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本文评述了近几年对戊脉安(Ⅰ)、硫氮(艹卓)酮(Ⅱ)及硝苯吡啶(Ⅲ)药物动力学的研究结果。摄入[~(14)C]-消旋(Ⅰ)80mg(80μCi)的4人尿液合并测定表明,48小时与5天各排出总放射性的55～60%与67～71%;其中原药占3～4%;N-脱烃基与N-脱甲基或去甲戊脉安(Ⅳ)占6%:C-N-C 键断裂与氮原子上短侧链脱落的代谢产物占22%。长期口服(Ⅰ)后,(Ⅳ)的血浆浓度近于(Ⅰ)。(Ⅰ)口服后90%被吸收,但经受显著的首过
This article reviews the results of studies on the pharmacokinetics of verapamil (Ⅰ), thiadiazole (Ⅱ) and nifedipine (Ⅲ) in recent years. The combination of [~ (14) C] - rac (80 mg) and 80 mg (80μCi) in urine showed that 55-60% and 67-71% of the total radioactivity were excreted at 48 hours and 5 days respectively. Drugs accounted for 3 to 4%; N-dealkylation with N-demethylation or desmethylation (Ⅳ) accounted for 6%: CNC bond cleavage and short-chain nitrogen atoms on the off side of the metabolites accounted for 22%. Long-term oral (Ⅰ), (Ⅳ) plasma concentration close (Ⅰ). (I) is absorbed 90% after oral administration, but undergoes a significant first pass