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基于渗透压释药原理的混合骨架控释片研究 被引量:2

Preparation of Hybrid-Matrix Controlled-Release Tablets Based on Osmotic Pressure Principle
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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。 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.
机构地区 中国药科大学
出处 《中国药业》 CAS 2017年第19期9-13,共5页 China Pharmaceuticals
基金 中国药科大学药学基地科研训练及科研能力提高项目(国家基础科学人才培养基金)[J1310032] 2016中国药科大学大学生创新创业训练计划项目[201610316209]
关键词 混合骨架控释片 酒石酸美托洛尔 星点设计-响应面优化法 体外释放 渗透压原理 hybrid-matrix controlled-release tablets metoprolol tartrate central composite design-response surface methodology release in vitro osmotic pressure principle
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