单纯形网格法优选马甲子总三萜自微乳处方  

Optimization Design of Total Triterpenes of Paliurus ramosissimus Self-emulsion Prescription by Simplex Lattice Method

作　　者：陈旺 帅丽霞 袁袁 谭镭[2] 詹雁[2] 阮佳[2] 徐超群[2] CHEN Wang;SHUAI Lixia;YUAN Yuan;TAN Lei;ZHAN Yan;RUAN Jia;XU Chaoqun(College of Pharmacy,Chengdu University of Traditional Chinese Medicine,Chengdu 611137 Sichuan,China;Sichuan Academy of Chinese Medicine Science,Chengdu 610041 Sichuan,China)

机构地区：[1]成都中医药大学药学院,四川成都611137 [2]四川省中医药科学院,四川成都610041

出　　处：《中药新药与临床药理》2022年第6期836-841,共6页Traditional Chinese Drug Research and Clinical Pharmacology

基　　金：国家重大新药创制项目(2018ZX09731013)。

摘　　要：目的采用单纯形网格法优化马甲子总三萜自微乳处方,并对其进行质量评价。方法通过溶解度考察、配伍实验及伪三元相图优化处方;以油相、乳化剂及助乳化剂比例为考察因素,以平均粒径、多分散系数以及载药量为评价指标,采用单纯形网格法优化马甲子总三萜自微乳的处方,并对自微乳的理化性质、体外溶出度进行评价。结果马甲子总三萜自微乳处方中油相为油酸乙酯(10%)、乳化剂为聚山梨酯-80(Tween-80,45%)、助乳化剂为二乙二醇单乙基醚(Transcutol P,45%)。所得自微乳外观棕黄均一透明,自微乳平均粒径(46.3±0.34)nm,多分散系数(0.198±0.012),Zeta电位(-8.1±0.13)mV,载药量(13.1±0.28)mg·g^(-1)。溶出度实验表明,马甲子总三萜自微乳20 min累积溶出率达80%。结论马甲子总三萜自微乳制备工艺简单,可显著改善马甲子素总三萜的水溶性和溶出度,有望提高其口服生物利用度。Objective To optimize the formulation of self-microemulsion containing total triterpenes from Paliurus ramosissimus by simplex lattice method and evaluate its quality.Methods Based on solubility experiment,compatibility test,and ternary phase diagram,taking proportion of oil phase,emulsifier and co-emulsifier as factors,the simplex lattice method was used to optimize formulation with average particle size,polydispersity index and drug loading as evaluation indexes.The physicochemical properties and in vitro dissolution were also determined.Results The optimal prescription composition was using the 10%ethyl oleate as oil phase,45%Tween-80 as emulsifier,and 45%Transcutol P as co-emulsifier.The resulted self-microemulsion exhibited brown yellow,uniform and transparent appearance,with an average particle size of(46.3±0.34)nm,a polydispersity index of(0.198±0.012),a Zeta potential o f(-8.1±0.13)mV,and a drug loading capacity of(13.1±0.28)mg·g^(-1).The solubility experiments showed that the accumulative dissolution was 80%in 20 min.Conclusion The preparation process of total triterpenes self-microemulsion is simple,it can significantly improve the solubility and dissolution of total triterpenes,which is expected to improve its oral bioavailability.

关 键 词：马甲子总三萜 马甲子素 自微乳 单纯形网格法 

分 类 号：R283.6[医药卫生—中药学]