盐酸小檗碱乳剂的处方研究  

Emulsion formulation optimization of berberine hydrochloride

作　　者：刘泽伟 刘黎瑶 王庆奎[2] 刘林 叶懿娴 LIU Ze-wei;LIU Li-yao;WANG Qing-kui;LIU Lin;YE Yi-xian(Tianjin Agricultural University,College of Basic Science,Tianjin 300384,China;Tianjin Agricultural University,Tianjin Key Lab of Aquatic Ecology and Aquaculture,Tianjin 300384,China)

机构地区：[1]天津农学院基础科学学院,天津300384 [2]天津农学院天津市水产生态及养殖重点实验室,天津300384

出　　处：《天津农学院学报》2020年第3期70-73,78,共5页Journal of Tianjin Agricultural University

基　　金：大学生创新创业计划训练项目(201810061236);天津市教委科研计划项目(2017KJ181);天津市水产产业技术体系创新团队项目(ITTFRS2017004);国家自然科学基金面上项目(31170442)。

摘　　要：小檗碱是中草药黄连的主要抗菌活性成分,常以盐酸盐的形式应用,但由于水溶性和脂溶性较差,广泛应用受到限制。因此,本研究在前期利用磷脂复合技术改善盐酸小檗碱脂溶性的基础上,将其制备成乳剂以提高稳定性和水中分散性。首先,将离心稳定性作为评价指标,通过单因素筛选,确定了乳剂处方中油相比例、乳化剂以及稳定剂用量的适宜范围。然后,以离心乳层保留率为评价指标,通过正交设计,确定了盐酸小檗碱乳剂的最优处方,即:油相(大豆油)、乳化剂(Poloxmer188)以及稳定剂(黄原胶)的质量比例分别为20%、3%以及1%。优选处方下盐酸小檗碱乳剂的分散性良好,为小檗碱的广泛应用奠定了物质基础。Berberine is the main antibacterial component of Coptis chinensis,which is often used in the form of hydrochloride clinically.Its application in solution environment is limited by its poor water solubility and lipophilicity.Thus,on the basis of improving water solubility of berberine hydrochloride by phospholipid complex technology in the early stage,berberine hydrochloride emulsion was prepared to improve its stability and water dispersivity.Firstly,centrifugal stability was taken as the evaluation index,and the suitable range of the oil phase proportion,emulsifier and stabilizer ratio in emulsion prescription was determined through single factor screening.Then,the optimum formulation of berberine hydrochloride emulsion was determined by orthogonal design with the retention rate of centrifugal emulsion as the evaluation index.In the optimum formulation,the mass ratio of oil phase(soybean oil),emulsifier(Poloxmer188)and stabilizer(xanthan gum)were 20%,3%and 1%,respectively.Under the optimum formulation,berberine hydrochloride emulsion can be prepared with favorable water dispersivity.This study provides the basis for further application of berberine hydrochloride.

关 键 词：盐酸小檗碱 单因素筛选 正交设计 乳剂 磷脂复合物 

分 类 号：P641.131[天文地球—地质矿产勘探] S152.72[天文地球—地质学]