Fast dissolving tablets of diclofenac sodium were prepared using direct compression after incorporating superdisintegrants such as cross linked carboxymethylcellulose, sodium starch glycolate and cross linked povidone in different concentrations. All the formulations were evaluated for the influence of disintegrants and their concentrations on the characteristics of fast dissolving tablet mainly in terms of disintegration time and dissolution rate. Tablets containing cross-linked carboxymethylcellulose showed better disintegrating character along with rapid release (90% drug release in 10 min.). No appreciable difference was found between the formulations containing other two superdisintegrants. The concentration of the superdisintegrants had also an effect on disintegration time and in vitro dissolution. There seems to be a trend towards use of higher level of disintegrants producing rapid disintegration and faster dissolution. The resulting tablets were also evaluated for its hardness and friability and were found to be independent of disintegrant concentration.

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Naphtho[2,1-b]furyl-2-carboxyhydrazide 1 has been condensed with various substituted acetophenones to obtain corresponding carboxy hydrazones 2, which on treatment with Vilsmeier-Haack reagent resulted in the formation of 2-[3-phenyl-4-formyl -1-carbonyl]naphtho[2,1-blfuran pyrazole derivatives 3a-f. The compound 1 has been converted into N-aroyl-N'-(naphtho[2,1-b]furan- 2-carbonyl)hydrazine 4a-c, which on cyclization with phosphorous oxychloride produced 2-[5- aroyl-1,3,4-oxadiazol-2-yl]naphtho[2,1-b]furans 5a-c. The compound 6 has been synthesized by the condensation of 1 with ethyl acetoacetate. Various naphtho[2,1-b]furan-2-[N'-(substituted benzopyran-2'-one-3'-carbonyl)]hydrazides 8a-d, have been prepared from compound 1 via compound 7.The compounds 8a-d have also been synthesized by direct condensation of 1 with 6- substituted coumarins. All newly synthesized compounds have been characterized by elemental analysis and spectral data and screened for antimicrobial, anthelmintic, antiinflammatory, analgesic and diuretic activities.

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Polymeric ophthalmic inserts containing indomethacin were formulated with combinations of two different types of polyvinyl alcohol (high-1,25,000 and low-14,000 molecular weights) and physically reinforced by heating (80o and 100o for 24 and 48 h) and freeze-thawing (3 and 6 cycles). In vitro drug release and permeation kinetics across goat cornea was studied in a continuous flowthrough apparatus and a modified Keshary-Chien cell, respectively, and compared with the nonreinforced inserts. The rate of indomethacin release was inversely proportional to low molecular weight polyvinyl alcohol content. The duration of heating had more effect on drug release than the temperature and freeze thawing was more successful in retarding the drug release. The permeation of indomethacin correlated well with the in vitro release.

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Two spectrophotometric methods in visible region have been developed for estimation of ambroxol hydrochloride in bulk drug and in tablets. In method A1 the -NH2 group of ambroxol reacts with sodium nitrite and forms a diazo compound which couples with N- (1-naphthy1)- ethylene diamine dihydrochloride to form a pinkish red chromogen which exhibits maximum absorption at 500 nm against a reagent blank. Method B is based on the reduction of ferric ions in its salt to ferrous ions by the drug, producing a yellowish orange chromogen with absorption maximum at 400 nm against the reagent blank. Beer's law was obeyed in the range of 10 to 50 μg/ml for method A and 40 to 240 μg/ml for method B. The results of analysis have been validated statistically and by recovery studies. The recovery ranged between 100.6 and 100.3% for method A and between 99.6 and 100.2% for method B. This paper describes new, simple and sensitive colourimetric methods for the estimation of ambroxol hydrochloride in bulk drug and pharmaceutical dosage forms.

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Two simple, accurate and precise methods for simultaneous estimation of losartan potassium and hydrochlorothiazide in combined dosage form have been described. First method employs formation and solving of simultaneous equations using 206.6 nm and 270.6 nm as two analytical wavelengths. Second method is dual wavelength method, which uses the difference of absorbance values at 206.6 and 261.4 nm for the estimation of losartan and absorbance values at 270.6 nm for the estimation of hydrochlorothiazide. Both the methods allow the simultaneous determination of losartan and hydrochlorothiazide in the concentration ranges employed for this purpose with the standard deviation of <1.0% in the assay of tablets.

