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• W2058744147 abstract "The objective of this study was to investigate the effect of tacrolimus (Tac) and xipamide (X) on mycophenolic acid (MPA) glucuronidation in precision-cut rat liver slices. To assess a possible effect of these two drugs, the influence of the anti-inflammatory drug niflumic acid (NA) - a well-known inhibitor for MPA glucuronidation in human liver microsomes - was used as a standard. MPA and its main metabolite mycophenolic acid glucuronide (MPAG) were determined by means of high-performance liquid chromatography. MPA glucuronidation rate showed a significant linear correlation (p = 0.012) with MPA concentrations from 15.61 up to 124.88 μM in the medium. That means, the enzyme(s) responsible for the glucuronidation of MPA worked far below Km-value. With all MPA concentrations tested, neither the addition of Tac (31.30 nM) nor of X (28.25 nM) influenced the glucuronidation of MPA. In comparison, NA at a concentration of 70.92 nM showed a marked inhibitory effect (by 72%). The present pilot-study indicates that precision-cut rat liver slices are a suitable in vitro model to characterize the glucuronidation of MPA to its primary metabolite MPAG and interferences with other substances." @default.
• W2058744147 created "2016-06-24" @default.
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• W2058744147 date "2003-01-01" @default.
• W2058744147 modified "2023-09-27" @default.
• W2058744147 title "Can xipamide or tacrolimus inhibit the glucuronidation of mycophenolic acid in rat liver slices?" @default.
• W2058744147 cites W1964078380 @default.
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• W2058744147 doi "https://doi.org/10.1078/0940-2993-00273" @default.
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