Simple, rapid and precise reversed-phase HPLC method has been developed for the quantitation of glimepiride in tablet on a Hypersil C-18 (15 cmx3.9 mm) column using a mobile phase consisting acetonitrile:0.05 M monobasic potassium phosphate (pH 6.0) (40:60 v/v) at a flow rate of 1.5 ml/min and detection at 210 nm. The retention time of glimepiride have been found to be 7.8 min and recoveries were between 99-101%. Validation of the proposed method also been done.

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Buccal films of salbutamol sulphate were prepared using three different polymers in various proportions and combinations. The physicochemical parameters like thickness, density, folding endurance, swelling index, mucoadhesive strength based on shear stress and tensile strength, water permeability, drug content and drug release characteristics were evaluated in order to study the effect of polymer and its concentration on the drug release. The properties of the drug free buccal films were compared with the films obtained after drug incorporation in order to study the effect of drug loading on the film characteristics. The thickness and density of all the films produced were in the range of 0.15 to 0.24 mm and 1 .104 to 1.445 g/cm3, respectively. High folding endurance was observed for films containing ethyl cellulose and its combination with hydroxypropylmethyl cellulose. The swelling index was found to be high for formulation F2 containing Eudragit RL100, 6% w/v and 3.2 g of glycerol 40% w/w. The results of the mucoadhesive strength measurement based on shear stress indicated that the buccal films of formulation F4 containing each 3% of hydroxypropylmethyl cellulose and ethyl cellulose exhibited a high value, but the tensile strength measurement studies indicated high mucoadhesive strength for formulation F2, Water permeability was found to be high for formulation F1 containing 6% w/v of Eudragit RL 100 and 2.4 g of glycerol 40% w/w. Drug content uniformity was observed for all films. The drug release studies indicated the first order controlled release kinetics in all cases and the release was extended up to 8 h for formulation F4. It was also observed that the lower the permeability coefficient the greater was the extended release characteristics for the buccal films. Finally it was concluded that the polymers and their combination influenced the film properties as well as release characteristics.

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In this study, the antibacterial activity of leaf of Punica granatum was investigated. Different solvents used were, water, ethanol, methanol, acetone, propanol, 1,4-dioxan, N,N-dimethylformamide (DMF) and benzyl alcohol. The selection of solvents was on the basis of their polarity. The antibacterial activity of six clinical strains (S. paratyphi, S. aureus, S. epidermidis, E. aerogenes P. aeruginosa and B. subtilis) was determined by Growth inhibition using Agar ditch diffusion assay. The aqueous extract was able to inhibit only B. subtilis and S. aureus and was ineffective against all the other four bacterial strains. On the other hand organic solvents proved much better in inhibiting the studied bacterial strains except benzyl alcohol extract which was ineffective against all tested bacterial strains. Among the various solvents, 1,4-dioxan proved to be best while propanol was least effective. Finally, E. aerogenes was found to be most resistant bacteria, while S. aureus, S. epidermidis and B. subtilis were most susceptible.

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A novel stability indicating HPLC has been developed for estimation of amlodipine in tablet formulation. The method was validated using specificity, stability in analytical solution, precision, accuracy and system suitability as parameters. The mobile phase consists of 0.05 M ortho-phosphoric acid buffer, methanol and acetonitrile in the ratio of 50:35:15 and the results show that the method is reproducible and accurate. Degradation of amlodipine was performed in various conditions and the resulting solution was analyzed on HPLC using ODS column (150x4.6mm) with a detection maxima of 361 nm. The method gave a good separation between drug and degradation peaks. Recovery studies gave results between 99.7 to 100.7 % for 5 mg tablets.

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A stability indicating simple, rapid and precise reversed-phase HPLC method has been developed for the quantitation of pioglitazone in tablet on a Hypersil C-8 (250x4.6 mm) column using a mobile phase consisting acetonitrile:0.15% v/v triethylamine (40:60 v/v) adjusted to pH 4.6 with orthophosphoric acid at a flow rate of 1.5 ml/min and detection at 220 nm. The retention time of pioglitazone have been found to be 7.6 min and recoveries were between 99-101%. Validation of the proposed method also been done.

