Posted by admin on Mar 31, 2016 in |
Metformin HCl (MH), is an oral anti-diabetic drug with less bioavailability, and a BCS class III, short plasma half-life as well as narrow absorption window. The objective of this research work is to obtain better delivery of MH to the upper part of GIT by increasing the mean residence time (MRT) in the stomach. For this, Gastroretentive swellable and floating sustained release tablets were prepared to prolong the gastric emptying that provides maximum drug at the site of absorption. Different formulations were prepared by wet granulation with the help of hydrophilic polymers like different grades of hyroxypropyl methyl cellulose (HPMC), xanthan gum (XG), sodium alginate (SA), carbopol 940; hydrophobic polymer like ethyl cellulose (EC); swelling agent like crospovidone (CP) and gas generating agent sodium bicarbonate (SBC). The formulations were evaluated for pre and post-compression characteristics; the formulation F5 gave the optimum result along with >24 hrs floating time and an in vitro release profile very near to desire release. Release kinetic studies showed that all batches followed Super case...
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Posted by admin on Mar 31, 2016 in |
Objective: Following World Health Organization tropical disease research mandate, there is definitive need for search of new lead molecules for development of drug against human lymphatic filariasis. Thiazolidineone derivatives has shown versatile therapeutic potential. The present study has been undertaken to explore the possible antifilarial effect of such synthetic compounds against filarial parasite, Brugia malayi. Methods: A series of 12 thiazolidineone derivatives, following synthesis and characterization, were screened for antifilarial potential in vitro against microfilarial stage of Brugia malayi; those showed significant effect were tested against adult parasites also. The pharmacological response in terms of loss of parasitic motility was assessed under microscope. Further dose dependent response and potential lethality onto host cells for such effective drugs were carried out. Result: Out of the tested compounds, four such compounds showed significant activity and those were tested against the adult worms; one of these compounds showed marked effect. The corresponding IC50 and LD50 values were deduced for each of these four effective compounds. Most of them showed a good therapeutic...
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Posted by admin on Mar 31, 2016 in |
Four crude extracts viz, methanol extract of fruit and n-hexane, dichloromethane, methanol extracts of the leaf of R. tetraphylla were investigated for in vitro antioxidant activity at different concentrations (5, 50 and 100 μg). Antioxidant ability is expressed as equivalents of ascorbic acid and was calculated using standard graph. The results indicated that the leaf n-hexane and methanol extracts was found to be significantly active at 5μg when compared with BHA, and at 50 μg concentration the methanol leaf extract found be very high. The fruit methanol extract was found to be active and the activity increased with increase in dose, but not as that of BHA. The experimental results show that the activity exhibited by the solvent extracts is dose...
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Posted by admin on Mar 31, 2016 in |
The present study relates to the stable fixed dose combination comprising of Aceclofenac as a glycolic acid ester of Diclofenac is having analgesic and anti-inflammatory action and Thiocolchicoside, as a glycosulfurated analogue of colchicine which is well known centrally acting muscle relaxant in unit dosage form and to the preparation method thereof. Aceclofenac is very susceptible to decomposition under hydrolytic, oxidative stress and exposure to light. The major degradation product identified was diclofenac, which was detected as an impurity in the formulation. Many of the marketed formulation of Aceclofenac tablets having problem of high content of diclofenac impurity. Diclofenac having more gastrointestinal adverse effects such as gastritis, gastrointestinal haemorrhage, haemorrhagic diarrhoea, gastrointestinal ulcer than that of Aceclofenac. It was challenge to develop Aceclofenac tablet formulation having diclofenac impurity within compendial limit. The compatibilty of Aceclofenac with various tableting excipients was investigated physically and by means of Differential Scanning Calorimetry (DSC). Aceclofenac alone and with other excipients in 1:1 binary mixtures were investigated before and after accelerated storage. An interaction...
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Posted by admin on Mar 31, 2016 in |
Coleus forskohlii is an Indian medicinal plant it treat various diseases of cardiovascular, respiratory, gastrointestinal, and central nervous systems. The purpose of this study was to investigate the anticancer activity of an ethanol extract of Coleus forskohlii against gastric cancer in AGS cancer cell lines. Gastric carcinoma cells were tested in vitro for cytotoxicity, Ao/EtBr staining for apoptotic cells, apoptotic DNA fragmentation in response to Coleus forskohlii extract. The protein expression of Bax, Bcl2 and Caspase-3 were analyzed through Western blotting. Treatment with Coleus forskohlii extract inhibited AGS cell proliferation dose and time dependently. Cells exposed to Coleus forskohlii extract showed typical hallmarks of apoptotic cell death. In conclusion, Coleus forskohlii ethanol extract has cytotoxic and apoptotic effects on Gastric carcinoma cells. Its mechanism of action might be associated with the apoptosis induction through up-regulation of the protein expressions of caspase-3 down-regulation of the protein expression of Bax and...
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