A simple, specific and accurate reverse phase high performance liquid chromatographic method was developed for the simultaneous determination of atorvastatin calcium and aspirin in capsule dosage forms. A phenomenex Gemini C-18, 5 mm column having 250 x 4.6 mm i.d. in isocratic mode, with mobile phase containing 0.02 M potassiumdihydrogen phosphate: methanol (20:80) adjusted to pH 4 using ortho phosphoric acid was used. The flow rate was 1.0 ml/ min and effluents were monitored at 240 nm. The retention times of atorvastatin calcium and aspirin were 5.4 min and 3.4 min, respectively. The linearity for atorvastatin calcium and aspirin were in the range of 0.5-4 mg/ml and 5-25 mg/ml, respectively. The recoveries of atorvastatin calcium and aspirin were found to be in the range of 98.02-100.68% and 98.38-101.42%, respectively. The proposed method was validated and successfully applied to the estimation of atorvastatin calcium and aspirin in combined capsule dosage forms.

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Microspheres of diltiazem hydrochloride were formulated using combination of polyethylene glycol 6000 and Eudragit RS 100 and Eudragit RS 100 alone by solvent evaporation and non-solvent addition methods with an aim to prolong its release. Six formulations prepared by using different drug to polymer ratios, were evaluated for relevant parameters and compared with marketed SR capsules. Depending upon the drug to polymer ratio, the entrapment, loading and encapsulation were found to range between 77.45±0.22 to 91.08±0.62% , 34.76±0.15 to 52.46±0.25% and 66.09±0.19 to 82.7 ±0.57%, respectively. The microspheres were spherical, discrete and compact and size distribution was between 4 to 24 µm. In vitro studies were carried out at different pH for a period of 12 h and compared with marketed formulation. As similarity factor f2 was 92.8 for FVI, it was subjected to further study. Formulations prepared using the combination of the retardants exhibited first order of drug release and zero order for preparations containing Eudragit RS 100 alone. The analysis of regression values of Higuchi plot and Korsmeyer-Peppas plot and "n" values of Korsmeyer-Peppas model suggested a combination of diffusional and dissolutional mechanism indicating the drug release from the formulations was controlled by more than one process. Drug polymer interaction was absent as evidenced by FT-IR and DSC thermograms. In vivo pharmacokinetic study of the formulation proved that prolongation of drug release was obtained by formulating as microspheres.

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The ability to deliver therapeutic agents to a patient in a pulsatile or staggered release profile has been a major goal in drug delivery research recently. This review will cover methods that have been developed to control drug delivery profile with different polymeric systems. Externally and internally controlled systems will be considered, including a range of technologies like preprogrammed systems as well as systems that are sensitive to modulated enzymatic or hydrolytic degradation, pH, magnetic fields, ultrasounds, electric fields, temperature, light and mechanical stimulation. These systems have the potential to improve the quality of life for patients undergoing therapy with a variable dosing regime.

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A reverse phase high performance liquid chromatography method was developed for the simultaneous estimation of aspirin and clopidogrel bisulphate in formulation. The separation was achieved by octadecyl column (C ₁₈ ) and acetonitrile:methanol:20 mM phosphate buffer at pH 3 (50:7:43 v/v) as eluent, at a flow rate of 1 ml/min. Detection was carried out at 240 nm. Quantitation was done by external standard calibration method. The retention time of aspirin and clopidogrel bisulphate was found to be 2.40 and 9.27 min, respectively. The method has been validated for linearity, accuracy and precision. Linearity for aspirin and clopidogrel bisulphate were in the range of 10-50 µg/ml for both the drugs. The mean recoveries obtained for aspirin and clopidogrel bisulphate were 100.86% and 100.20%, respectively. The developed method was found to be accurate, precise, selective and rapid for the simultaneous estimation of aspirin and clopidogrel bisulphate in capsules.

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A derivative spectrophotometric procedure has been developed for the simultaneous determination of individual combination of aceclofenac and tramadol with paracetamol in combined tablet preparation. Tablet extracts of the drugs were prepared in distilled water. The zero crossing point technique and the compensation technique were used to estimate the amount of each drug in the combined formulations, and were compared. The results were found to be accurate and free from interferences. The procedure is rapid, simple, nondestructive, and does not require solutions of equations. Calibration graphs are linear (r=0.9999), with a zero intercept up to 24 mg/ml of each drug in combination with paracetamol. Detection limits at the p = 0.05 level of significance were calculated to be 0.5 mg/ml of aceclofenac, tramadol and paracetamol respectively.