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Two simple, accurate, rapid and sensitive methods have been developed for the estimation of ethamsylate in pharmaceutical dosage forms. Method A is based on the reduction of Folin- Ciocalteau phenol reagent by ethamsylate in presence of 20% sodium carbonate solution giving blue chromogen, which shows maximum absorption at 740 nm while method B is based on the reduction of ferric ions (ferric nitrate) to ferrous ions by ethamsylate which then reacts with 1,10-phenanthroline to produce reddish coloured complex showing maximum absorption at 435 nm against reagent blank. In both the methods Beer's law was obeyed in the concentration range of 5-25 μg/ml.

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A simple spectrophotometric method has been developed for the estimation of nabumetone in pure and pharmaceutical dosage forms. In this method, the drug is made to react with ferric chlorideand 1,10-phenanthroline when a red complex is formed. The chromogen can be estimated at 517 nm against a reagent blank. The method obeys Beer's law in the concentration range of 1-5μg/ml of the drug.

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The synthesis of some new potentially bioactive 4-thiazolidinone has been undertaken. The required 2-(substituted benzalhydrazinocarbonyl)-3,5-dichloro-benzo(b)thiophene(2) was prepared by reaction of 2-hydrazinocarbonyl-3,5-dichloro benzo(b)thiophene(1) with different aryl aldehyde. The compounds (2) on cyclocondensation with thioglycolic acid under micro wave irradiation as well as In a conventional way yielded the corresponding 4-thiazolidinones (3). The structures of synthesized compounds were deduced on the basis of their elemental analyses and spectral analyses (IR and 1H NLIR). The synthesized compounds were evaluated for their antimicrobial activity.

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Two methods, one titrimetic and the other spectrophotometric, for the determination of prcpranolol hydrochloride in bulk drug and in its tablets have been described. Both methods are indirect and involve the determination of the chloride content of the hydrochloride of the drug. In titrimetry, the sample solution is treated with a known excess of silver nitrate and after the precipitations is complete, unreacted silver nitrate is back titrated with thiocyanate using iron (Ill) as indicator. Spectrophotometry makes use of the reaction between chloride and mercury (II) thiocyanate in which thiocyanate ions will be displaced and complexed with iron (Ill) for subsequent rneasurement at 460 nm. Titrimetry is applicable for 1-9 mg of drug whereas spectrophotometry is applicable in the concentration range of 10-50 μg/ml.The detection limit, the quantification limit, molar absorptivity and Sandell sensitivity values of the spectrophotometric method have been reported. These methods were successfully applied to the determination of propranolol in tablets with the percentage recovery of 97.9-100.9 % (titrimetry) and 99.1-102.5 % (spectrophotometry).

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Substituted sulphonanilides of diphenyl ether, benzyl phenyl ether and diphenylamine were synthesized which were structurally related to antiinflammatory drug nimesulide. Synthesized compounds displayed antiinflammatory activity comparable with that of nimesulide. From the result it can be concluded that the replacement of methane sulphonanilide group with other sulphonanilide and replacement of ether oxygen with -OCH2-,-NH- decreases activity.

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In the present study five copolymeric blends of polycaprolactone-polyethylene glycol were prepared by ring opening polymerization technique. These were characterized by IR and NMR studies and by determination of critical micelle concentration. The copolymeric blends were optimized from the entrapment capacity, release rate and stability studies of the nimesulide loadedmicelles prepared using such copolymers. These micellar preparations had shown better stability at refrigerated temperature. The formulation prepared by dialysis method using copolymer, having molar ratio of ε-caprolactone to methoxypolyethylene glycol fifty-to-one, was used for further studies in rats. Mean residence time and bio-distribution studies showed that the micelles have higher circulation time in blood and lesser distribution in other tissues as compared to plain drug solution.

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The present study was aimed at formulation, performance evaluation and stability studies of new vesicular drug carriers system called protransfersomes bearing norgestrel. Protranfersomes of norgestrel were prepared and extensively characterized for drug loading, vesicular shape, vesicular size and size distribution, entrapment efficiency, degree of deformability, transit time, rate of hydration, drug diffusion across rat skin and stability study at 4o and at room temperature. The effects of various parameters such as type of alcohol, type of surfactant and amount of drug of formulation on transdermal permeability profile were assessed. In vitro flux, permeability coefficient and release rate pattern of norgestrel was calculated for transdermal delivery of norgestrel. In the release rate study, no lag phase could be detected and the release of norgestrel from proposed formulation through rat skin was found to be constant but slow (sustained release). Entrapment efficiency was found to be nearly 95% and it depends on the type of surfactant and concentration of surfactant. After one month storage of formulation in liquid crystalline nature, drug content and other characteristic parameters were not changed. Proposed system also cornpared for in vitro performance with well-known vesicular system proliposomes, and shows better skin permeation. Results indicate that the protransfersomal formulation for transdermal drug delivery of norgestrel provides effective contraception, better stability, higher entrapment efficiency, ability as a self penetration enhancer, easy to scale up and better for transdermal delivery as compared to proliposomes.

