Patel Sanjay S, Ray S, Thakur R S
Department of Pharmaceutics, Krupanidhi College of Pharmacy, #5 Sarjapur road, Koramangala, Bangalore-560034, India.
Acta Pol Pharm. 2006 Jan-Feb;63(1):53-61.
Floating matrix tablets are designed to prolong the gastric residence time after oral administration, at a particular site and controlling the release of drug especially useful for achieving controlled plasma level as well as improving bioavailability. With this objective, floating dosage form containing clarithromycin as drug was designed for the treatment of Helicobacter pylori. Tablets containing hydroxypropylmethylcellulose (HPMC), drug and different additives were compressed using wet granulation and D-optimal design technique. The study shows that tablet composition and mechanical strength have great influence on the floating properties and drug release. Incorporation of gas-generating agent together with polymer improved drug release, besides optimal floating (floating lag time < 30 s; total floating time > 10 h). The drug release was sufficiently sustained (more than 8 h) and anomalous diffusion as well as zero-order was confirmed. Optimization of the evaluating parameters with 'design expert' software was employed to get final optimized formulation. The optimized formulation was obtained using 62.5% clarithromycin, 4.95% HPMC K15M, 18.09% HPMC K4M, 12.96% sodium bicarbonate which gave floating lag time < 30 s with a total floating time > 10 h, in vitro release profile very near to the target in vitro release profile and follows anomalous diffusion as well as zero order pattern of release.
漂浮型骨架片旨在延长口服给药后在特定部位的胃滞留时间，并控制药物释放，这对于实现血浆药物浓度的控制以及提高生物利用度特别有用。出于这一目的，设计了含克拉霉素的漂浮剂型用于治疗幽门螺杆菌。采用湿法制粒和D-最优设计技术压制含有羟丙基甲基纤维素（HPMC）、药物和不同添加剂的片剂。研究表明，片剂组成和机械强度对漂浮性能和药物释放有很大影响。除了实现最佳漂浮效果（漂浮滞后时间<30秒；总漂浮时间>10小时）外，加入产气剂与聚合物一起可改善药物释放。药物释放得到充分维持（超过8小时），并证实存在非菲克扩散以及零级释放。使用“设计专家”软件对评估参数进行优化，以获得最终的优化配方。优化后的配方使用62.5%的克拉霉素、4.95%的HPMC K15M、18.09%的HPMC K4M、12.96%的碳酸氢钠，其漂浮滞后时间<30秒，总漂浮时间>10小时，体外释放曲线非常接近目标体外释放曲线，且遵循非菲克扩散以及零级释放模式。