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Mucoadhesive buccal tablets of metoprolol tartarate were fabricated with objective of avoiding first pass metabolism and prolonging duration of action. The mucoadhesive polymers used in formulation were Carbopol-934, hydroxypropylmethylcellulose, hydroxyethylcellulose and sodium carboxymethylcellulose. The formulations were characterized for physiochemical parameters, in vitro release studies and in vivo placebo studies. The best mucoadhesive performance and in vitro drug release profile were exhibited by the tablets containing hydroxyethylcellulose and Carbopol-934 in ratio 1:2. This product was more comfortable to the user due to absence of erosion, faster hydration rate and less viscosity of surrounding environment. In vivo placebo studies did not show any side effects.

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Ultra thin multilayer capsules are attractive and stable systems capable of delivering the bioactives. Ultra thin multilayer capsules consist of polyelectrolytic materials that are formed in the presence of a template. This is achieved through layer-by-layer adsorption of oppositely charged macromolecules on to colloidal particles. Upon extraction, the resulting cavities retain affinity for the bioactives. This review considers the fabrication, of ultra thin multilayer capsules, physiochemical properties and role of ultra thin multilayer capsules within a pharmaceutical remit. Ultrathin multilayer capsules have potential for creating satisfactory drug dosage forms.

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Steam distillation, petroleum ether, and ethanol extracts from Hyptis suaveolens leaves were evaluated for their antimicrobial activity in vitro . Steam distillation extract exhibited broad-spectrum antibacterial and antifungal activity against the tested organisms. It showed highest antifungal and antibacterial activity against Aspergillus niger and Micrococcus luteus, respectively. Activity indices of A. niger against miconazole (25 µg/ml) and M. luteus against chloramphenicol (10 µg/ml) were 0.89 and 0.67, respectively.

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Acyclovir, an antiviral is used in the treatment of ocular infections. Acyclovir is effective against human herpes viruses including Herpes simplex virus type 1 and 2, Varicella Zoster virus, Epstein-Barr virus and Cytomegalovirus. Acyclovir is available as a 3%w/w eye ointment to be applied 5 times a day in the eye. The present investigation was aimed at designing a twice a day ocular inserts of acyclovir by melt extrusion technique to improve patient compliance, using hydroxypropylcellulose as a thermoplastic polymer. Also, the developed formulation would overcome the greasy nature of the eye ointment. The developed inserts were stable, non-irritant and provided release of the drug over a period of 10 hours in vitro .

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This study was carried out to assess the influence of pharmacist provided patient counseling on patients' perception about the disease management and quality of life in type 2 diabetes mellitus patients. The present study was a randomized, prospective controlled study conducted over a period of six months in two community pharmacies in Calicut, Kerala, India. A total of seventy (48 male and 22 female) type 2 diabetes mellitus patients were enrolled and randomized into test and control groups. Patients in the test group received patient counseling and patient information leaflets from the pharmacist, where as the control group patients received the counseling and patient information leaflets only at the end of the study. After the baseline, two follow-ups were made with sixty days interval between the follow-ups. During each visit patient's random capillary blood glucose was measured by using a standard Glucometer. Suitably designed and validated knowledge, attitude and practices questionnaire was administered at baseline and final follow up for both test and control group patients to assess the disease management awareness. Audit of diabetes-dependent quality of life questionnaire was administered to measure the quality of life in both control and test group patients at each follow up. At the end of the study, knowledge, attitude and practices scores found markedly improved in test group patients. Mean capillary blood glucose levels were decreased in test group ( P <0.05) and an improvement in mean quality of life scores ( P <0.05) was observed. Where as a reduction of quality of life score ( P <0.05) and a non-significant increase of capillary blood glucose levels ( P >0.05) was observed in the control group patients. The correlation between the capillary blood glucose levels and quality of life scores were also found to be highly significant in the test group (r= 0.955). The results of the study suggests that, pharmacist provided patient counseling has an impact in improving the perception about disease, diet and life style changes and in turn on glycemic control and overall quality of life in diabetic patients. Pharmacist provided patient counseling might be considered as an important element in implementing the disease management program.

