Department of Pharmaceutics, Rajiv Academy for Pharmacy, Mathura, Uttar Pradesh, India.
AAPS PharmSciTech. 2012 Mar;13(1):174-83. doi: 10.1208/s12249-011-9738-3. Epub 2011 Dec 20.
The aim of the present study was to develop asymmetric membrane (AM) tablets for controlled delivery of highly water-soluble antihistaminic drug triprolidine hydrochloride. The solubility of triprolidine hydrochloride was modulated through the incorporation of coated sodium chloride crystals encapsulated with asymmetric membrane coating polymer, cellulose acetate butyrate. Formulation of AM tablets was based on a 2(3) factorial design to study the effect of formulation variables, namely, polymer concentration, level of pore former, and amount of osmogen on the in vitro release. Core tablets prepared by wet granulation and coated with asymmetric membrane by a dip coating method were evaluated. Statistical analysis was done with the Design Expert Software 8.0.2 (USA), and the polynomial equation generated by Pareto charts was used for validation of the experimental design. The interaction chart and response surface plots deduced the simultaneous effect of independent variables on in vitro drug release. The in vitro drug release was inversely proportional and directly related to the level(s) of polymer and pore former in the membrane, respectively. The level of osmogen not only increased the osmotic pressure but also controlled the drug release due to a common ion effect. The drug release of the optimized formulation (F6) followed zero-order kinetics, which would be capable of reducing the administration, and was stable over 3 months. SEM photographs revealed asymmetry in membrane structure.
本研究旨在开发不对称膜（AM）片剂，用于控制高水溶性抗组胺药盐酸曲普利啶的释放。通过将包裹有不对称膜包衣聚合物醋酸丁酸纤维素的包衣氯化钠晶体掺入，调节盐酸曲普利啶的溶解度。AM 片剂的配方基于 2(3) 因子设计，以研究配方变量（即聚合物浓度、致孔剂水平和渗透压调节剂的用量）对体外释放的影响。通过湿法制粒制备芯片，并通过浸涂法用不对称膜包衣。使用 Design Expert Software 8.0.2（美国）进行统计分析，并使用 Pareto 图生成的多项式方程对实验设计进行验证。交互图和响应曲面图推导出独立变量对体外药物释放的协同影响。体外药物释放与膜中的聚合物和致孔剂水平呈反比和直接相关。渗透压调节剂的水平不仅增加了渗透压，而且由于同离子效应，还控制了药物释放。优化配方（F6）的药物释放遵循零级动力学，这将能够减少给药次数，并且在 3 个月内保持稳定。SEM 照片显示了膜结构的不对称性。
