摘要
目的:基于磷脂复合物(PC)研究黄芩提取物(BA)自微乳给药系统(SMEDDS)的处方设计及制备工艺,并进行体外质量评价。方法:以BA-PC为中间体,通过溶解度实验、绘制伪三元相图和星点设计-效应面法确定BA-PC-SMEDDS的最佳处方;优化制备工艺并对其理化性质、稳定性、体外释放度进行评价。结果:BA-PC-SMEDDS最优处方为油酸乙酯为油相,吐温-80为乳化剂,二乙二醇单乙醚为助乳化剂;油相质量分数14.39%,Km值2.71,为简化处方,将处方修定为油相质量分数14.5%,混合乳化剂Km2.7;平均粒径为(16.83±0.04)nm,多分散系数(PDI)为(0.127±0.002),Zeta电位为(-12.02±0.03)mV,载药量为(16.75±0.09)mg/g;BA-PC-SMEDDS在pH为1.2、5.0、7.4的缓冲盐溶液中具有良好的体外释放效果。结论:BA-PC-SMEDDS粒径小,载药量高,外观良好,性质稳定,提高了难溶性成分黄芩苷的溶解度及体外释放度,具有增加口服生物利用度的潜力。
Objective:To study the formulation and preparation of self-microemulsion drug delivery system(SMEDDS)of extract of Huangqin(Scutellariae Radix)(BA)based on phospholipid complex(PC),and evaluate its quality in vitro.Methods:The optimal formu⁃lation of BA-PC-SMEDDS was determined by solu⁃bility test,pseudo-ternary phase diagram and central composite design-response surface methodology by taking the BA-PC as the intermediate,optimized the preparation process and evaluated its physico⁃chemical properties,stability,and in vitro release.Results:The ethyl oleate was selected as the oil phase in the optimal formulation of BA-PC-SMEDDS,tween-80 as the emulsifier,and the diethylene glycol monoethyl ether as the co-emulsifier.The mass fraction of the oil phase was 14.39%,the Km value of the mixed emulsifier was 2.71.To simplify the prescription,the mass fraction of the oil phase was revised to 14.5%and the Km value of the mixed emulsifier was 2.7;The average particle size was(16.83±0.04)nm,Polydispersion index(PDI)was(0.127±0.002),Zeta potential was(-12.02±0.03)mV,drug loading was(16.75±0.09)mg/g.BA-PC-SMEDDS had good in vitro release effect in buffer salt solution of pH 1.2,5.0 and 7.4.Conclusions:BA-PC-SMEDDS has the advantages of small particle size,high drug loading,good appearance and stable properties.It can improve the solubility and in vitro release of Baicalin,which has great potential to increase oral bioavailability.
作者
孙文秀
宋基正
李梦琦
石玉
胡豫
李凌军
SUN Wenxiu;SONG Jizheng;LI Mengqi;SHI Yu;HU Yu;LI Lingjun(Shandong University of Traditional Chinese Medicine,Jinan 250355,China)
出处
《山东中医药大学学报》
2025年第1期96-105,共10页
Journal of Shandong University of Traditional Chinese Medicine
基金
国家中医药管理局高水平中医药重点学科项目(编号:zyyzdxk-2023119)。
关键词
黄芩提取物
磷脂复合物
自微乳给药系统
平衡溶解度
伪三元相图
星点设计-效应面法
体外释放
extract of Huangqin(Scutellariae Radix)
phospholipid complex
self-microemulsion drug delivery system
equilibrium solubility
pseudo-ternary phase diagram
central composite design-response surface methodology
in vitro release
作者简介
孙文秀,2021年级硕士研究生,研究方向:中药制剂方向;通信作者:李凌军,教授,博士研究生导师,主要从事中药新制剂、新剂型研究及药物体内过程研究。邮箱:sdzyylilingjun@163.com。
