Formulation and Evaluation of Sustained Release Matrix Tablets of Isoxsuprine Hydrochloride by Direct Compression Method

摘要

A sustained-release tablet formulation should ideally have a proper release profile insensitive to moderate changes in tablet hardness that is usually encountered in manufacturing. Isoxsuprine hydrochloride is structurally a novel vasodilator. The short biological half-life (5±2 hr) and the fast clearance make the drug, a suitable candidate for the development of modified release formulation. A novel oral controlled delivery system for isoxsuprine hydrochloride was developed and optimized. Matrix tablets of isoxsuprine hydrochloride were prepared by using hydroxypropylmethylcellulose (HPMC K15), Gaur Gum and PVP K 30 as polymer substance to achieve required sustained release profile. The matrix tablets were prepared by direct compression method which is now days considered a cost effective and simple method of manufacturing. It is considered as an appropriate method for hygroscopic and thermolabile substances. Six formulations of different polymer percentages were formulated (F1-F6). Pre-compression parameters were evaluated. The influence of matrix forming agents and binary mixtures of them on isoxsuprine hydrochloride release was investigated. The formulated tablets were characterized by hardness, friability, thickness, weight variation and in vitro drug release. The formulated tablets had acceptable physicochemical characters. There was no chemical interaction found between the drug and excipients throughout FT-IR and UV study thought of in the present investigation. The quantity of isoxsuprine hydrochloride present in the tablets and the release medium were estimated by a simple, rapid and validated UV method. The dissolution results show that increased amount of polymer resulted in reduced and extended drug release. F4 formulation is the optimum formulation due to its better targeting profile in terms of release. First order kinetic profiles were achieved. This formulation may provide an alternative for oral controlled delivery of isoxsuprine hydrochloride and be helpful in the future treatment of peripheral vascular disease.