盐酸小檗碱自微乳释药系统的制备与体外评价  

Preparation and Evaluation in vitro of Self-microemulsifying Drug Delivery System of Berberine Hydrochloride

作　　者：韩冰 关延彬[1,2] 田雨冬 贾永艳[1,2] 刘改枝[1] HAN Bing;GUAN Yan-bin;TIAN Yu-dong;JIA Yong-yan;LIU Gai-zhi(School of Pharmacy,Henan University of Traditional Chinese Medicine,Zhengzhou 450040,China;Collaborative Innovation Cen-Irr for Rrspiratoiy Disease Diagnosisand Treatment & Chinese Medicine Development of Henan Province,Zhengzhou 450040,China;Department of Urology Surgery,the First Affiliated Hospital of Zhengzhou University,Zhengzhou 450052,China)

机构地区：[1]河南中医药大学药学院,河南郑州450040 [2]呼吸疾病诊疗技术与新药研发河南省协同创新中心,河南郑州450040 [3]郑州大学第一附属医院泌尿外科,河南郑州450052

出　　处：《中药材》2018年第10期2398-2402,共5页Journal of Chinese Medicinal Materials

基　　金：河南省科技攻关项目(182102310096);河南中医学院省属科研业务专项基金(2014KYYWF-QN12);河南省高等学校重点科研项目(16A350001);河南省教育厅项目(18B360002)

摘　　要：目的:研究盐酸小檗碱自微乳释药系统的制备工艺,并对其进行表征和体外释放行为考察。方法:通过溶解度试验、自乳化效率试验及伪三元相图对盐酸小檗碱自微乳进行处方筛选。以粒径和载药量为考察指标,采用星点设计-效应面优化法对盐酸小檗碱自微乳处方进行优化并验证。结果:盐酸小檗碱自微乳最优处方为中链甘油三酯(MCT)∶RH40∶聚乙二醇400的质量比为23.29%∶54.08%∶22.63%,载药量为95 mg/g,平均粒径为58 nm。盐酸小檗碱自微乳在人工肠液中,2 h内累积释放度>90%。结论:盐酸小檗碱自微乳制备工艺简单,有效改善了盐酸小檗碱的溶出速度。Objective:To study the preparation of self-microemulsion drug delivery system of berberine hydrochloride(BBR-SMEDDS)and to evaluate its characterization and release behavior in vitro.Methods:The compositions of BBR-SMEDDS were investigated by solubility assay,self-emulsifying efficiency test and pseudo-ternary phase diagram analysis.The grain diameter and drug loading were used as valuation parameters,and the prescription was optimized and validated by central composite design and response surface methodology.Results:The best prescription was medium chain triglyceride(MCT)∶RH40∶polyethylene glycol 400(23.29%∶54.08%∶22.63%)with the drug loading of 95 mg/g,the average particle size was 58 nm.The cumulative release of berberine hydrochloride was above 90% during 2 hours in artificial intestinal juice.Conclusion:The preparation technology of BBR-SMEDDS is easy and can significantly increase the dissolution of berberine hydrochloride in vitro.

关 键 词：盐酸小檗碱 自微乳释药系统 伪三元相图 星点设计 

分 类 号：R283.6[医药卫生—中药学]