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

查看全文 作　　者：Huiyi [1]Wu;Xiaoying [1]Long;Fei [1]Yuan;Li [1]Chen;Sujing [1]Pan;Yunjun [1]Liu;Yoshiko [2]Stowell;Xiaoling [2]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》索引2014年第4卷第3期,共10页

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

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

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