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《Chinese Journal of Experimental Traditional Medical Formulae》 2015-11
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Intestinal Absorption Investigation of Scutellarin Ethyl Ester by in situ Single Pass Intestinal Perfusion Model

XU Xue-lin;YI Hong;ZHAO Jie;XIE Xiao-ke;WANG Zhi-min;ZHANG Qi-wei;LIU Xiao-qian;GAO Hui-min;Shaanxi University of Chinese Medicine;National Engineering Laboratory for Quality Control Technology of Chinese Herbal Medicines,Institute of Chinese Materia Medica,China Academy of Chinese Medical Sciences;Tianjin University of Traditional Chinese Medicine;Jiangsu Kanion Pharmaceutical Co. Ltd.;  
Objective: To investigate absorption mechanism of scutellarin ethyl ester( DZY-02).Method: In situ single pass intestinal perfusion model was established,HPLC was adopted to study absorptions of three dose groups of DZY-02 in different segments,effects of different protein inhibitors on absorption parameters of DZY-02 in different intestinal segments were investigated. Result: Absorption rate constant and effective permeability coefficient( Peff) were no significantly differences in different segments of rat intestine or concentration of DZY-02, Peffwas more than 0. 2 × 10-4cm·s-1. Protein inhibitors had no obvious effects on intestinal absorption of DZY-02. Conclusion: DZY-02 is a high-permeability candidate drug and can be absorbed in whole intestinal segments,transport mechanism of DZY-02 in vivo is similar to passive diffusion. DZY-02 may be not a substrate of P-glycoprotein and breast cancer resistance protein.
【Fund】: 国家“重大新药创制”科技重大专项(2012ZX09103201-009 2012ZX09103201-027);; 中国中医科学院客座研究员联合创新研究项目(ZZ070837)
【CateGory Index】: R285.5
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