Gunjal P T, Shinde M B, Gharge V S, Pimple S V, Gurjar M K, Shah M N
Formulation and Development Department, Zuventus Healthcare Ltd, T-184 MIDC Bhosari, Pune-411 026, India.
Emcure Pharmaceutical Ltd, Emcure House, Pune-411 026, India.
Indian J Pharm Sci. 2015 Sep-Oct;77(5):563-72. doi: 10.4103/0250-474x.169036.
The objective of this present investigation was to develop and formulate floating sustained release matrix tablets of s (-) atenolol, by using different polymer combinations and filler, to optimize by using surface response methodology for different drug release variables and to evaluate the drug release pattern of the optimized product. Floating sustained release matrix tablets of various combinations were prepared with cellulose-based polymers: Hydroxypropyl methylcellulose, sodium bicarbonate as a gas generating agent, polyvinyl pyrrolidone as a binder and lactose monohydrate as filler. The 3(2) full factorial design was employed to investigate the effect of formulation variables on different properties of tablets applicable to floating lag time, buoyancy time, % drug release in 1 and 6 h (D1 h,D6 h) and time required to 90% drug release (t90%). Significance of result was analyzed using analysis of non variance and P < 0.05 was considered statistically significant. S (-) atenolol floating sustained release matrix tablets followed the Higuchi drug release kinetics that indicates the release of drug follows anomalous (non-Fickian) diffusion mechanism. The developed floating sustained release matrix tablet of improved efficacy can perform therapeutically better than a conventional tablet.
本研究的目的是通过使用不同的聚合物组合和填充剂,开发并制备s(-)阿替洛尔的漂浮型缓释骨架片,采用表面响应方法对不同的药物释放变量进行优化,并评估优化产品的药物释放模式。用纤维素基聚合物制备了各种组合的漂浮型缓释骨架片:羟丙基甲基纤维素、作为产气剂的碳酸氢钠、作为粘合剂的聚乙烯吡咯烷酮和作为填充剂的一水乳糖。采用3(2)全因子设计来研究处方变量对片剂不同性质的影响,这些性质适用于漂浮滞后时间、漂浮时间、1小时和6小时的药物释放百分比(D1h、D6h)以及药物释放90%所需的时间(t90%)。使用方差分析对结果的显著性进行分析,P<0.05被认为具有统计学显著性。s(-)阿替洛尔漂浮型缓释骨架片遵循 Higuchi 药物释放动力学,表明药物释放遵循非菲克扩散机制。所开发的具有更高疗效的漂浮型缓释骨架片在治疗上比传统片剂表现更好。