Rostock G, Faulhaber H D, Gohlke H R, Prehm C
Pharmazie. 1986 Apr;41(4):258-60.
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.
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。