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The influence of three solvents for the polymer (chloroform, dichloromethane and ethyl acetate) employed in the preparation on the drug release from ethyl cellulose microcapsules was studied. Diclofenac sodium was used as core and microcapsules were prepared by an emulsion solvent evaporation method. All the three solvents gave discrete, large sized, free flowing spherical microcapsules. The microcapsules were evaluated for size analysis, drug content, microencapsulation efficiency, wall thickness, drug release characteristics, influence of solvent employed on diclofenac sodium release from microcapsules, surface characteristics. Diclofenac release from the microcapsules was, followed first order kinetics and influenced by the size of the microcapsules and the solvent employed in their preparation. Among the solvents employed chloroform was found to be more suitable for slow release of diclofenac from ethyl cellulose microcapsules.

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Ulcers were induced in thirty six hours fasted Sprague Dawley rats by aspirin or ethanol or pylorus ligation plus aspirin treatment. In each induction procedure there were three groups namely, normal control, positive control and test. In all the three separate experiments the group receiving oral administration of E. alba prior to ulcer induction showed highly significant reduction in the occurrence of gastric ulcers as well as gastric inflammation (after 4 h of treatment) as compared to the control groups. Moreover, the potency of E. albaas an antiulcer agent was comparable to the activity of the proton pump inhibiting drug rabeprazole (positive control). These results emphasize on the need to diversify into alternative therapeutic approaches pertaining to herbal medicine where in a single easily available plant may provide answers to several therapeutic challenges as observed in the anti ulcer activity shown by methanol extract of E. alba.

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Quinine sulphate, an antimalarial agent, is extremely bitter in taste. The present communication deals with development of taste-masked resinates of quinine sulphate using ion exchange resins. The drug resin complexation procedure was optimized with respect to parameters like drug to resin ratio, volume of medium and taste of the complex. The taste-masked complex was then formulated into a prototype suspension base. The suspension was evaluated for various quality control parameters. Taste evaluation of the suspension showed complete masking of the bitterness of the drug. In vitro release studies revealed complete drug elution from the complex after a period of 30 min in pH 1.2 buffer.

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Mucoadhesion is a topic of current interest in the design of drug delivery systems. Mucoadhesive microspheres and microcapsules exhibit a prolonged residence time at the site of application or absorption and facilitate an intimate contact with the underlying absorption surface and thus contribute to improved and/or better therapeutic performance of drugs. In recent years such mucoadhesive microspheres have been developed for oral, buccal, nasal, ocular, rectal and vaginal routes for either systemic or local effects. The principles underlying the development of mucoadhesive microspheres and the research work carried out on these systems are reviewed here.

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The presence of circadian rhythms in human health and illness has been alluded to since the time of Hippocrates. However, it was not until the 1960's that a large variety of physiologic functions and biologic rhythms were described. Biologic variations have now been reported for several physiologic processes and play an important role in the manifestation of many illnesses. The past decade has witnessed rapid advances in the field of chronobiology, which are now being incorporated into clinical medicine, pharmacology and pharmacy practice. A number of chronotherapeutic medications, aiming at synchronizing medications and the intrinsic biorhythms of disease have been developed by novel drug delivery technology. In some cases, conventional medications are being administered according to circadian rhythms. This article focuses on biorhythms and the emerging role of chronotherapeutics in optimizing the treatment of several diseases.

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A simple, fast, precise and accurate liquid chromatographic method was developed for the simultaneous estimation of paracetamol, methocarbamol and diclofenac potassium in tablets. Drugs were chromatographed on a reverse phase Hypersil C18 column using a mobile phase, 25 mM phosphate buffer (pH adjusted to 7.0±0.1) and acetonitrile in the ratio of 65:35 v/v. The flow rate was 1.2 ml/min and the effluent was detected at 225 nm. Chlormezanone was used as an internal standard. The retention time of paracetamol, methocarbamol and diclofenac potassium were 2.74, 3.82 and 6.05 min, respectively. The method was linear (correlation co-efficient was more than 0.999), precise (percentage residual standard deviation for 0.15 for paracetamol, 0.17 for methocarbamol and 0.16 for diclofenac potassium), accurate (overall mean average recovery yields: 99.9% for paracetamol, 100% for methocarbamol and 101% for diclofenac potassium) and selective. Due to its simplicity and accuracy, the method was suitable for routine quality control analysis of these drugs in combined dosage form.

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Cosmeceutical antidandruff hair styling gel formulations containing 0.5 to 1.5% of ketoconazole were developed using Carbopol 940, PEG-400, ethanol and water. All the formulations were characterized for viscosity, rheology, spreadability, pH, texture, drug content and antimicrobial activity against Malassezia furfur. Optimized gel formulation was tested for stability at varying temperature. Formulation containing 1% ketoconazole showed promising performance with respect to stability and antimicrobial activity. Thus, formulation containing 1% ketoconazole could be used as an effective antidandruff hair styling gel.

