摘要
目的:研究HP-β-CD(hydroxypropyl-β-cycloextrin)与紫杉醇在水溶液中的包合作用方法:采用等摩尔系列法和相溶解度法等测定HP-β-CD与紫杉醇在水溶液中的包合比及包合过程中的热力学参数变化。结果:HP-β-CD与紫杉醇在水中可形成1:2以上摩尔比的包合物。紫杉醇与HP-β-CD的相溶解度曲线呈现典型的AP型,AH大于0,升高温度有利于包合反应的进行,且附加剂的加入有助于提高紫杉醇的溶解度。结论:HP-β-CD可增加药物紫杉醇的溶解度,选择合适的投料比、适当的温度和恰-当的水溶性辅料(HPMC)对包合物的制备是至关重要的。
Objective： To-investigate the complexes of HP-β-CD and paclitaxel in aqueous solutions. Method： The inclusion process and the changes in thermodynamic parameters of HP-β-CD paclitaxel complexes were studied by the methods of equimolar se- ries and lbhase solubility. Result ： Above 1 ： 2 molar ratio, inclusion complexes of paclitaxel and HP-β-CD could be formed in aqueous solution. The phase solubility diagram exhibited AP type, and the enthalpy change （ AH° ） was found to be above zero, suggeg that raising temperature could enhance the formation of the complexes. Additives could increase the solubility of paclitaxel. Conclusion： HP- β-CD can increase the solubility of paclitaxel with appropriate inclusion molar ratio, temperature and additives.
出处
《中国药师》
CAS
2012年第1期3-6,共4页
China Pharmacist
基金
中国博士后科学基金项目(编号:20060390978)
