   Thulluru A;Srikanth G;Firoz S;Chowdary V C E; Aruna K;Geetha K (Pharmaceutics Dep, Sree Vidyanikethan College of Pharmacy, Tirupati-517 102, Email: ashokthulluru@gmail.com) : Formulation and in vitro evaluation of frovatriptan succinate oral disintegrating tablets by direct compression technique. J pharma Sci Tech 2017, 6(2), 82-7.

The aim of present study was to formulate Frovatriptan Succinate (FS) as Orally disintegrating tablets (ODT) using various concentrations of super disintegrents like, Sodium Starch Glycolate (SSG), croscarmellose sodium (CCS), crospovidone (CPV) by direct compression. To enhance its bioavailability and to fasten its onset of action in comparison to its conventional tablets. Standard calibration curve of FS was obtained in pH 6.8 phosphate buffer by spetrophotometric method, drug-excipient compatibility studies were carried by isothermal stress studies and confirmed by FT-IR studies. All the Formulations were evaluated for pre-compression, post-compression studies. Accelerated stability studies up to 6 months were conducted for the optimized formulation (F9). The drug-excipient compatibility studies reveals that all the excipients used are compatible with FS. Pre & post compression parameters were within the acceptable limits for all formulations. An in vitro dissolution kinetic study indicates the release rate of FS from ODT increases as the concentration of super disintegrents increases. Among all super disintegrents formulations with CPV are having faster release profiles and the order of super disintegrants to enhance dissolution rate in the formulations of FS ODT is CPV <62> CCS <62> SSG. Formulation F9 (8% w/w CPV) released 100% of drug with in 6 min was considered as the optimal ODT among all the nine formulations tested in this study. Optimized formulation (F9) passed the test for stability in its in final pack. Hence, an effective FS ODT dosage form for treating acute migraine attack was formulated by direct compression technique.

5 illus, 5 tables, 18 ref

019624   Tensingh Baliah N;Jeeva P (Botany Post Graduate Dep, Ayya Nadar Janaki Ammal College, Sivakasi, Tamilnadu, Email: tens007@rediffmail.com) : Isolation, identification and characterization of phosphate solubilizing bacteria isolated from economically important tree species. Int J Sci Nat 2016, 7(4), 870-6.

The present investigation is aimed at to isolation, identification and characterization of phosphate solubilizing bacteria from the economically important tree species such as lemon, jackfruit and mango. The population level of PSB was higher in the rhizosphere soils collected from lemon followed by jack fruit. Two isolates from each tree species, totally 6 PSB - 122 - strains were isolated and used for further studies. The isolated strains such as JP1, JP2, LP1, MP1 and MP2 were identified as Bacillus megaterium and remain LP2 as Pseudomonas putida. The strains were characterized under in vitro by measuring the P solubilization zone in solid medium, determining pH change of the medium and estimating the phosphatase activity, organic acids production and available phosphorus. Among six strains, MP1 was found to be superior in forming halo zone formation in the solid medium followed by LP1; the maximum pH reduction noticed in MP1 followed by MP2; JP1 and JP2 good in organic acid production and JP1 able to produce more phosphatase followed by JP2. The isolated PSB strains were differed with respect to utilization of various carbon, nitrogen, aminoacid and vitamin sources.

7 tables, 41 ref

019623   Sudhakar C K;Jain S;Charyulu R N (Pharmacy Dep, Lovely professional Univ, Jalandhar, Punjab, Email: ckbhaipharma@gmail.com) : Comparison study of liposomes, transfersomes and ethosomes bearing lamivudine. Int J pharm Sci Res 2016, 7(10), 4214-21.

The aim of this study was to compare the skin permeation of liposomes, transfersomes and ethosomes of lamivudine under non-occlusive conditions. The liposome and transfersomes prepared by thin film hydration method and ethosomes were prepared by slight modification on hot method. The Liposomal formulation (LP1) ethosomal formulation (ET2) and transfersomal (TF2) formulation showed highest entrapment 49.76 ± 2.1%, 81.97 ± 1.5% and 83.81 ± 1.4%, optimal nanometric size range 515 ± 4.6 nm, 374 ± 8.9nm and 315 ± 8.5nm and smallest polydispersity index0.529±0.019,0.432± 0.011 and 0.422± 0.009 respectively. The results of skin fluorescence experiments showed that penetration depth and fluorescence intensity of calcein from ethosomes and transfersomes was much greater than that from liposomes. Stability studies indicated that there was no significant physical change in vesicular formulation for 45 days at different temperatures. The in vitro result indicates that liposome retrain on the surface of skin due to poor permeation power, transfersomes improve penetrates of lamivudine and made drug easiest to accumulate in the skin. Ethosomes enhances permeation the drug to the deeper layer of skin and enter into systemic circulation rather than skin deposition. Transferosomes and ethosomes are able to cross the stratumcorneum and permeate drug to deeper tissue compare to liposomes.

