泰诺福韦酯β-环糊精包合物的制备和研究

Preparation technique and identification of tenofovir dipivoxil β-cyclodextrin inclusion complex

目的:制备泰诺福韦酯-β-CD包合物。方法:通过饱和水溶液法制备泰诺福韦酯-β-CD包合物,并对其工艺进行优化;采用紫外分光光度法考察包合物溶出度。结果:饱和水溶液法制备包合物的最佳工艺为:温度60℃、包合摩尔比为1∶1、搅拌速度1000r/min、搅拌时间6h;所得包合物载药量为(29.36±1.22)%,收率为(94.12±5.87)%;鉴别试验结果表明已形成包合物。结论:泰诺福韦酯包合物能显著增大药物的溶解度,为开拓应用范围、提高药效奠定了基础。

Objective ：To prepare and identify tenofovir dipivoxil β-cyclodextrin. Methods ：The compose route could be seen in the picture one.Tenofovir dipivoxil β-cyclodextrin was prepared by saturated water solution technique.The molar ratio of host and guest was studied in inclusion processby ultraviolet spectrophotometer. Results： The recovery of tenofovir dipivoxil β-cyelodextrin were respective （29.36±1.22）% and （94.12±5.87）% by optimizing conditions which were 60℃ ,host-guest molar ratio 1：1 and stiring rate 1 000 r/rain. Conclusion： The solubility and stability of tenofovir dipivoxil could be enhanced markedly by preparing the inclusion complex with β-cyclodextrin.