中文摘要：

目的 探讨以羟丙甲纤维素（HPMC）/乙基纤维素（EC）为混合骨架,制备基于渗透压释药原理的水溶性药物酒石酸美托洛尔（MT）控释片的可行性.方法 以HPMC/EC为混合骨架,用粉末直接压片法制备;在单因素考察基础上,以控释片在1 h和12 h累积释放度、1~12 h内释药曲线线性拟合度R2为评价指标,用星点设计-响应面优化处方工艺,探究其体外释药行为和机理.结果 骨架材料用量、HPMC/EC比例、乳糖用量均对药物释放度有明显影响;其最优处方为骨架材料用量为74.66%,HPMC/EC比例为1：2,乳糖用量为5.40%;制得的骨架控释片在12 h内释药恒定,其释药行为包含渗透压原理.结论 所制成的混合骨架控释片可用于控制MT的释放,制备工艺简单,体外释药平稳,具有一定的应用前景.

英文摘要：

Objective To investigate the feasibility of using hydroxypropyl methylcellulose （ HPMC ） / ethyl cellulose （ EC ） as the matrix skeleton materials to prepare water-soluble drug-metoprolol tartrate （ MT ） controlled-release tablets. Methods The and HPMC/EC was used as the hybrid-matrix, the MT hybrid-matrix controlled-release tablets were prepared by the direct power compression method. According to the results of the single factor evaluation, the central composite design-response surface methodology was used to optimize the formulation. The accumulative release at 1, 12 h and the correlation coefficient R2 from 1 h to 12 h were chosen as the dependant variables and the release behavior in vitro and drug release mechanism were investigated. Results The amount of hybrid-matrix material, the ratio of HPMC/EC and the amount of lactose had significant effects on the release of the drug. The optimum formulation containing 74. 66% hybrid-matrix material , 1/2 HPMC/EC and 5. 40% lactose exhibited a zero-order release and drugs were released steadily from the matrix within 12 h. The drug release was controlled by osmotic pressure. Conclusion Hybrid-matrix controlled-release tablets can be used to control the release of MT, the preparation process is simple and stable for the drug release in vitro, which has a certain application prospect.