28 ref

019622   Srivastava S;Choudhary G P (Pharmacognosy Dep, School of Pharmacy, DAVV, Indore, Madhya Pradesh, Email: sweta.koka@gmail.com) : Anti-tussive activity of ethyl acetate and - 121 - methanol extracts of Adhatoda vasica Nees. Int J pharm Sci Res 2016, 7(10), 4180-3.

The present study was carried out to evaluate anti-tussive activity of ethyl acetate and methanolic extract of leaves of Adhatoda vasica Nees. As cough is a natural reflex expulsive defense mechanism of the body, it is the most common symptom of respiratory disease. Ammonium hydroxide and Sulphur dioxide induced cough models in mice were used for evaluation of antitussive activity of ethyl acetate and methanolic extracts of leaves Adhatoda vasica. The ethyl acetate and methanolic extract of leaves Adhatoda vasica was orally administered at the dose levels of 500 mg/kg b.w. showed maximum inhibition of cough by 82% and 81% respectively. The standard anti-tussive drug Codiene phosphate (10mg/kg b.w.) showed maximum inhibition of cough by 84%. It was found that both extracts of Adhatoda vasica showed anti-tussive activity and obtained percentage inhibition of cough reflex is approximately comparable as standard drug.

11 ref

019621   Sondes Sahli;Jaballah A;Khlifi L;Henda Chahed;Ferchichi S;Miled A (NO, Biochemistry Lab CHU Farhat HACHED, Street Doctor Moreau, 4000 Sousse, Tunisia, Email: sahlisondes@yahoo.fr ) : Study of the involvement of adiponectin and homa-ir in tunisian subjects with metabolic syndrome. Int J pharm Sci Res 2016, 7(10), 4022-7.

Metabolic syndrome (MS) is a multi-factorial disorder with insulin resistance as a major characteristic. Adiponectin, an adipocyte derived cytokine, can regulate glucose levels and lipid homeostasis by its insulin sensitizer properties. Low circulating levels of serum adiponectin has been reported as a risk factor for the development of MS. The aim of this case control study was to investigate the association of serum adiponectin concentration, insulin resistance and various risk factors with MS among Tunisian participants. We designed a case-control study involving 100 patients with MS (84 females and 16 males, mean age 54±11 years) and 100 healthy controls (60 females and 40 males, mean age 51±10 years). Serum total cholesterol and triglyceride were determined by enzymatic methods. Insulin resistance was calculated using the homeostasis model assessment (HOMA-IR) = fasting insulin (uU/ml) x fasting plasma glucose (mmol/l)/22.5 and serum adiponectin levels were measured by enzyme-linked immunosorbent assay. Interestingly, 72% of the subjects with MS had high blood pressure. Compared with controls, patients had significantly higher levels of triglycerides (1.64±0.88 mmol /l; 1.07±0.43 mmol/l; p=0.03) and lower levels of high-density lipoprotein cholesterol (1.26±0.41 mmol/l; 1.58±0.30 mmol/l; p=0.04). In addition, there was a significant difference in serum adiponectin levels between the subjects with MS and controls (13.96±5.23 μg/ml; 22.24±9.07 μg/ml; p=0.006) and the mean levels of HOMA-IR were 5.23±3.52 and 1.83±0.93 for patients and controls, respectively. In conclusion, hypoadiponectinemia and insulin resistance represent risk factors for MS development.

40 ref

019620   Sirohi U;Mukesh Kumar;Chauhan P;Singh M K; Navneet Kumar;Prakash S;Chand P;Naresh R K;Sharma V R;Chaudhary V (Horticulture Dep, S.V.P.U.A.T., Meerut-250 110, Email: k.mukesh123@yahoo.com) : Genetic diversity in single and double type of tuberose (Polianthes tuberosa L.) germplasm using randomly amplified polymorphic DNA (RAPD) markers. Int J agric statist Sci 2017, 13(2), 519-26.