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Mucilage extracted from Ocimum gratissimum seeds were subjected to toxicity studies for its safety and preformulation studies for its suitability as a suspending agent. Zinc oxide suspensions were prepared and compared with different concentrations of Ocimum gratissimum mucilage, tragacanth and sodium CMC. The mucilage extracted is devoid of toxicity. The mucilage was found to be a superior suspending agent than tragacanth and is comparable to sodium CMC. Studies indicate that the extracted mucilage may be a good source as a pharmaceutical adjuvant specifically as a suspending agent.

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A simple visible spectrophotometric method has. been developed for the estimation of repaglinide in tablet formulations. Beer's law is obeyed in the concentration range of 5-50 μg/ml of repaglinide. The method is simple, precise and accurate for pure analyte with recovery of 99.5-99.9%. It does not require any separation of soluble excipients present in tablets, as they do not interfere in the estimation.

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A simple, sensitive HPTLC method was developed for the analysis of atorvastatin calcium in its commercial single component tablet formulations (10 mg/tablet). The stationary phase was precoated silica gel 60 F254. The mobile phase used was a mixture of benzene: methanol, (7:3 v/v). Combination of benzene: methanol offered optimum migration (RF=0.46±0.02). Detection of the spots was carried out at 281 nm. The method was validated in terms of linearity (200-600 ng/spots), precision (intra-day variation: 0.25 to 1.01%, inter-day variation: 0.21 to 0.88%), accuracy (99.2±0.48) and specificity. The limit of detection and limit of quantification for atorvastatin calcium were found to be 40 ng/spot and 200 ng/spot, respectively. The proposed method was successfully applied to determine atorvastatin calcium content of 10 individual tablet units o f two market formulations, after extracting atorvastatin calcium with methanol. Both the formulation complied with the USP specifications (RSD less than or equal to 6 %) of the content uniformity test. The proposed HPTLC method can analyse ten or formulation units simultaneously on a single plate and provides a faster and cost-effective quality control tool for routine analysis of atorvastatin calcium tablet formulation.

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Sulfonamides exhibit broad range of biological activities. Several sulfonamides are used in therapy such as celecoxib, nimesulide, delavirdine, acetazolamide, methazolamide, furosemide, ethoxzolamide, dichlorphenamide, dorzolamide, brinzolamide, sulpiride, sotalol, tolbutamide, chlorpropamide, tolazamide, acetohexamide, glipizide, gliburide, glymidine, zonisamide, thiothixene and famotidine. So far, modifications of the sulfonamides have proven highly effective and modifications that have been made so far do not exhaust the possible changes that can be made to improve potency and efficacy of these sulfonamides. The present review highlights the recently synthesized sulfonamides possessing important potential biological activities. It would be interesting to see whether new sulphonamide derivatives can be utilized as potent therapeutic agents in future.

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From the 2-butanone fraction derived out of the aqueous alcoholic extract of the fresh aerial parts of Alternanthera pungens, three C-glycoflavones, vitexin (1), isovitexin (2) and orientin (3) and an yellow solid composed of their 2"-O-β-D glucopyranosides (4-6) were isolated and characterised. Fully assigned sets of proton and carbon resonances, based on detailed 1D and 2D NMR measurements, including 1H COSY, HMQC and HMBC experiments, enabled the deduction of definitive evidence for the C- and the O-glycosidic linkages of the three biosides. Antioxidant potential of these six compounds was evaluated using two different assays, namely, the Trolox equivalent antioxidant capacity and the coupled oxidation of B-carotene and linoleic acid (autoxidation) assays. Compounds 3 and 6 were fairly active while the others were mildly active in both the assays.

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The antimicrobial activity of the different extracts of the stem bark of Toddalia asiatica was performed on Staphyloccus aureus, Escherichia coli and Candida albicans, respectively. Screening for wound healing activity was performed by excision wound model and incision wound model with both uninfected and infected wound with cocktail of bacteria comprising Staphyloccus aureus and Escherichia coli. The results of antimicrobial activity revealed that all the extracts exhibited varying degree of antibacterial activity against Staphyloccus aureus and Escherichia coli but none of the extracts were effective against Candida albicans. The studies on excision and incision wound healing models with and without infection showed that there is almost complete healing on the 12th post wounding day with all tested extracts. The degree of wound contraction with all extracts were in order of petroleum ether extract>chloroform extract>acetone extract>ethanol extract>aqueous extract. After infection with cocktail of tested bacteria, the order of tensile strength of the wounds of the animals treated with different extracts remained unchanged. The above findings justify potential wound healing properties of the stem bark as suggested in the folklore claims.