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Ayurvedic eye drops preparation contains aqueous extracts of different herbs. Ethnobotanical survey shows that plants used in Ayurvedic eye drops formulation are rich source of tannin and tannin like compounds. Antioxidant and antimicrobial properties of ayurvedic eye drops are attributed to the presence of tannins and tannin like compounds. Therefore in the present study an attempt has been made to determine the tannin content in some ayurvedic eye drops, by using Folin-Denis method. A blue colored complex is formed by using phosphotungustomolybdic acid. Estimation was done on UV/Vis spectrophotometer. The tannin content of all the three brands was found to be 420, 918 and 270.49 µg/ml. The results obtained are reproducible with coefficient of variation less than 1.0% . Hence the present approach can be used as one of the parameters for the standardization of ayurvedic eye drop preparations.

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Three simple, accurate, economical and reproducible UV spectrophotometric methods for simultaneous estimation of two component drug mixture of ranitidine hydrochloride and ondansetron hydrochloride from combined tablet dosage form have been developed. First developed method involves formation and solving of simultaneous equations at 267.2 nm and 314.4 nm. Second method was developed making use of first order derivative spectroscopy using 340.8 nm and 276.0 nm as zero crossing points for estimation of ranitidine hydrochloride and ondansetron hydrochloride respectively. Third method is based on two wavelength calculation, wavelengths selected for estimation of ranitidine hydrochloride were 266.1 nm and 301.8 nm and for ondansetron hydrochloride 305.7 nm and 319.2 nm. The results of analysis have been validated statistically and by recovery studies.

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An attempt has been made to develop buccoadhesive bilayered tablets comprising of drug containing bioadhesive layer and drug free backing layer to release the drug for extended period of time with reduction in dosing frequency. Tablets of terbutaline sulphate were prepared by direct compression method using bioadhesive polymers like Carbopol 934P, Methocel K4M, Methocel K15M and sodium carboxy methyl cellulose either alone or in combinations with backing layer of ethyl cellulose. The physical characteristics, swelling index, surface pH, in vitro bioadhesion strength, and in vitro release of formulated tablets were shown to be dependent on characteristics and composition of bioadhesive materials used. The modified in vitro assembly was used to measure and compare the bioadhesive strength of tablets with fresh porcine buccal mucosa as a model tissue. The maximum bioadhesive strength was observed in tablets formulated with Carbopol 934P alone and strength decreases with decrease in its content. The tablets were evaluated for in vitro release in pH 6.8 phosphate buffer for 10 h using a standardized dissolution apparatus. In order to determine the mode of release, the data was subjected to Korsmeyer and Peppas diffusion model. All the formulations followed non-Fickian release mechanism. Carbopol 934P and Methocel K4M in the ratio of 1:1 could be used to design effective and stable buccoadhesive tablets of terbutaline sulphate.

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Novel mucoadhesive chitosan microspheres were developed to explore the possibilities of non invasive delivery of insulin. The mucoadhesive chitosan microspheres were prepared by emulsification method. Formulations were characterized for various physiochemical attributes, shape, surface morphology, size and size distribution, drug payload, swelling ability and mucoadhesion. Mucoadhesive chitosan microspheres bearing insulin were evaluated for in vitro drug release and in vitro drug permeation through mucosal membrane. In vivo performance was studied on blood plasma level of glucose. Glutaraldehyde cross-linked microspheres showed better reduction of blood glucose level than citric acid cross-linked microspheres. The in vivo performance of mucoadhesive microspheres showed prolonged and controlled release of drug as compared with the conventional dosage form.

