Usha

Oral route is the easiest and most convenient route for drug administration.  The major problem in oral drug formulations is low and erratic bioavailability, which mainly results from poor aqueous solubility. This may lead to high inter and intra subject variability, lack of dose proportionality. It is estimated that 40% of active substances are poorly water soluble. The solubility of such drugs is increased by formulating self emulsifying drug delivery system (SEDDS). Self emulsifying drug delivery systems have gained exposure for their ability to increase solubility and bioavailability of poorly water soluble drugs. SEDDS are isotropic mixtures of oil, surfactants, solvents and co-solvents/surfactants, which emulsify to produce fine oil-in-water emulsions upon gentle agitation. SEDDS typically produce emulsions with a droplet size between 100–300 nm. Solid SEDDSs are being developed from liquid/semisolid SEDDS mainly by adsorption on solid carriers, spray drying, lyophilization, melt extrusion, and nanoparticle technology. This review focuses on newer approaches for development of SEDDS and Solid SEDDS.

1,4-Benzothiazine derivatives having variable antifungal activity against four species of fungus such as Candida albicans, Trichophyton rubrum, Epidermophyton floccosum and Malassazia furfur  were selected to develop 2D and 3DQSAR models. The best 2DQSAR model was selected, having correlation coefficient r2 (0.8747) and cross validated squared correlation coefficient q2 (0.7145) with external predictive ability of pred_r2 (0.9658). 2DQSAR parameters are Quadrople1, SssCH2count, XA Average hydrophobicity, X Amost hydrophilic area and Polar surface area excluding P and S contributed in the model. The best 3DQSAR model having the correlation coefficient r2= 0.8635 was selected for further study. The model was further validated by means of crossed squared correlation coefficient q2 =0.7614 and pred_r2 =0.6654, which show that the model has good predictive ability and was developed by Forward SW-MLR. From QSAR model it concluded that the bulky substitution is require at para and meta position of Phenyl ring and less bulky substitution at ortho position of phenyl ring for antifungal activity.

A series of [Alkyl or un/substituted phenyl]-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-2-yl)acetamide were designed and synthesized. In vitro antifungal activity assay indicates that the 1,4-Benzothiazine has good antifungal activity against most of the tested pathogenic fungi i. e. Candida albicans, Trichophyton rubrum, Epidermophyton floccosum and Malassazia furfur. Some few compounds such as BTA-43 and BTA-56 have significant antifungal activity and broader spectrum, which are promising leads for the development of novel antifungal agents. The structures of the synthesized compounds were established on the basis of IR, NMR, 13CNMR and Mass spectra data.

A specific, accurate and precise reverse phase high performance liquid chromatographic method was developed and validated for the estimation of vardenafil in bulk and pharmaceutical formulation. A Hypersil BDS C 8, 5μ column having 250 x 4.6 mm internal diameter in isocratic mode with mobile phase containing buffer and acetonitrile (60:40, v/v) was used. The flow rate was 1.0 ml/min and effluents were monitored at 240.0 nm over the concentration range of 50-250 µg/ml. The retention time obtained for vardenafil was 5.4 min. The method was validated for linearity, accuracy, repeatability, precision, specificity (in terms of acid, alkali, peroxide and thermal degradation), limit of detection, limit of quantification and ruggedness. Chromatographic peak purity data demonstrated specificity of the method to estimate vardenafil in presence of degradation products.  Limit of detection and limit of quantification were found 0.0125 µg/ml and 0.025 µg/ml respectively. Accuracy in terms of recovery of vardenafil from tablet formulation was found to be above 98 % indicating that vardenafil can be estimated from tablet dosage form without interference from the excipients. The validation data proves the potential utility of the proposed method for the quantitative determination of vardenafil in tablet formulation.

Nelumbo nucifera Gaertn. (Family -Nymphaeaceae) commonly known as Indian lotus. Also known as the sacred lotus has been used in the indigenous system of medicine. Phytochemical constituents, free radical scavenging activity and total antioxidant activity of various extracts of Nelumbo nucifera flowers were carried out in the study. Phytochemicals were extracted from Nelumbo nucifera flowers using various solvents such as aqueous, benzene, chloroform, ethanol, ethyl acetate and methanol and petroleum ether. Screening of phytochemicals showed positive results for the presence of flavanoids, alkaloids, phenols, glycosides, carbohydrates and tannins. Phytochemicals were best extracted in methanol. The antioxidant activity of the extracts was measured in terms of reducing power and 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging capacity. The methanolic extract was found to possess comparatively higher antioxidant properties. So, the present data suggests that methanolic extract of lotus flower constitute significant amounts of phytochemical compounds and are good source of antioxidants.

A simple, accurate, precise and reproducible method has been developed for the simultaneous estimation of Vildagliptin and Metformin hydrochloride in combined tablet dosage forms. As there are no reported UV methods for the simultaneous estimation of Vildagliptin and Metformin hydrochloride in their combined dosage form, a need was felt to develop new methods to analyze the drugs simultaneously. The estimation was done by multi-wavelength technique, at wavelengths of 217 nm and 234 nm over the concentration ranges of 0.7µg/ml and 7 µg/ml with mean recovery 100% for both drugs Vildagliptin and Metformin hydrochloride respectively. The results of the analysis were validated statistically and recovery studies were carried out as per ICH guide lines. Thus the proposed method can be successfully applied for the simultaneous estimation of Vildagliptin and Metformin hydrochloride in routine analysis work.

Trigonella foenum-graecum (Fenugreek) (Leguminosae) is employed as a herbal medicine. Its seeds are known for their carminative, tonic and antidiabetic effects. A curative dose of Trigonella foenum-graecum also produces antiulcer action1. In this study we have investigated the Ethnopharmacological activities of the aqueous extract of the seeds Trigonella foenum-graecum in normal mice using different route of administration . The methanolic extract administered through the same route produced various effect only at the dose of 1 g/kg body weight. The aqueous extract is under further investigation to determine the chemical structure of the active component. The presence of hypoglycaemic, antiflamatory, antianalgesic activity in aqueous and methanolic extract indicates that the active compounds are polar in nature. The effects of fenugreek seed extract on the alterations in serum thyroid hormone concentrations were studied in adult male mice and rats. Simultaneously, hepatic lipid peroxidation and the activities of the antioxidant enzymes, viz superoxide dismutase  and catalase were examined. Present study reports analgesic activity of petroleum ether, chloroform, ethyl acetate and methanolic extracts of leaves and seeds of Trigonella foenum-graecum Linn. Key word: Evaluation, Ethno pharmacological Activity, methi seed.