Combined use of phospholipid complexes and self-emulsifying microemulsions for improving the oral absorption of a BCS class IV compound, baicalin  

作　　者：Huiyi Wu Xiaoying Long Fei Yuan Li Chen Sujing Pan Yunjun Liu Yoshiko Stowell Xiaoling Li 

机构地区：[1]School of Traditional Chinese Medicine,Guangdong Pharmaceutical University,Guangzhou 510006,China [2]Department of Pharmaceutics,Thomas J Long School of Pharmacy&Health Sciences,University of the Pacific,CA 95211,USA

出　　处：《Acta Pharmaceutica Sinica B》2014年第3期217-226,共10页药学学报（英文版）

基　　金：This work was supported by grants from the National Natural Science Foundation of China(No.30973953C1909)。

摘　　要：The aim of this study was to develop a formulation to improve the oral absorption of baicalin(BA)by combining a phospholipid complex(PC)and self-emulsifying microemulsion drug delivery system(SMEDDS),termed BA–PC–SMEDDS.BA–PC was prepared by a solvent evaporation method and evaluated by complexation percentage(CP).The physicochemical properties of BA–PC were determined.The synergistic effect of PC and SMEDDS on permeation of BA was studied in vitro with Caco-2 cells and in situ with a single pass intestinal perfusion model.The improved bioavailability of BA in BA–PC–SMEDDS was confirmed in an in vivo rat model.The CP of BA–PC reached 100%when the molar ratio of drug to phospholipid(PP)was Z1:1.The solubility of BA–PC increased in both water and octanol,and the log P o/w of BA–PC was increased significantly.BA–PC–SMEDDS could be dispersed more evenly in water,compared to BA and BA–PC.Both the Caco-2 cell uptake and single-pass intestinal perfusion models illustrated that transport of BA in BA–PC was lower than that of free BA,while improved significantly in BA–PC–SMEDDS.The relative bioavailability of BA–PC(1:2)–SMEDDS was 220.37%.The combination system of PC and SMEDDS had a synergistic effect on improving the oral absorption of BA.

关 键 词：BAICALIN SMEDDS Phospholipid complex Caco-2 cell Single-pass intestinal per-fusion BIOAVAILABILITY 

分 类 号：R94[医药卫生—药剂学]