Genetic - 120 - variation among 21 tuberose genotypes were evaluated using seven randomly amplified polymorphic DNA markers. The results revealed that the RAPD markers produced much better reproducible bands and were more efficient in grouping germplasm. Polymorphic information content varied from 0.37-0.98 with an average value of 0.813, resolving power vary from 0.28 to 5.61 with an average 2.67, while the marker Index varied from 0.74 to 5.98 with an average value of 2.70, respectively. The number of RAPD fragments generated per primer set ranged from 1 to 7 with an average 3.57 bands per primer and fragment sizes varying from 180-1400 bp. A total of 19 polymorphic bands generated 100% polymorphism. All germplasms were clearly differentiated by their RAPD fingerprints. The Jaccard similarity indices (J) based on RAPD profiles were subjected to UPGMA cluster analysis. The dendogram generated by RAPD markers revealed four major groups and noted considerable amount of genetic variation among the genotypes. Genotypes namely Mexican White Double and Swarna Rekha cultivar were found to be more diverse in molecular analysis.

3 illus, 3 tables, 34 ref

019619   Shrirao A V;Bhilegaonkar S (Pharmacology Dep, Shobhaben Pratapbhai Patel School of Pharmacy and Technology Managemen, Mumbai-400 056, Email: shilpabhilegaonkar@gmail.com) : Solubility enhancement and development of dispersible tablet of candesartan clexitil. Int J pharm Sci Res 2016, 7(10), 4164-9.

Candesartan Cilexitil is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. Candesartan cilexitil is a BCS class II drug having low solubility and high permeability. Candesartan Cilexitil is a prodrug which is rapidly converted to the active drug, Candesartan, by ester hydrolysis during absorption from the gastrointestinal tract. The bioavailability of Candesartan Cilexitil is approximately 15% after an oral administration. To increase bioavailability of such drug, solubility and dissolution are important parameters. To increase solubility of candesartan cilexitil, spray drying technique was incorporated with use of Fluidised Bed Processor. Also dissolution rate was improved with the use of appropriate superdisintegrants. Superdisintegrants used are Croscarmellose sodium, Crospovidone and Sodium starch glycolate. Dissolution rate of Candesartan Cilexitil from prepared dispersible tablet was compared with marketed formulation. Results have shown that solubility of Candesartan Cilexitil has been increased and dissolution rate was improved significantly. The transformation of Candesartan Cilexitil from crystalline to amorphous state by spray drying and the use of superdisintegrants are considered among the factors which contributed in improvement of Candesartan Cilexitil dissolution.

15 ref

019618   Shrirao A V;Bhilegaonkar S (Pharmacology Dep, Shobhaben Pratapbhai Patel School of Pharmacy and Technology Managemen, Mumbai, Maharashtra-400 056, Email: shilpabhilegaonkar@gmail.com) : Solubility enhancement and development of dispersible tablet of candesartan cilexitil. Int J pharm Sci Res 2016, 7(10), .

Candesartan Cilexitil is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. Candesartan cilexitil is a BCS class II drug having low solubility and high permeability. Candesartan Cilexitil is a prodrug which is rapidly converted to the active drug, Candesartan, by ester hydrolysis during absorption from the gastrointestinal tract. The bioavailability of Candesartan Cilexitil is approximately 15% after an oral administration. To increase bioavailability of such drug, solubility and dissolution are important parameters. To increase solubility of candesartan cilexitil, spray drying technique was incorporated with use of Fluidised Bed Processor. Also dissolution rate was improved with the use of appropriate superdisintegrants. Superdisintegrants used are Croscarmellose sodium, Crospovidone and Sodium starch glycolate. Dissolution rate of Candesartan Cilexitil from prepared dispersible tablet was compared with marketed formulation. Results have shown that solubility of Candesartan Cilexitil has been increased and dissolution rate was improved significantly. The transformation of Candesartan Cilexitil from crystalline to amorphous state by spray drying and the use of superdisintegrants are considered among the factors which contributed in improvement of Candesartan Cilexitil dissolution.

15 ref