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The Disposition of Oxymatrine in the Vascularly Perfused Rat Intestine-Liver Preparation and Its Metabolism in Rat Liver Microsomes  Li Hua Huang, Yun Ming.

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Presentation on theme: "The Disposition of Oxymatrine in the Vascularly Perfused Rat Intestine-Liver Preparation and Its Metabolism in Rat Liver Microsomes  Li Hua Huang, Yun Ming."— Presentation transcript:

1 The Disposition of Oxymatrine in the Vascularly Perfused Rat Intestine-Liver Preparation and Its Metabolism in Rat Liver Microsomes  Li Hua Huang, Yun Ming Zhong, Xiao Hong Xiong, Mei Feng Cen, Xuan Ge Cheng, Gui Xiang Wang, Ji Sheng Chen, Su Jun Wang  Journal of Pharmaceutical Sciences  Volume 105, Issue 2, Pages (February 2016) DOI: /j.xphs Copyright © 2016 American Pharmacists Association® Terms and Conditions

2 Figure 1 Chemical structures of OMT (PubChem CID: ), MT (PubChem CID: ), and sophocarpine (IS, PubChem CID: ). Journal of Pharmaceutical Sciences  , DOI: ( /j.xphs ) Copyright © 2016 American Pharmacists Association® Terms and Conditions

3 Figure 2 Schematic representation of (a) the in situ perfused rat intestine-liver preparation, and (b) the recirculated intestine preparation. Journal of Pharmaceutical Sciences  , DOI: ( /j.xphs ) Copyright © 2016 American Pharmacists Association® Terms and Conditions

4 Figure 3 In the once-through perfused intestinal-liver preparation, perfusate concentration-time of OMT and MT in portal vein and hepatic vein, respectively. No MT was detected in portal plasma (mean ± SD, n = 6). Journal of Pharmaceutical Sciences  , DOI: ( /j.xphs ) Copyright © 2016 American Pharmacists Association® Terms and Conditions

5 Figure 4 Accumulation concentration of OMT and MT during its recirculated intestine perfusion after the intraduodenal administration of OMT (5 mg) during 120 min (mean ± SD, n = 6). Journal of Pharmaceutical Sciences  , DOI: ( /j.xphs ) Copyright © 2016 American Pharmacists Association® Terms and Conditions

6 Figure 5 Effect of P450 inhibitors on liver microsomal OMT metabolism. P450 isoform-selective inhibitors were used at different concentration with microsomes from rat livers. Control experiments were incubated without chemical inhibitors. These chemical inhibitors were: α-naphthoflavone (CYP1A2), quinidine (CYP2D1), diethyldithiocarbamate (CYP2E1), and ketoconazole (CYP3A2). Each column represents mean percent control of formation rates of MT and error bars are standard deviation of the mean (n = 3). Journal of Pharmaceutical Sciences  , DOI: ( /j.xphs ) Copyright © 2016 American Pharmacists Association® Terms and Conditions

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