盐酸小檗碱纳米乳口服给药系统的制备及体外评价  

Preparation and in vitro evaluation of berberine hydrochloride nanoemulsion oral drug delivery systems

作　　者：戴玮莉 金婴 王婷[2] 唐晓萌 顾清 DAI Weili;JIN Ying;WANG Ting;TANG Xiaomeng;GU Qing(Department of Pharmacy,Zhabei Central Hospital of Shanghai Jingan District,Shanghai 200070,China;School of Pharmacy,Shandong University of Traditional Chinese Medicine,Jinan 250355,China;Department of Pharmacy,Changhai Hospital,Naval Military Medical University,Shanghai 200433,China)

机构地区：[1]上海市静安区闸北中心医院药剂科,上海200070 [2]山东中医药大学药学院,山东济南250355 [3]海军军医大学第一附属医院药剂科,上海200433

出　　处：《药学实践杂志》2022年第1期28-33,43,共7页Journal of Pharmaceutical Practice

基　　金：上海市科委生物医药科技支撑项目(18401931500)。

摘　　要：目的制备盐酸小檗碱纳米乳,优选其处方组成和制备工艺,并对其外观、粒径及体外释放行为等进行评价。方法采用水滴加法制备盐酸小檗碱纳米乳,绘制纳米乳伪三元相图。选择星点设计-效应面法对纳米乳处方进行优化,确定最优处方组成比例。对制备的盐酸小檗碱纳米乳的粒径、电位、外观形态、体外释药行为等进行表征。结果确定了盐酸小檗碱纳米乳的最优处方为油相Capryol 90占体系的32.84%,表面活性剂吐温-80占体系的33.90%,助表面活性剂1,2-丙二醇占体系16.95%,水相占体系15.25%,制备的纳米乳呈澄清透明、形状规则、大小均一的球状,平均粒径为(68.85±8)nm,多分散系数为(0.245±0.03),载药量为0.83 mg/g。纳米乳的体外释药行为考察,表明其具有一定的缓释效果,其体外释药行为符合一级释放动力学方程。结论本研究制备的盐酸小檗碱纳米乳可为该药的临床用药提供新的给药剂型。Objective To prepare berberine hydrochloride nanoemulsion,optimize its formulation composition and preparation process,and investigate its in vitro characteristics.Methods BBR-NE was prepared by water drop addition and pseudo-ternary phase diagram was drawn.The formulation of NE was optimized by central composite design-response surface methodology to choose the optimal formulation composition.The particle size,potential and appearance of the prepared BBR-NE were characterized.Results The optimal prescription of BBR-NE was determined as the oil phase Capryol 90 accounted for 32.84%of the system,the surfactant Tween-80 accounted for 33.90%,the co-surfactant 1,2-propylene glycol accounted for 16.95%,and water relative system accounted for 15.25%.The prepared NE was clear and transparent in appearance,regular in shape and uniform in size,with an average particle diameter of(68.85±8)nm,polydiseperse index of(0.245±0.03)and drug loading of 0.83 mg/g.The in vitro drug release results of NE showed that the in vitro drug release behavior was passive diffusion,which had a certain slow releasing effect and met the first-order release equation.Conclusion The BBR-NE can provide a new dosage form for the clinical use of berberine.

关 键 词：盐酸小檗碱 纳米乳 伪三元相图 星点设计-效应面法 体外评价 

分 类 号：R283.6[医药卫生—中药学]