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Two simple, specific, accurate and precise methods, namely, reverse phase high performance liquid chromatography and high performance thin layer chromatography were developed for estimation of nebivolol hydrochloride in tablet dosage form. For the HPLC method, Lichrospher 100 C-18, 5 µm column consisting of 200×4.6 mm i.d. in isocratic mode, with mobile phase containing 50 mM KH ₂ PO ₄ buffer (pH 3.0±0.1):acetonitrile: (45:55 v/v) was used. The flow rate was 1.0 ml/min and effluent was monitored at 282 nm. The retention time was found to be 3.76±0.02 min. For the high performance thin layer chromatographic method a Camag system comprising of Linnomat V automatic sample applicator, Hamilton syringe, Camag TLC Scanner-3, Camag Win CAT software with stationary phase precoated silica gel 60F ₂₅₄ and mobile phase consisting of ethyl acetate:toluene:methanol: ammonium hydroxide (1:6:2:0.1 v/v/v/v) were used. The detection of spot was carried out at 282 nm. The R _f value was found to be 0.33±0.02. The methods were validated in terms of linearity, accuracy and precision. The linearity curves were found to be linear over 10-150 µg/ml for high performance thin layer chromatography and 100-600 ng/spot for high performance thin layer chromatography. The limit of detection and limit of quantification for high performance thin layer chromatography were found to be 2.0 and 10 µg/ml, respectively, and for the high performance thin layer chromatography, 30 and 100 ng/spot, respectively. The proposed methods were successfully used for estimation of nebivolol hydrochloride in tablet dosage form.

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According to the local traditional healers in Ooty, leaves of Passiflora mollissima Bailey are being used as an antidiabetic drug. In this direction, the ethanol extract of Passiflora mollissima was tested for its anti diabetic activity in alloxan-induced diabetic rats. The extract was studied at two dose level, 100 mg/kg and 200 mg/kg respectively. The activity was compared with reference standard, phenformin and control. The plant extract at a dose of 100 mg/kg and 200 mg/kg significantly ( P <0.001) lowered the blood sugar level of hyperglycemic rats.

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A simple and reproducible high performance thin layer chromatography method for the determination of tinosporaside in Tinospora cordifolia was developed and is described. This method involves separation of compounds by TLC on pre-coated silica gel 60F 254 plates with a solvent system of toluene: acetone: water (5:15:1) and scanned using densitometric scanner in UV reflectance photomode at 220 nm. The linearity was observed in the range of 0.5 to 8 mg. The tinosporaside content of 0.40% w/w was observed in test sample. The average percentage recovery value of 99.24±0.49 was obtained. The proposed method being precise and sensitive can be used for detection, monitoring and quantification of tinosporaside in Tinospora cordifolia .

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The phytochemical studies on the leaves of Prosopis cineraria resulted in isolation of methyl docosanoate, diisopropyl-9,10-dihydroxyicosane-1,20-dioate, tricosan-1-ol and 7,24-tirucalladien-3-one. While diisopropyl-10,11-dihydroxyicosane-1,20-dioate is a hitherto unreported compound, methyl docosanoate, tricosan-1-ol and 7,24-tirucalladien-3-one are being reported for the first time from P. cineraria . These compounds have been characterized on the basis of spectral and other data.

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Nifedipine, an important therapeutic agent in the management of cardiovascular disorder is recommended to administer as modified release dosage form in order to avoid the fluctuations in blood levels. An in vitro evaluation of modified release formulations, marketed in India was conducted and compared their performance with a novel matrix-based multi particulate system. The results indicate that even though the marketed formulations are found to comply to the definition of modified release formulations and predicted to produce therapeutic blood level for a prolonged period of time, the fluctuations were expected to be found uncontrolled except in the osmotic systems and the matrix-based multi particulate system. Thus, it was concluded that novel matrix-based multi particulate system were found to be superior to any other marketed formulations with respect to the therapeutic advantage as well as manufacturing feasibility.

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Since oral bioavailability of atenolol and metoprolol tartrate is poor, different matrix -type transdermal patches incorporating atenolol and metoprolol tartrate were formulated with an objective to study the effect of polymers on transdermal release of the drugs. The polymers selected were polyvinylpyrrolidone, cellulose acetate phthalate, hydroxypropylmethylcellulose phthalate and ethyl cellulose. The patches were formulated using combination of polymers and propylene glycol and 1,8-cineole as plasticizer and penetration enhancer, respectively. The physico-chemical evaluation of the polymer matrices was performed for suitability. The interaction among various components of the matrices was studied by performing Differential Scanning Calorimetry and Scanning Electron Micrography of the formulated patches. In vitro permeation studies were performed using rat abdominal skin as the permeating membrane in Keshary-Chien cell. The results indicated that maximum release was obtained at 48 h (85% and 44% of atenolol and metoprolol tartrate, respectively). The drug permeation studies across cadaver skin showed about 27% of reduction in the amount of drug release as that compared to rat abdominal skin was used.

