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[两种普萘洛尔制剂在稳态原发性高血压患者中的相对生物利用度比较药代动力学研究]

[Comparative pharmacokinetic studies on the relative biologic availability of two propranolol preparations in patients with steady state essential hypertension].

作者信息

Rostock G, Faulhaber H D, Gohlke H R, Prehm C

出版信息

Pharmazie. 1986 Apr;41(4):258-60.

PMID:3725870
Abstract

Plasma propranolol concentrations were analyzed after Obsidan (VEB Isis-Chemie, Zwickau, GDR) (= preparation A) and another propranolol-preparation (= preparation B) in 10 patients with arterial hypertension of clinical stage I-II in a cross-over design. The concentration-time-curves (AUC0----infinity) were investigated up to 24 h after the oral intake of 40 mg of both preparations of propranolol and were nearly identical. In comparison with preparation B the relative bioavailability F was 104% for preparation A. The steady-state plasma concentrations of propranolol were within the therapeutic range of 50-100 ng/ml. They showed only interindividual variations about the factor 2-3. Peak plasma concentrations were observed 1,5-2 h after the oral application. There were no statistical differences in the pharmacokinetic parameters between the both preparations. The rate of elimination constants of 0,065 to 0,073 h-1 after preparation A and B explain the long duration of the therapeutic efficacy during chronic treatment.

摘要

采用交叉设计,对10例临床I-II期动脉高血压患者服用Obsidan(民主德国茨维考VEB伊西斯化学公司生产)(=制剂A)和另一种普萘洛尔制剂(=制剂B)后的血浆普萘洛尔浓度进行了分析。口服40mg两种普萘洛尔制剂后,研究其浓度-时间曲线(AUC0----无穷大)至24小时,结果几乎相同。与制剂B相比,制剂A的相对生物利用度F为104%。普萘洛尔的稳态血浆浓度在50-100ng/ml的治疗范围内。它们仅表现出个体间约2-3倍的差异。口服给药后1.5-2小时观察到血浆峰值浓度。两种制剂的药代动力学参数无统计学差异。制剂A和B给药后消除常数率为0.065至0.073h-1,这解释了慢性治疗期间治疗效果的持续时间较长。

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