Journal of Pharmaceutical Research

81-89

Authors: Tiewlasubon Uriah, Mrityunjaya B. Patil, Sivaiah Kumar

Purpose: To evaluate the in vitro antioxidant and hepatoprotective activity of Nepenthes khasiana leaf extracts against ethanol-induced hepatotoxicity. Approach: In vitro antioxidant activity was measured spectrophotometrically for the methanolic and aqueous leaf extracts of N. khasiana using different assays i.e DPPH, superoxide anion and hydroxyl radical scavenging activity. For hepatoprotective effect, the rats of either sex were administered with 30% w/v ethanol at a dose of 5 g/kg b.w. orally for three weeks. Methanolic extract of N. khasiana leaf was administered to the experimental rats at 100 mg, 200 mg and 400 mg/kg, p.o. for three weeks. The hepatic markers such as alanine aminotransferase (ALT), aspartate amino transferase (AST), alkaline phosphatase (ALP), total bilirubin and total proteins were evaluated and supported by histopathological studies of the liver. Findings: The methanolic leaf extract of N. khasiana exhibited strong antioxidant capacity with IC values 50 of 23.33±0.441, 62.75±0.713 and 38.38±0.425 μg/mL respectively and this extract was selected for hepatoprotective studies. The results showed that administration of methanolic leaf extract of N.khasiana reversed the liver damage due to alcohol as evident from histopathological studies of the liver. The HPTLC fingerprinting analysis of the methanolic leaf extract of N. khasiana at different wavelengths revealed presence of many compounds which may provide basic information regarding the isolation, purification, characterization and identification of marker chemical compounds of the plant species. Originality: The present study is the first time evaluation of the hepatoprotective effect of the methanolic leaf extract of N. khasiana on ethanol-induced liver injury in rat models. The isolation and characterisation of the active principle require extensive research in the future. Conclusion: From our study, the methanolic leaf extract of N. khasiana shows potent hepatoprotective effects, hence it can be used as a natural protecting agent against liver damage.

94-97

Authors: A. Ankit, Mohammed Gulzar Ahmed, C. H. Vinay, A. Sanjana

Purpose: Gastric retentive drug delivery devices can be used for controlled drug delivery systems containing drugs, which are degraded in the colon. The main objective of the present study is to design and formulate gastric retentive controlled release dosage form of bisoprolol fumarate in order to improve the gastric residence time, which in turn increases its bioavailability. Approach: Floating dosage form of bisoprolol fumarate was prepared by direct compression method using different concentration and grades of hydroxypropyl methylcellulose and sodium bicarbonate. Prepared powder mixtures and tablets were subjected to various pre-compression and post-compression evaluations respectively. Findings: Powder mixture showed good flow properties for uniform die filling. The SEM analysis showed minimum number of pores and erosion on the surface of the tablet. The optimized formulation F8 gave floating lag time less than 3 min with a floating time of 12 h, and an in vitro release profile very near to the desired release. The prepared dosage form reported to follow the zero order release and non-Fickian mechanism. Best formulations were subjected to accelerated stability studies. The assay results showed that the drug was stable for 3 months without any change in the drug content. Conclusion: Finally it can be concluded that the gastric retentive time of bisoprolol can be increased by formulating it in a floating dosage form.