DOI: 10.5176/2345-783X_PHARMA13.07
Authors: D. Nagasamy Venkatesh
Abstract:
The objective of present investigation was to prepare and evaluate the in vitro and in vivo performance of once a day abacavir sustained release matrix tablets. Abacavir, an antiviral drug used in the treatment of human deficiency virus (HIV). The half-life of this drug is 1.54 ± 0.63 hours and this necessitates its administration of twice a day. Abacavir sustained release matrix (SR) and immediate release (IR) tablets were formulated employing wet granulation method. Excipients used in the study did not alter the chemical properties of the drug as indicated by Fourier Transform Infra Red (FT-IR) and Differential Scanning Calorimetry (DSC). Tablets were evaluated for various pharmacotechnical parameters and the results were within the official limits. In vitro dissolution studies were carried out in phosphate buffer saline - PH 7.2 (PBS) using USP dissolution apparatus (XXIII- type II, paddle) with a rotational speed 50 rpm maintained at a temperature of 37±0.5° C for a period of 24 hours. The drug release from the system followed first order kinetics obeying non-fickian diffusion. An optimized sustained release matrix tablets was selected and subjected for in vivo oral bioavailability study using rabbit model. When compared to IR tablets, SR tablets of abacavir showed a 1.92 times fold increase in oral bioavailability (AUC0-t), 2.82 times fold increase in half-life (t½) and 2.78 times lower elimination rate constant (kel). This inturn may reduce dosing frequency, decreased fluctuation of drug in plasma level and provide better patient compliance in terms dose related side effects and cost.
Keywords: Abacavir, Sustained release matrix tablets, release kinetics, bioavailability studies
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