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Cyclosporine A is an immunosuppressive agent, which is widely used for organ transplantation, autoimmune and other diseases. Cyclosporine inhibits the calcineurin and thereby causes inhibition of chondrogenesis. Cyclosporine crosses the placenta and reaches to the embryo, and thereby may affect them. Many females, that should receive cyclosporine, are in childbearing age. The objective of this study was to determine whether cyclosporine administration has any effect on weight and crown-rump length of mouse embryos. Many out bred adult mice were selected. Female mice were mated overnight with males, checked in the morning for vaginal plug. Pregnant mice were randomly assigned into experimental and control groups. The experimental group received cyclosporine and control group received an equivalent amount of olive oil on days 7, 8, and 9 of gestation. Pregnant mice were killed and embryos were removed on days 13, 16, and 18 of gestation. The weight and crown-rump length of embryos were recorded. Comparison between two groups was made using t. test. There were highly significant differences between crown-rump length of experimental and control groups on days 16 and 18 ( P <0.05), but on day 13, crown-rump length difference was not significant. In all ages of gestation, the experimental group had less weight than the control group ( P <0.05). Results of this study indicate that cyclosporine causes low weight and low crown-rump length in mice embryos.

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Complexing a drug may alter the rate and extent of drug absorption. The complex formation is very well applied in the administration of poorly water-soluble drugs. The drugs selected for the study are cyclooxygenase-2 inhibitors, are potent anti-inflammatory drugs with very low water solubility. The water solubility of these drugs was enhanced by complexing with β -cyclodextrin. In vitro absorption studies using isolated inverted bovine gut technique showed greater rate of transport of these drugs when complexed with β -cyclodextrin. The increase in the rate of transport is due to the formation of inclusion complexes with β -cyclodextrin that in turn increases the absorption. Studies also reveal that as the concentration of complexing agent increases the rate of absorption also increases proportionately. A statistical correlation was attempted between the mean percent drug dissolved at time 't' and quantity of drug absorbed at time 't/2'. When relation of in vitro drug dissolution and in vitro drug absorptions were studied, it was found that the r ² -values for all formulations are within 0.947 to 0.997. This indicates a strong positive correlation between the in vitro drug dissolution and absorption of the drug through everted gut.

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The objective of this study was to obtain an optimum formulation for microencapsulating venlafaxine hydrochloride ion-exchange resins. This was achieved by investigating various factors which influenced the drug release. The percentage of drug released was used as an index to investigate the individual factor. The optimum coating formulation was acquired by orthogonal experiments in which the concentration of coating material in acetone was 3%, the ratio of drug-resin complexes to coating materials was 8:1 and the ratio of plasticity-agent to coating material was 5%. The results indicated that the use of ion-exchange resins along with a suitable coating material would be a feasible way to prepare a marked prolonged release type of microcapsules by the emulsion solvent diffusion method.

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The proposed method is a simple, accurate, precise, specific and rapid method for the simultaneous estimation of gatifloxacin and ornidazole in bulk and tablet formulations. A column in isocratic mode, with a mobile phase consisting of acetonitrile: 0.025 M potassium dihydrogen phosphate buffer (50:50 v/v) with 0.5% v/v of triethylamine and its pH adjusted to 3.0 with glacial acetic acid were used. The flow rate was set at 1.0 ml/min and UV detection was carried out at 300 nm. The retention time of gatifloxacin and ornidazole were 2.89±0.017 min and 4.21±0.022 min, respectively. Linearity of gatifloxacin and ornidazole were found in the range of 2-24 µg/ml and 5-60 µg/ml, respectively. The developed HPLC method was extended for dissolution studies. The dissolution testing was performed at 50 rpm and 100 rpm in 0.1 N hcL0 as dissolution medium by paddle method.

