辛酸癸酸聚乙二醇甘油酯在口服制剂中的应用及促吸机理  

Application of Caprylocaproyl Polyoxylglycerides in Oral Dosage Forms and Mechanism of Promoting Absorption

作　　者：杨怡静 王雨青 刘杰 YANG Yijing;WANG Yuqing;LIU Jie(Gattefosse China Trading CO.,LTD,Shanghai,201203,China)

机构地区：[1]嘉法狮(上海)贸易有限公司,上海201203

出　　处：《药学与临床研究》2021年第6期449-453,共5页Pharmaceutical and Clinical Research

摘　　要：脂质处方在提高难溶性药物口服生物利用度方面有着独特的应用。现总结了近年来国内外相关文献报道,介绍一种脂质材料Labrasol(辛酸癸酸聚乙二醇甘油酯)在口服制剂中提高药物生物利用度的具体应用,并且从体外和体内两方面综述了其在提高难溶性药物生物利用度方面可能的作用机制,包括体外可提高BCSⅡ类和Ⅳ类药物的体外溶解度、减小乳滴的粒径;体内可促进药物肠黏膜的吸收,对CYP450、UGT酶和P-gp糖蛋白具有一定的抑制作用,促进药物的淋巴吸收等作用。Lipid formulation has unique applications in improving oral bioavailability of insoluble drugs.Based on some relevant domestic and foreign literatures in recent years,the application of one lipid material,Labrasol(Caprylocaproyl Polyoxylglycerides)in improving the bioavailability of drugs in oral dosage forms is summarized and introduced in this article.The possible mechanism of Labrasol in improving the bioavailability of insoluble drugs is also reviewed from both in vitro and in vivo,such as in improving the solubility of BCSⅡ/IV class drugs,reducing the particle size of emulsion drops in vitro;promoting the absorption of drugs in intestinal mucosa,inhibiting CYP450,UGT enzyme and P-gp glycoprotein,and promoting the lymphatic absorption of drugs in vivo.

关 键 词：辛酸癸酸聚乙二醇甘油酯 LABRASOL 脂质处方 自乳化 增溶 生物利用度 表面活性剂 吸收机理 

分 类 号：R969.1[医药卫生—药理学]