羟丙基-β-环糊精对阿克他利的包合作用研究  

Study on inclusion complex of actarit with hydroxypropyl-β-cyclodextrin

作　　者：戴玉杰[1] 张雯雯[1] 朱凌云[1] 

机构地区：[1]天津科技大学生物工程学院,天津300457

出　　处：《中国新药杂志》2008年第19期1695-1699,共5页Chinese Journal of New Drugs

摘　　要：目的:考察羟丙基-β-环糊精(HP-β-CD)对阿克他利的包合作用。方法:采用旋光度法确定包合比;搅拌法制备包合物;红外光谱法和X-射线衍射法对包合物进行鉴定;相溶解度法研究包合物的增溶作用及包合过程中热力学参数的变化。结果:最佳包合比为1∶1,包合过程中的吉布斯自由能变化(ΔG0)、焓变(ΔH0)和熵变(ΔS0)均为负值;形成包合物后,阿克他利的溶解度和溶出速率均有显著增加。结论:HP-β-CD能明显增加阿克他利的溶解度,包合反应是一个自发的放热过程。Objective：To study the inclusion effects of hydroxypropyl-β-cyclodextrin （HP-β-CD） on actarit. Methods：The inclusion ratio of HP-β-CD was determined by measuring the optical activity. The inclusion complex was prepared by the stirring method and characterized by Fourier transform infrared spectroscopy（FTIR） and X-ray diffraetion（XRD）. The phase solubility method was used to study the solubilization effects of HP-β-CD on actarit and thermodynamic profiles in the complexation. Results：The optimal inclusion ratio was 1： 1. All ther- modynamic parameters of AGo ΔG^0,ΔH^0 and ΔS^0 in the complexation were negative values. The solubility and dissolution were both improved when actarit was entrapmented with HP-β-CD. Conclusion：The solubility of actarit is increased markedly by HP-β-CD. The complex reaction is a spontaneous and exothermic process.

关 键 词：阿克他利 羟丙基-Β-环糊精 包合物 旋光度法 相溶解度法 

分 类 号：R913[医药卫生—药学] R971.1