甘草黄酮自微乳化释药系统的制备及其质量评价  

Preparation and quality evaluation of licorice flavonoids self-microemulsifying drug delivery system

作　　者：仲粒 李小芳[1] 廖艳梅 刘罗娜 龙家英 张琳琳 ZHONG Li;LI Xiao-fang;LIAO Yan-mei;LIU Luo-na;LONG Jia-ying;ZHANG Lin-lin(Key Laboratory of Research and Utilization of Chinese Medicinal Resources in Sichuan Province,Key Laboratory Breeding Baseof Co-founded by Sichuan Province and Ministry of Science and Technology,Ministry of Education Key Laboratory ofStandardization of Chinese Herbal Medicine,College of Pharmacy,Chengdu University of Traditional Chinese Medicine,Chengdu611137,China)

机构地区：[1]成都中医药大学药学院中药材标准化教育部重点实验室四川省中药资源系统研究与开发利用重点实验室——省部共建国家重点实验室培育基地

出　　处：《中草药》2019年第13期3044-3051,共8页Chinese Traditional and Herbal Drugs

基　　金：成都市科技局科技惠民项目(2016-HM01-00299-SF);四川省中医药管理局科研项目(2018YY001)

摘　　要：目的研究甘草黄酮自微乳的处方与制备工艺,并对其质量进行评价。方法通过溶解度实验、油相与乳化剂配伍实验及伪三元相图的绘制,筛选甘草黄酮自微乳的处方组成;以平均粒径、自乳化时间、载药量为评价指标,采用单纯形网格法优化处方,并对甘草黄酮自微乳的理化性质、体外溶出度及稳定性进行评价。结果甘草黄酮自微乳处方中油相为肉桂油(10%)、乳化剂为RH-40(55%)、助乳化剂为1,2-丙二醇(35%)。所得自微乳外观均一透明,自乳化后平均粒径(16.30±0.22)nm,多分散指数0.155±0.008,Zeta电位(-20.11±0.50)m V,载药量(86.03±0.37)mg/g。溶出度实验表明,甘草黄酮30min累积溶出率达90.65%。稳定性实验表明,高温与光照影响甘草黄酮自微乳的稳定性,应低温避光保存。结论甘草黄酮自微乳制备工艺简单,质量稳定,能显著增加药物的溶解度,从而提高甘草黄酮的口服生物利用度,为该有效部位相关制剂的进一步研究与开发提供参考。Objective To study the prescription and preparation technology of licorice flavonoids self-microemulsifying drug delivery system (LF-SMEDDS) and evaluate its quality. Methods The optimal formulation of LF-SMEDDS was screened by test of solubility, compatibility of oil and emulsifier, and pseudo-ternary phase diagram. Simplex lattice method was applied to optimize formulation with average particle size, polydispersity index and drug loading as evaluation indexes, the physicochemical characteristics, in vitro dissolution and stability were also determined. Results The optimal prescription composition of LF-SMEDDS was 10% of Cinnamomi Cortex oil, 55% of RH-40, and 35% of 1,2-propanediol. The LF-SMEDDS exhibited uniform and transparent appearance, with the average particle size of (16.30 ± 0.22) nm, polydispersity index of 0.155 ± 0.008, Zeta pontential of (?20.11 ± 0.50) mV and drug loading of (86.03 ± 0.37) mg/g. The results of in vitro dissolution test indicated that the accumulative dissolution of LF was 90.65% at 30 min. The stability experiment showed that LF-SMEDDS was affected by high temperature and illumination, indicating that it should be stored at low temperature and protected from light. Conclusion The LF-SMEDDS is simple in preparation and stable in quality, significantly increasing the solubility of LF and improving its oral bioavailability, which can provide reference for further research and development about the related preparations of the active fraction.

关 键 词：甘草黄酮 自微乳 单纯形网格法 体外溶出度 稳定性 

分 类 号：R283.6[医药卫生—中药学]