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Camptothecines have a broad spectrum of antitumor activity both in vitro and in vivo and various clinical properties. Nothapodytes foetida has much higher contents of camptothecine (0.3% dry weight) and its analogs than all other botanical sources of camptothecines. This article indicates the need of systematic studies on cell cultures of Nothapodytes foetida to enhance the production of camptothecine and its analogs by employing various strategies.

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Periodontal diseases are conditions that affect the supporting structures of the teeth. Advances in understanding the etiology and pathogenesis of periodontitis have led to the development of a number of targeted systems for administration of drug into the periodontal pocket. This article reviews the various types of targeted delivery devices (both degradable and non-degradable), which deliver the therapeutic agents directly to the periodontal pocket. Improvement in clinicaland microbiological parameters and reduction in dose have been reported with these systems.

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The present study was aimed at development and characterization of engineered commensal bacteria for site-specific targeting of enzymes. Separation of plasmid (pJR2 and GB4) and transformation in Lactobacillus acidophilus was carried out using a reported method. Azo polymers were synthesized using water-soluble and water- insoluble monomers belonging to acrylate series. The synthesized polymers were characterized for physical appearance, solubility and film forming properties. Effect of microbial flora of colon on polymers was seen by incubating the glass cover slips coated with azo polymers in sterilized nutrient broth containing freshly voided human fecal culture suspension. Colon-specific drug delivery system was developed by mixing the bacterial pellet with skimmed milk and then coating these granules with azo- and pH-sensitive polymer. Lowering of galactose concentration and a-oxoglutaric acid concentration were monitored to in vitro characterize E. coli (56) and E. coli(797), respectively. In vivo screening of developed oral, colon-specific formulation, azo polymer coated granules of engineered E. coli(56) producing galactokinase (GK) and engineered E. coli(797) producing glutamate dehydrogenase (GDH) was performed on rabbits. D-galactose, which is the substrate for enzyme galactokinase and ammonium chloride, was administered intraperitoneally to all rabbits. The lowering of blood galactoselevel and urea level was observed with respect to variable time interval.

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The present study is designed to investigate the effect of BN50739, a platelet activating factor receptor antagonist, on ischaemia-reperfusion induced myocardial injury in rats. In the anaesthetized rat, the heart was subjected to ischaemia by left coronary artery ligation for 45 min followed by reperfusion for 90 min. Infarct size, electrocardiography parameters and serum creatine phosphokinase concentration were estimated to determine the extent of ischaemia-reperfusion induced injury. Serum malondialdehyde concentration was estimated to assess the extent of lipid peroxidation. BN 50739 (5 mg/kg, i.v.) administered after 45 min of ischaemia markedly reduced the infarct size, prevented the loss of R wave, attenuated ST elevation, reduced serum creatine phospho kinase and malondialdehyde concentration. The cardioprotective effect of BN50739 may be due to inhibition of platelet activating factor-induced activation of neutrophils and consequent lipid peroxidation.

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Achyranthes bidentata Blume belonging to the family Amaranthaceae was investigated for antibacterial activity against Bacillus subtilis (NCM-2439), Staphylococcus aureus (NCIM-2492), Pseudomonas aeruginosa (NClM-2053) and Escherichia coli (NCIM-2068) organisms, using agar diffusion method. The petroleum ether, chloroform, methanol and aqueous extracts showed significant antibacterial activity. Our findings offer experimental support to the therapeutic claimson this herb as useful against bacterial infections.

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Having considered the lipophilicity of norgestrel (log p = 3.31) an important contributor to its action mechanism, interaction of the drug with total lipids of blood have been investigated using phospholipid binding, fatty acid composition and peroxidation phenomena as the parameters under investigation. The objective was to derive an insight into the pharmacodynamic behavior of the drug. Significant loss of phospholipid along with changes in fatty acid composition was observed after incubation of whole blood with norgestrel (60 ng/ml, contraceptive concentration in blood). This may be ascribed to binding affinity of norgestrel with lipid constituents in blood. Lipid binding affinity of the drug may have a role in the mediation of its therapeutic effect. Lipid peroxidation induction potential of norgestrel has been quantitatively measured in the context of its toxicity. The results reveal that norgestrel caused significant extent of lipid peroxidation. Ascorbic acid, an antioxidant, could significantly reduce norgestrel-induced lipid peroxidation.

