Hobbs D C, Twomey T M, Palmer R F
J Clin Pharmacol. 1978 Aug-Sep;18(8-9):402-6. doi: 10.1002/j.1552-4604.1978.tb02456.x.
Prazosin was administered orally to 24 normotensive human subjects in the form of capsules or as a solution. Plasma concentrations indicate that drug is almost completely bioavailable from the capsules, although levels peak more slowly than from drug in solution. Drug leaves plasma with a half-life of approximately 2.3 hours. Examination of data from each subject on repeated dosing indicates considerable intrasubject consistency in pharmacokinetic response despite intersubject variability. The absence of the pharmacologically active metabolites in plasma suggests that the hypotensive response derives from drug only. Prazosin is bound to human plasma proteins to the extent of 97%.
将哌唑嗪以胶囊形式或溶液形式口服给予24名血压正常的人体受试者。血浆浓度表明,药物从胶囊中几乎完全生物可利用,尽管其血药浓度峰值出现的速度比溶液中的药物慢。药物从血浆中消除的半衰期约为2.3小时。对每位受试者多次给药的数据检查表明,尽管受试者之间存在变异性,但药代动力学反应在受试者内部具有相当大的一致性。血浆中不存在药理活性代谢物,这表明降压反应仅源于药物本身。哌唑嗪与人体血浆蛋白的结合率为97%。