溶解度法研究纤维素类聚合物抑制超饱和吲哚美辛结晶的规律  

Research on the Rules of Crystallization Inhibition of Cellulose Polymers Against Supersaturated Drugs by Solubility Test

作　　者：时念秋[1,2] 张勇[2] 冯波[1] 张秀荣[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,长春130012 [3]北京大学药学院,北京100191

出　　处：《中国药学杂志》2016年第13期1137-1142,共6页Chinese Pharmaceutical Journal

基　　金：吉林省科技发展计划资助项目(20160520046JH);吉林市科技局科技计划项目(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：目的研究纤维素类聚合物抑制超饱和状态下药物结晶的规律。方法通过制备超饱和状态下的无定型药物,并利用测定溶解度的方法,来分析纤维素聚合物类型、加入量、离子强度和黏度对于生物药剂学分类系统(BCS)Ⅱ类模型药物吲哚美辛的结晶抑制影响。结果羟丙甲基纤维素-E15(HPMC E15)具有最强的结晶抑制效应,纤维素聚合物加入量增多、纤维素聚合物黏度的减少和离子强度的增大会导致聚合物抑制药物结晶能力的增强。结论本实验可有助阐明纤维素类聚合物抑制超饱和状态下药物结晶的规律,对纤维素聚合物抑制药物结晶的实际应用提供科学指导。OBJECTIVE To explore the characteristics of crystallization inhibition by cellulose polymers against supersaturated drugs. METHODS The biopharmaceutics classification system （BCS） Ⅱ class drug indometacin was selected as the model drug. Supersaturated amorphous drug solid was prepared and the solubility of indometacin was measured. The types, added amounts, i- onic intensity and viscosity of cellulose polymers were employed as influential factors to assess the crystallization inhibition effect of pol- ymers against indometaein. RESULTS HPMC E15 displayed the strongest crystallization inhibition effect. The crystallization inhibi- tion was enhanced by adding larger amount of polymers, decreasing the viscosity of polymers and increasing the ionic intensity. CON- CLUSION The study is helpful to clarify the profiles that cellulose polymers inhibit the crystallization of drugs in supersaturated states. This research may provide scientific guide for the practical application of cellulose polymers for drug crystallization.

关 键 词：纤维素类聚合物 溶解度 超饱和状态 结晶抑制 

分 类 号：R944[医药卫生—药剂学]