Spahn-Langguth H, Benet L Z
Department of Pharmacology, Johann-Wolfgang-Goethe University, Frankfurt a/M., Germany.
Pharmacology. 1993 May;46(5):268-73. doi: 10.1159/000139054.
Because of the labile nature of acyl glucuronides under physiologic conditions, metabolic rates of formation calculated using traditional methods may be confounded by concomitant rates of degradation. True metabolic formation rates may be approximated by stabilization of the metabolic product or by purifying the metabolite and calculating its degradation rate under similar conditions to that utilized in the formation experiments. This latter degradation rate is used to correct the apparent formation parameter in the absence of inhibitors. The advantages and limitations of each approach are reviewed employing studies to characterize rates of acyl glucuronidation for nonsteroidal antiinflammatory drugs.
由于酰基葡萄糖醛酸在生理条件下的不稳定性，使用传统方法计算的形成代谢率可能会受到同时发生的降解率的干扰。真正的代谢形成率可以通过稳定代谢产物或通过纯化代谢物并在与形成实验中使用的条件相似的条件下计算其降解率来近似。在没有抑制剂的情况下，后一种降解率用于校正表观形成参数。通过研究非甾体抗炎药的酰基葡萄糖醛酸化率来综述每种方法的优缺点。
