纤维素类聚合物抑制超饱和状态下药物结晶的规律特征  

Rules and characteristics of crystallization inhibition of cellulose polymers against drugs in supersaturated states

作　　者：时念秋[1,2] 张勇[2] 张秀荣[1] 冯波[1] 李正强[2] 齐宪荣[3] 

机构地区：[1]吉林医药学院,吉林吉林132013 [2]吉林大学生命科学学院分子酶学工程教育部重点实验室,吉林长春130012 [3]北京大学药学院,北京100191

出　　处：《药学学报》2016年第3期462-468,共7页Acta Pharmaceutica Sinica

基　　金：吉林省教育厅资助项目(吉教科合字2015第401号);吉林市杰出青年科技人才项目(201464053);中国博士后科学基金面上项目(2015M571374);吉林省科技发展计划项目(20140311110YY)

摘　　要：本文旨在研究纤维素类聚合物抑制超饱和状态下药物结晶的规律特征。主要利用模拟液态超饱和过程和制备超饱和药物固体,利用溶出仪测定不同时间点药物含量的方法,分析纤维素聚合物类型、加入量、离子强度和黏度对BCS II类模型药物吲哚美辛的结晶抑制影响。结果表明,HPMC E15具有最强的结晶抑制效应,聚合物加入量越多,抑制吲哚美辛结晶能力越强。聚合物黏度的减少和离子强度的增大会导致聚合物抑制吲哚美辛结晶能力的增强。本研究可对纤维素类聚合物抑制超饱和状态下药物结晶提供科学指导。This study aims to explore the characteristics of crystallization inhibition by cellulose polymers at the supersaturated states of drugs. The study was performed by simulating supersaturated process and preparing supersaturated drug solid, and was carried out by measuring the content of drugs at different time points using dissolution apparatus. The types, amounts, ionic intensity and viscosity of cellulose polymers were examined to assess the crystallization inhibition effect on BCS II class drug indomethacin. HPMC E15 exhibited the strongest crystallization inhibition effect. The more added, more obvious crystallization suppression was observed against indomethacin. The decrease in viscosity and increase in ionic intensity led to an enhanced inhibition. The research provides a scientific guide for the crystallization inhibition of supersaturated drug by cellulose polymers.

关 键 词：纤维素类聚合物 超饱和状态 无定型 结晶抑制 

分 类 号：R943[医药卫生—药剂学]