中国药房2012，Vol.23Issue(45)：4275-4277,3.DOI:10.6039/j.issn.1001-0408.2012.45.19
西罗莫司-羟丙基-β-环糊精包合物的制备
Preparation of Sirolimus-hydroxypropyl-β-cyclodextrin Inclusion
鲁一 1谢文忠 1王莹 1凌春生 2章莹1
作者信息
- 1. 开封市第一人民医院&河南大学附属人民医院药剂科,河南开封475000
- 2. 河南大学药学院,河南开封475004
- 折叠
摘要
Abstract
OBJECTIVE: To prepare Sirolimus-hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion, and to investigate the improvement effect of HP-β-CD inclusion on the dissolution of sirolimus. METHODS: The preparation technology of Sirolimus-HP-β-CD inclusion was optimized by orthogonal test with ratio of sirolimus to HP-β-CD (mol: mol), inclusion temperature and inclusion time as factors using inclusion rate and yield rate as index. The validation test was conducted among dissolution and X-ray diffraction method structure. RESULTS: The optimal preparation technology was as follows: ratio of sirolimus to HP-β-CD of 1 :6 (mol: mol), inclusion temperature of 25 ℃ , inclusion time of 6 h. Average inclusion rate of 3 batches of inclusion was 25.4% (RSD=1.16%) and average yield was 86.5% (RSD=0.83%). With the increase of HP-β-CD concentration, the dissolution of sirolimus increased from 1.18 μg·mL-1 to 49.97 μg·mL-1. The crystal diffraction profiles of inclusion were in line with those of HP-β-CD. CONCLUSION: The inclusion process of sirolimus with HP-β-CD is simple and easy to operate, and can improve the dissolution of sirolimus.关键词
西罗莫司/羟丙基-β-环糊精/包合物/正交试验/溶解度Key words
Sirolimus/ Hydroxypropyl-β-cyclodextrin/ Inclusion/ Orthogonal design/ Dissolution分类
医药卫生引用本文复制引用
鲁一,谢文忠,王莹,凌春生,章莹..西罗莫司-羟丙基-β-环糊精包合物的制备[J].中国药房,2012,23(45):4275-4277,3.
