Wang Z, Okamoto M, Kurosaki Y, Nakayama T, Kimura T
Faculty of Pharmaceutical Sciences, Okayama University, Japan.
Biol Pharm Bull. 1996 Jun;19(6):901-4. doi: 10.1248/bpb.19.901.
The pharmacokinetic behavior of glycyrrhizin (GZ) was examined in D-galactosamine-intoxicated (GAL) rats. When GZ was administered intravenously, the apparent volume of distribution (Vdss) and the total body clearance (CLtotal) were more significantly decreased in GAL rats than those in normal rats. When GZ was administered orally, the area under the plasma concentration-time curve (AUC), the mean residence time (MRT) and the time to reach the maximum plasma concentration (Tmax) for GZ were higher, but the maximum plasma concentration (Cpmax) in GAL rats was lower than that in normal rats. The bioavailability of GZ, however, was not significantly changed. On the other hand, the AUC for glycyrrhetic acid (GA), a main metabolite of GZ, after oral administration of GZ was higher in GAL rats than in normal rats, although there was no significant difference in MRT or Tmax, Cpmax or the bioavailability for GA between GAL and normal rats. The reasons for these differences in GAL rats would be changes in the absorption rate (reduced gastric emptying rate) and reduction of the hepatic elimination rates (biliary excretion of GZ and hepatic metabolism of GA).
在D-半乳糖胺中毒（GAL）大鼠中研究了甘草酸（GZ）的药代动力学行为。静脉注射GZ时，GAL大鼠的表观分布容积（Vdss）和总体清除率（CLtotal）比正常大鼠显著降低。口服GZ时，GZ的血浆浓度-时间曲线下面积（AUC）、平均驻留时间（MRT）和达到最大血浆浓度的时间（Tmax）较高，但GAL大鼠的最大血浆浓度（Cpmax）低于正常大鼠。然而，GZ的生物利用度没有显著变化。另一方面，口服GZ后，GZ的主要代谢产物甘草次酸（GA）的AUC在GAL大鼠中高于正常大鼠，尽管GAL大鼠和正常大鼠之间GA的MRT、Tmax、Cpmax或生物利用度没有显著差异。GAL大鼠中这些差异的原因可能是吸收速率的变化（胃排空率降低）和肝脏消除率的降低（GZ的胆汁排泄和GA的肝脏代谢）。