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The purpose of research was to evaluate suitability of sorbitan monosterate organogels for nasal delivery of propranolol hydrochloride. The organogels of liquid paraffin were rigid and that with cottonseed and sesame oil were weak. Sorbitan monosterate organogels in isopropyl myristate has desired stability and consistency. Water incorporates the desired polarity for gel formation while alcohol breaks the interconnected gel network. The X-ray diffraction pattern confirms incorporation of water in micellar gel network. Polysorbate cosurfactants enhance the stability of organogeis by increased viscosity. The viscosity increase was proportionate to chain length of tween surfactants. The water holding capacity, and hence the electrical conductivity increases with sorbitan monosterate concentration. The release retardant effect of propranolol hydrochloride through sheep nasal mucosa was observed with the order of Tween 20<Tween 60<Tween 80. The organogels exhibit useful pharmaceutical properties. However the gels need to be further optimized for sustain transnasal drug administration.

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To study the antiinflammatory activity of Nothapodytes foetida, Miers using Wistar rats of either sex, the leaves of Nothapodytes foetida were extracted using petroleum ether and then with ethanol for 72 h each. Both the extracts were in 3 dose levels of 50 mg/kg, 100 mg/kg and 200 mg/kg. Antiinflammatory activity of the extracts was studied by carrageenan-induced hind paw edema in rats and the paw measured plethysmometrically at 0,2 and 4 h after injection. The activities of the extracts were compared with control and standard, ibuprofen. All the drugs were administered orally. When compared to the petroleum ether extract the antiinflammatory activity of ethanolic extract was found to be effective and 200 mg/kg dose of ethanolic extract significantly (P<0.01) reduced the inflammation, which was comparable with that of the standard, ibuprofen.

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A simple and sensitive spectrofluorimetric method was developed for the determination of atenolol in tablet dosage forms. The method was based on the reaction of atenolol with 0.1 N sodium hydroxide solution in boiling water bath, which shows strong fluorescence having excitation and emission wavelengths 278 nm and 302 nm, respectively. Linear relationship for the fluorescence - intensity was obtained in the concentration range of 5.0-25.0 μg/ml. The method was validated. statistically and was applied successfully for the determination of atenolol in tablet dosage forms.

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In an effort to search for more active CNS depressants, a series of spirobarbiturates incorporated with thiazolidinones and azetidinones were synthesized and evaluated for their sedative, hypnotic and anticonvulsant activities. Starting bis compounds (1a-d) were prepared from the reaction of acetone and substituted aldehydes. These bis compounds on Michael addition with barbituric acid give rises to triones (2a-d), which on condensation with NH2NH2.H2O afforded (3a-d) which on reaction with different aromatic aldehydes afforded and Schiff bases (4a-n). These on cyclocondensation with thiolactic acid and chloroacetyl chloride furnished the final products (5a-n) and (6a-n), respectively. Result of toxicity studies and central nervous system depressant activities of these compounds are reported. The structures of the products have been delineated by chemical reaction, elemental analysis and spectral studies.

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Nalidixic acid and metronidazole in combination are routinely used as antidiarrhoeal. The present investigation attempts to develop estimation method for these two drugs in combined dosage forms. It was found that both the drugs follow the Beer's Law from 2.0-10.0 μg/ml and 2.0-12.0 μg/ml at 257 and 277 nm, respectively. The absorptivity (1%, 1 cm), values at the specified wavelengths for nalidixic acid was found to be 1232.84 and 211.05, respectively and for metronidazole 263.65 and 376.18, respectively. Thus, the present method is simple, rapid and accurate and is based on the principle of simultaneous UV spectrophotometric determination of binary mixture.

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An attempt has been made to enhance solubility and dissolution of rofecoxib by complexation using dimethyl β-cyclodextrin. Complexes were prepared by physical mixture, kneading and spray drying methods. The prepared complexes were evaluated by Fourier transform infra-red spectroscopy, X-ray diffraction, differential scanning calorimetry and scanning electron microscopy. Release profile of the drug from the complexes were studied in pH 1.2 and pH 7.4 and it was found that the marketed preparation showed lesser release characteristics as compared to the complex prepared by kneading method.

