Box-Behnken设计-效应面法优化莲心碱羟丙基-β-环糊精包合物制备及表征  

Optimal Preparation and Characterization of Liensinine HP-β-CD Inclusion Compound by Box-Behnken Design-Response Surface Methodology

作　　者：周江[1] 吴婷婷[1] 李美云[1] 雷小小 唐婷[1] 桂卉[1] 

机构地区：[1]湖南省中药现代化研究重点实验室湖南中医药大学药学院,湖南长沙410208

出　　处：《中国中医药信息杂志》2016年第3期80-84,共5页Chinese Journal of Information on Traditional Chinese Medicine

基　　金：湖南省高校创新平台开放基金(13K078);湖南省科技计划项目(2013SK3100)

摘　　要：目的优选莲心碱羟丙基-β-环糊精(HP-β-CD)包合物的最佳制备工艺,考察莲心碱HP-β-CD包合物体外溶出性质。方法采用饱和水溶液法制备包合物,以45 min体外累积溶出度为指标,采用三因素三水平Box-Behnken设计,考察HP-β-CD与莲心碱投料比、搅拌时间、包合温度对制备工艺的影响,对结果进行多元线性和二项式拟合,效应面法筛选出最佳包合工艺,进行预测分析和验证试验,并应用显微电镜扫描法、差示量热扫描法、红外光谱、X射线衍射法对包合物进行结构表征。结果莲心碱HP-β-CD包合物的最佳制备工艺为:HP-β-CD用量为莲心碱投料量的4.5倍,搅拌时间为3.7 h,包合温度为52℃。表征鉴定结果显示莲心碱HP-β-CD包合物已形成。结论本研究优选的最佳包合工艺稳定可行,能显著提高莲心碱的溶出度,增加其生物利用度。Objective To optimize the preparation of liensinine HP-β-CD inclusion compound; To investigate its dissolution performance in vitro. Methods The inclusion compound of liensinine was prepared by using saturated water solution method; the cumulative dissolution(45 min) was used as an indicator and Box-Behnken design was adopted to evaluate the influence of feed ratio, mixing time and inclusion temperature on preparation process. Results were analyzed by multiple linear and binomial fitting; response surface methodology was used to screen the optimal inclusion process; predictive parsing and verification experiment were conducted; SEM, DSC, IR, and XRD were applied for the structural characterization of inclusion compound of liensinine. Results The optimal preparation process was: HP-β-CD was 4.5 times the amount of liensinine feeding amount; mixing time was 3.7 h; inclusion temperature was 52 ℃. HP-β-CD inclusion compound of liensinine formed. Conclusion Optimal inclusion process is stable and feasible, which can significantly improve the dissolution of liensinine and increase its bioavailability.

关 键 词：莲心碱 羟丙基-Β-环糊精 包合物 Box-Behnken设计-效应面法 累积溶出度 

分 类 号：R283.5[医药卫生—中药学]