辣椒碱-β-环糊精包合物的研制及包合常数的测定

中国药物警戒 ›› 2015, Vol. 12 ›› Issue (3): 147-149.

辣椒碱-β-环糊精包合物的研制及包合常数的测定

李宏树¹，²,张岭²,陈莉²,张莉²*

1中国人民武装警察部队河北总队医院药剂科，河北石家庄050050;
2中国人民武装警察部队后勤学院救援医学系药剂学教研室，天津 300162

收稿日期:2014-12-18 出版日期:2015-03-08 发布日期:2015-07-28
通讯作者: 张莉，女，教授?硕导，药物制剂研究与开发。
作者简介:李宏树，男，药师，临床药学。

Preparation of Capsaicin-β-cyclodextrin Inclusion Complex and Predicting Inclusion Constants

LI Hong-shu¹,²,ZHANG Ling²,CHEN Li²,ZHANG Li²*

1Department of Pharmacy, Hebei Municipal Corps Hospital,Hebei Shijiazhuang 050050, China;
2Department of Pharmaceutic, Logistic University of Chinese People's Armed Police Forces, Tianjin 300039, China

Received:2014-12-18 Online:2015-03-08 Published:2015-07-28

摘要/Abstract

摘要： 目的制备辣椒碱-β-环糊精包合物，考察其溶解度。方法采用共沉淀法制备包合物，用正交设计优化包合物形成的最佳条件，采用相溶解度法测定包合物的表观溶解度和包合稳定常数。结果通过正交试验筛选的最优条件为包合时间6 h，搅拌强度70 rpm，包合温度70℃，辣椒碱与β-环糊精质量比为1:21，溶液pH值为11。在25、37、45℃条件下包合物中辣椒碱的溶解度极大值分别为0.32、0.60、1.08 mg·mL-1。结论辣椒碱与β-环糊精能形成稳定的包合物，制成包合物后辣椒碱的溶解度增加。

关键词: 辣椒碱, β-环糊精, 包合物, 包合常数

Abstract: Objective To prepare capsaicin-β-cyclodextrin inclusion complex (CAP-β-CD) and inspect their solubilities. Methods CAP-β-CD was prepared by the coprecipitation method and optimum formation conditions for preparation was selected by orthogonal design. The measurements of the apparent solubility and equilibrium constant were carried out by phase solubility diagram. Results The optimal conditions for forming CAP-β-CD complexes were 21:1 of capsaicin to cylcodextrin molar ratio, 70℃of temperature, 70 rpm of stirring strength, and 6 h of reaction duration at pH 11. The solubilities of capsaicin in inclusion complexes were the biggest at 25, 37, 45 ℃, which were 0.32, 0.60, 1.08 mg·mL-1, respectively. Conclusion By forming stable inclusion complex with β-CD, the solubility of capsaicin was increased.

Key words: capsaicin, β-cyclodextrin, inclusion complex, inclusion constants

中图分类号:

R943

李宏树,张岭,陈莉,张莉. 辣椒碱-β-环糊精包合物的研制及包合常数的测定[J]. 中国药物警戒, 2015, 12(3): 147-149.

LI Hong-shu,ZHANG Ling,CHEN Li,ZHANG Li. Preparation of Capsaicin-β-cyclodextrin Inclusion Complex and Predicting Inclusion Constants[J]. Chinese Journal of Pharmacovigilance, 2015, 12(3): 147-149.