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EN
Abstract A novel floating controlled release drug delivery system of Sitagliptin phosphate was formulated in an effort to increase the gastric retention time of the dosage form and thereby increased drug bioavailability. The tablets were prepared by wet granulation method using Psyllium Husk and tragacanth gum as a release retarding polymers and sodium bicarbonate as a gas generating agent. All the designed nine batches of floating tablets were evaluated for physical characteristics viz. weight variation, thickness, content uniformity, hardness, floating capacity, swelling studies. All formulations had floating lag time of less than 1 min and constantly floated for 12 h except F1, F4 and F7 (that dissolved completely in 8 h or less than 8 h). In vitro drug release studies were carried out for 8 h and release mechanism was further evaluated by linear regression analysis, F9 composed of 30% Psyllium Husk, 10% tragacanth gum and 18% sodium bicarbonate sustained the drug release for longer period. The formulations followed first order kinetics, Higuchi drug release kinetics with diffusion as the dominant mechanism of drug release and the release exponent ranged (0.452-0.635) indicating that the drug release from all formulations was by non-Fickian diffusion mechanism. The prepared floating tablets of STP (F9) might be a promising drug delivery system with sustained release action and improved bioavailability.
EN
The liver as a vital body organ is adversely affected by hazardous chemicals and drugs. Paracetamol widely used as analgesic and antipyretic drug produces severe hepatotoxicity at high doses. Present study was designed to investigate the hepatoprotective activity of Polygonum perfoliatum L. used on folklore basis. Aqueous methanolic extract of the plant was prepared. Preliminary phytochemical and HPLC analyses were carried out to identify and quantify chemical constituents respectively. For hepatoprotective activity, Wistar rats were divided into six groups as normal control, standard (silymarin) control, negative control and extract treated groups i.e., 125, 250 and 500 mg/kg/day per oral. Paracetamol was administered orally, following seven days of previously stated therapy. Biochemical parameters of hepatotoxicity such as serum glutamic pyruvate transaminase (SGPT), serum glutamic oxaloacetate transaminase (SGOT), alkaline phosphatase (ALP) and total bilirubin were measured in all groups. Histopathological evaluation of liver was also carried out. Benzoic acid, chlorogenic acid, gallic acid, m-coumaric acid, quercetin and vitamin E were detected in the plant extract through HPLC. The hepatoprotective effect of 500 mg/kg/day therapy was more pronounced than 125 and 250 mg/kg dose. However, the effect of plant extract was less pronounced than standard silymarin therapy. It can be concluded that the plant extract possessed significant hepatoprotective activity that may be attributed to quercetin, benzoic acid, gallic acid and vitamin E present in it.
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