论文部分内容阅读
地尔硫(diltiazem,以下简写为Dil)是一种钙通道阻滞剂,被广泛用于治疗各种心绞痛、高血压和窦性心动过速。Dil可经脱乙酰作用、N-脱甲基作用、O-脱甲基作用和结合作用等广泛代谢。有人报告,口服Dil后,血浆中主要代谢物为脱乙酰基Dil(M_1),最近也有人报告N-脱甲基Dil(MA)可能是血浆中占优势的代谢物。作者用HPLC法研究长期用Dil治疗的病人血样中Dil及其代谢物的稳定性,发现病人血中50％母体药转化为MA,只有12％转化为M_(1)。当全血在采样和离心之间于室温放
Diltiazem (hereinafter abbreviated as Dil) is a calcium channel blocker that is widely used to treat various angina pectoris, hypertension and sinus tachycardia. Dil can be extensively metabolized by deacetylation, N-demethylation, O-demethylation and binding. It has also been reported that the major metabolite in plasma after oral administration of Dil is deacetyl Dil (M_1). Recently, it has also been reported that N-demethyl Dil (MA) may be the predominant metabolite in plasma. The authors used HPLC to study the stability of Dil and its metabolites in patients treated with Dil for a long time and found that only 50% of the mother’s drug in the blood was converted to MA and only 12% was converted to M_ (1). Whole blood is released at room temperature between sampling and centrifugation