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The binding of nimesulide, a cox-2 inhibitor, to bovine serum albumin was investigated by equilibrium dialysis method at different temperatures and pH conditions. The Scatchard plots were prepared based on these drug-protein binding data. The number of binding sites (n), the value of association constant (K) at different conditions and different thermodynamic parameters (i.e., standard free energy change ΔG°, standard enthalpy change ΔH° and standard entropy change ΔS°) of nimesulide-BSA binding were determined. The result shows that number of binding sites is around 2.5 and the value of association constant is decreasing with increasing temperature and pH. It also reveals that the value of ΔG° and ΔH° were highly negative and ΔS° was also negative. The result indicates that the interaction between nimesulide and bovine serum albumin is exothermic and spontaneous in nature. It is postulated that nimesulide-bovine serum albumin interaction may occur due to hydrogen bond formation and ionic interaction.

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lon-pair extractive spectrophotometric method was developed for the estimation of repaglinide. This method is based on the formation of an yellow colored ion-pair complex with bromothymol blue in presence of acid phthalate buffer (pH 2.4). This complex was then extracted with chloroform. The color of resulting solution was determined at λmax 438 nm. The calibration curve was found to be linear in the range of 5 to 25 μg/ml. The recovery study values ranges from 98 to 100% and % RSD was found to be 1.183.The LOD and LOQ were found t o be 0.97 μg/ml and 3.25 μg/ml, respectively. The method was found to be precise, accurate and sensitive. The method can be successfully applied for its tablet formulation.

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A simple, fast, precise and accurate reverse phase HPLC method was developed for the simultaneous estimation of paracetamol and rofecoxib in tablets. This method is based on using a Hypersil C18 column with a mobile phase of 20 mM phosphate buffer (pH 7.0±0.1) and acetonitrile in the ratio of 55:45 v/v. Valdecoxib was used as an internal standard-The retention times for paracetamol, rofecoxib and valdecoxib were 2.61, 10.09 and 12.31 min, respectively. The proposed method has also been validated. The method was found to be linear (r>0.999), precise (RSD: 0.82% for paracetamol, 0.42% for rofecoxib), accurate (mean percentage recovery yields: 99.3% for paracetamol and 98.4% for rofecoxib) and selective. Due to these attributes, the proposed method could be used for routine quality control analysis of these drugs in combined dosage forms.

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Two new reagents, neocuproine and bathocuproine are proposed for simple, sensitive and selective spectrophotometric methods for the determination of dibenzazepine class of drugs. In the proposed method copper (lI) reacts with imipramine hydrochloride, desipramine hydrochloride, clomipramine hydrochloride, trimipramine maleate and opipramol and subsequently with neocuproine or bathocuproine in an acetic acid medium to yield yellow or orange-red colour, with maximum absorption at 460 or 480 nm, respectively. A reaction mechanism is proposed with drug - metal and reagent ratio of 1:2.

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A facile synthesis of 4-aryl-thieno-[2,3-d]-pyridazines (4a-g) have been achieved by cyclisation of 1-aroylhydrazones (3a-g) using polyphosphate ester. All the synthesized compounds have been characterized by elemental analysis and spectral data. In addition, they were screened for antibacterial, antifungal, anticonvulsant and antiinflammatory activities.

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We sought to determine that whether acute and delayed cardioprotection offered by remote aortic preconditioning involves gadolinium sensitive-stretch activated channels. Hearts of sham operated rats, isolated 40 min and 24h after the isolation of abdominal aorta, were subjected to global ischaemia for 30 min followed by reperfusion for 120 min. Coronary effluent was analyzed for lactate dehydrogenase and creatine kinase release to assess the degree of cardiac injury. Myocardial infarct size was estimated macroscopically by using triphenyl tetrazolium chloride staining. Remote aortic preconditioning, immediately and 24 h before, subjecting the isolated heart to 30 min ischaemia and 120 min reperfusion markedly reduced lactate dehydrogenase and creatine kinase release in coronary effluent and myocardial infarct size. lntraperitoneal administration of gadolinium chloride (30 mg/kg) showed protection against sustained ischaemia and reperfusion whereas it did not seems to modulate the cardioprotective effect of remote aortic preconditioning. On this basis we concluded that the cardioprotective effect of remote aortic preconditioning did not involves stretch-activated channels.

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