盐酸沙格雷酯不对称膜胶囊的制备及体外释药试验  

Investigation on the Preparation of Asymmetric membrane capsules of sarpogrelate hydro-chloride and it's drug releasing in vitro

作　　者：张伟[1] 傅红兴[2] 李慧[2] 蔡娟娟[1] 朱益如[2] 贾雪超[2] 

机构地区：[1]宁波大学医学院附属医院药剂科,浙江宁波315000 [2]温州医学院药学院,浙江温州325035

出　　处：《温州医学院学报》2012年第6期553-555,560,共4页Journal of Wenzhou Medical College

基　　金：温州市科技局科研基金资助项目(Y20080220);平阳县科技局科研基金资助项目(AS201003);浙江省大学生科技创新活动计划项目

摘　　要：目的:制备盐沙格雷酯不对称膜胶囊剂并研究其体外释药规律。方法:以盐酸沙格雷酯为药物模型,醋酸纤维素为囊膜材料,加入致孔剂F68,PEG-400为增塑剂,丙酮:乙醇=4:1为溶媒,采用蘸胶工艺制备囊壳。通过实验选择不同的致孔剂比例,研究其药物释放规律。结果:以60%、80%、100%F68为致孔剂制备的胶囊,药物在24 h时有90%以上从不对称膜胶囊中释放;致孔剂F68比例为40%时,药物释放符合零级方程,致孔剂比例为100%时,药物释放符合Higuchi方程。结论:药物盐酸沙格雷酯在致孔剂含量低的不对称膜胶囊中呈缓释释药,在致孔剂含量高的不对称膜胶囊中呈控释释药。Objective： To prepare asymmetric membrane capsules of sarpogrelate hydro-chloride and investigate it＇ s release behavior in vitro. Methods： With sarpogrelate hydro-chloride as a model drug and cellulose CA as capsule materials, the shell of osmotic pump capsule were prepared by dip plastic method and mechanical drill treatment, adding pore-foaming agent, PEG-400 as plasticizer, acetone：ethanol=4：1 as solvent. By selecting a series of different porogen and release solution to study the rules of drug release. Results： More than 90% of the loaded drug was released in 24 hours in the capsules with 60%, 80% and 100% P68 as pore agents. The drug release behavior in 40% formula could be best described by zero-order kinetic equation, while in 100% formula could be best described by Higuchi kinetic equation. Conclusion： In low content of hole agents in this asymmetric membrane capsules, the drug is in sustained-release, while in the high content of hole agents, the drug release is in controlled-release.

关 键 词：盐酸沙格雷酯 不对称膜胶囊 缓控释 制备 

分 类 号：R944[医药卫生—药剂学]