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Tablets of aspirin (a moisture degradable drug) have been film coated with two analogous Eudragit RL and RS copolymers designated here as A and B which differ only in their cation content in the ratio 2:1 (A:B). A, is therefore more hydrophilic than B. The tablets were film coated with ethanol solutions of these two polymers. Film coating with either A or B significantly reduced the moisture uptake potentials of the tablets but caused an increase in the disintegration times of the tablets and retarded dissolution rates. The mean disintegration times were 0.5±0.1 min (uncoated tablets), 16±2.5 min (tablets coated with A) and 115±3.6 min (tablets coated with B). The corresponding dissolution rates % h ^-1 were 28.3 for uncoated, 16.6, coated with A and 14.8, coated with B, respectively. Thus, coating with polymer B considerably impaired the disintegration and dissolution properties of the tablets.

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A simple and sensitive high performance thin layer chromatography (HPTLC) method has been developed for the quantitative estimation of linezolid in its single component tablet formulations (600 mg). Linezolid was chromatographed on Silica Gel 60 F₂₅₄ TLC plate using methanol: benzene (2:8 v/v) as mobile phase. Linezolid showed Rf value 0.45 + 0.03 and scanned at 258 nm using a Camag TLC scanner 3. The method was validated in terms of linearity (200-1400 ng/spot), precision (intra-day variation, 0.75 to 1.26% and inter-day variation, 1.2 to 2.8%), accuracy (97.8 to 100.4%) and specificity. The limit of detection and limit of quantification for linezolid were found to be 16.7 ng/spot and 50.7 ng/spot, respectively. The developed method was successfully used for the assay of linezolid tablet formulations. The method was found to be simple, sensitive, specific, accurate and precise and can be used for the routine quality control testing of linezolid marketed formulations.

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Antifungal activities of different extracts of Millingtonia hortensis were investigated against various fungal pathogens. Methanol extract was found to have stronger activity than fluconazole against yeast like fungi: 4 fold against Candida krusei with 4 µg/ml minimal inhibitory concentration and 2 fold (MIC- 2 µg/ml) against Sacharomyces cerevisiae , though it showed the same activity as fluconazole against Candida glabrata . Aqueous extract also exhibited 4 fold stronger activity against Candida krusei (MIC- 4 µg/ml) and 4 fold (MIC; 2 µg/ml) against Sacharomyces cerevisiae . Chloroform and ethyl acetate extract showed lower activities against all fungal pathogens except for Candida krusei, compared with the standard. Against the filamentous fungus, Trichosporon cutaneum , all extracts showed less activity than the standard.

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Antioxidant activity of the crude methanol extract of Pseudarthria viscida (L) Wight and Arn. stem and root was performed by1,1-diphenyl-2-picrylhydrozyl (DPPH) radical quenching assay and reducing power test models. Both stem and root extracts exhibited potential antioxidant activity in both the assays.

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4,6-Diaryl substituted-4,5-dihydro-2-amino pyrimidines have been synthesized by the reaction of chalcones with guanidine nitrate. Their chemical structures have been confirmed by means of IR and NMR data and by elemental analysis. The compounds were screened for antibacterial activity against 16 gram-positive bacterial strains in minimum inhibitory concentration. The minimum inhibitory concentration of the compound II has found to be better than the reference standards taken for the antibacterial screening. Sulphamethoxazole and trimethoprim were taken as reference standards.

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A series of nicotinyl 4-oxathieno[2,3- d ]pyridine-2-ylmethyl esters, title compounds were synthesized. Compound IIIa was subjected to in vivo antihyperlipidemic activity in Wistar rats. The activity exhibited by synthesized compound was found to be less as compared to that produced by a standard, atorvastatin, administered in the form of suspension in 2% gum acacia. The activity was even lesser than that produced by the lead IIa.

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Two simple methods, ultra violet spectroscopy and high performance thin layer chromatography for the determination of ropinirole in tablet dosage form are described. Detection wave lengths for spectrophotometric and high performance thin layer chromatographic methods were found to be 250 nm and 254 nm, respectively. For the spectrophotometric method, the linearity was found to be in the range of 5-30 mg/ml and for high performance thin layer chromatographic method; linearity was found to be between 40 and 120 mg/ml.

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