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Microspheres of eudragit L100 and S 100 containing insulin, protease inhibitor and bile salts were prepared by solvent diffusion technique. The chemical interaction between the drug, polymers and adjuvants was evaluated by FTlR and found that there was no interaction between them. In vitro release studies were carried out using metabolic shaker. The microspheres showed delayed release. Based on the in vitro release profile, ideal batches of rnicrospheres (prepared with Eudragit L100 alone and S100 alone as carriers and 1% aprotinin and 1% sodium glycocholate) were selected and used for in vivo evaluation of hypoglycemic effect. The in vivo hypoglycemic effect was determined in rats by measuring the blood glucose level using a glucometer. In the in vivo evaluation, insulin microspheres prepared with Eudragit L-100,1% aprotinin and 1% sodium glycocholate showed prolonged hypoglycemic effect for 3 h when compared with intravenous injection of bovine insulin.

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Ibuprofen dispersible tablets using Plantago ovata mucilage powder, Ocimum basilicum mucilage powder, Plantago ovata husk powder and Ocimum basilicum seed powder as disintegrants were prepared and disintegrating property was studied. The swelling index of the above disintegrants was studied. Disintegrating property of the above disintegrants were evaluated by comparing with the formulations of starch powder as standard disintegrant. The study revealed that Plantago ovata seed powder and mucilage powder were effective in low concentrations (5%) as disintegrants compared to others. The study further revealed a poor relation between the swelling Index and disintegrating efficiency.

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The ethanolic extract of the pseudobulbs of Desmotrichum fimbriatum Blume yielded four new hydrocarbons along with stearic acid. The structures of the phytoconstituents have been established as 18-cyclohexyl-n-octadecane, 24-cyclohexyl-n-tetracosane,n -heneicosayl-1-propionate, and 23-cyclohexyl n-tricosanyl-1-propionate.

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The effect of ethyl acetate extract of Sarcostemma brevistigma was investigated in rat to evaluate the antiinflammatory activity. Carrageenin-induced rat paw edema model and cotton pellet granuloma methods were employed to test antiinflammatory activity. The ethyl acetate extract (650 mg/ kg) produced the inhibition of carrageenin-induced rat paw edema and also found to be effective in cotton pellet granuloma studies. The result indicated that the ethyl acetate extract produced significant (P<0.001) antiinflammatory activity when compared to control

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The successive extracts of Dioscorea bulbifera (bulbils) has been investigated for in vitro antimicrobial activity against Klebsiella pneumoniae, Escherichia coli, Bacillus aureus, Proteus vulgaris, Staphylococcus aureus, Aspergillus niger, Aspergillus flavus, Aspergillus fumigatus and Rhizopus nigricans. The petroleum ether and chloroform extracts showed significant activity against A. fumigatus and R. nigricans. The petroleum ether and distilled water extract showed good activity against K. pneumoniae. The chloroform extract showed feeble activity against S. aureus.

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The focus of the present study is to investigate the immunostimulant effect of Kalayak ghrita, an herbal formulation. The study of this formulation in respect to humoral and cell-mediated immune response showed that oral administration of Kalayak ghrita enhanced the antibody titre as well as foot pad swelling response to the antigenic challenges with sheep red blood cells. The herbal formulation belongs to the Panchgavya class of ayurvedic formulations in which one or more of the five bovine products (milk, ghee, curd, urine and dung) are used along with herbs. The formulation was administered at doses 50,100, 150 and 200 mg/kg/day to healthy rats. Results of the present study suggest a dose-dependent immunostimulant effect of Kalayak ghrita in rats.

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A simple, precise and accurate reverse phase high performance liquid chromatographic method has been developed for the determination of metoprolol tartrate in pharmaceutical formulations. An ODS C18 (25 cm X 4.6 mm) column from Shimadzu in isocratic mode, with mobile phase acetonitrile:methanol:0.5 % glacial acetic acid in triple distilled water: triethylamine (56:18:26:0.1v/v) was used. The flow rate was 1 ml/min and effluent was monitored at 280 nm. Betaxolol hydrochloride was used as the internal standard. The retention times were 4.6 mm and 5.8 mm for metoprolol tartrate and betaxolol hydrochloride respectively. The linearity range was found to be 0.1-40 μg/ml.

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