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本文研究了２０名健康志愿者口服单剂量和多剂量普萘洛尔（ＰＰＬ）后原形物及其活性代谢物４－羟普萘洛尔（４－ＯＨ－Ｐ）的药代和药效动力学。结果显示单剂量给药时４－ＯＨ－Ｐ的血药浓度较高，Ｃ（ｍ）＿（ｍａｘ）２６．１±１３．２ｎｇ／ｍｌ，ＡＵＣ（ｍ）１８０±６９ｎｇ·ｈ／ｍｌ，分别为ＰＰＬ的０．５０和０．７３倍；Ｔ＿（１／２）Ｋ（ｍ）１０．２±５．７ｈ，为ＰＰＬ的２．４倍。ＰＰＬ产生负性频率作用的药效半衰期显著长于血浆浓度半衰期（８．７８±２．２７ｖｓ４．２３±１．３３ｈ，Ｐ＜０．０５）。表明４－ＯＨ－Ｐ在ＰＰＬ的β阻滞效应中起重要作用。本文同时建立的ＰＰＬ及４－ＯＨ－Ｐ药代一药效学统一模型将有助于指导临床合理用药和药效学定量研究。
In this paper, the pharmacokinetics and pharmacodynamics of protoplasts and 4-hydroxypropanalol (4-OH-P) in 20 healthy volunteers after oral administration of propranolol (PPL) learn. The results showed that the plasma concentrations of 4-OH-P in single-dose group were higher than those in control group (26.1 ± 13.2ng / ml and 180 ± 69ng · h / ml, respectively) 0.50 and 0.73 times of PPL; T_ (1/2) K (m) 10.2 ± 5.7h, which is 2.4 times PPL. The half-life of PPL with negative frequency was significantly longer than that of plasma (8.78 ± 2.27 vs 4.23 ± 1.33 h, P <0.05). This indicates that 4-OH-P plays an important role in the beta blockade of PPL. The PPL and 4-OH-P pharmacopoeial unified model established at the same time will help to guide clinical rational use of drug and pharmacodynamics quantitative research.