Gohel M C, Soni C D, Nagori S A, Sarvaiya K G
Department of Pharmaceutics and Pharmaceutical Technology, L. M. College of Pharmacy, Navrangpura, Ahmedabad-380 009, India.
Indian J Pharm Sci. 2008 May-Jun;70(3):292-7. doi: 10.4103/0250-474X.42974.
The aim of present study was to prepare novel modified release press coated tablets of venlafaxine hydrochloride. Hydroxypropylmethylcellulose K4M and hydroxypropylmethylcellulose K100M were used as release modifier in core and coat, respectively. A 3(2) full factorial design was adopted in the optimization study. The drug to polymer ratio in core and coat were chosen as independent variables. The drug release in the first hour and drug release rate between 1 and 12 h were chosen as dependent variables. The tablets were characterized for dimension analysis, crushing strength, friability and in vitro drug release. A check point batch, containing 1:2.6 and 1:5.4 drug to polymer in core and coat respectively, was prepared. The tablets of check point batch were subjected to in vitro drug release in dissolution media with pH 5, 7.2 and distilled water. The kinetics of drug release was best explained by Korsmeyer and Peppas model (anomalous non-Fickian diffusion). The systematic formulation approach enabled us to develop modified release venlafaxine hydrochloride tablets.
本研究的目的是制备新型盐酸文拉法辛控释压制包衣片。羟丙基甲基纤维素K4M和羟丙基甲基纤维素K100M分别用作片芯和包衣的释放调节剂。在优化研究中采用了3（2）全因子设计。将片芯和包衣中的药物与聚合物比例选为自变量。将第1小时的药物释放和1至12小时之间的药物释放速率选为因变量。对片剂进行尺寸分析、抗压强度、脆碎度和体外药物释放特性研究。制备了一个检查点批次的片剂，其片芯和包衣中药物与聚合物的比例分别为1:2.6和1:5.4。将检查点批次的片剂在pH值为5、7.2的溶出介质和蒸馏水中进行体外药物释放研究。药物释放动力学最适合用Korsmeyer和Peppas模型（非菲克反常扩散）来解释。系统的制剂方法使我们能够开发出盐酸文拉法辛控释片。
