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口服活性炭对兔静脉注射普萘洛尔后药代动力学的影响。

Effect of oral activated charcoal on propranolol pharmacokinetics following intravenous administration to rabbits.

作者信息

al-Meshal M A, el-Sayed Y M, al-Angary A A, al-Dardiri M M

机构信息

Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

出版信息

J Clin Pharm Ther. 1993 Feb;18(1):39-44. doi: 10.1111/j.1365-2710.1993.tb00564.x.

Abstract

The pharmacokinetics of propranolol following intravenous administration (1 mg/kg), with and without treatment with oral activated charcoal, was investigated in rabbits. In charcoal-treated rabbits a significant reduction in propranolol serum concentrations was observed compared to control animals. Charcoal treatment significantly reduced the half-life of elimination (16.6%) and the mean residence time (19%) of propranolol. A 17% increase in the systemic clearance and a 14% decrease in AUC were also noted. Charcoal administration did not significantly alter the volume of distribution (Vc' V(area) and Vss) or the apparent distribution half-life. A two-compartment model adequately described propranolol in control and treated rabbits. The results indicate that administration of oral activated charcoal enhances the systemic elimination of propranolol. This is presumably mediated by interruption of the enterohepatic circulation of propranolol by activated charcoal.

摘要

在兔子身上研究了静脉注射普萘洛尔(1毫克/千克)后,无论是否口服活性炭治疗的药代动力学情况。与对照动物相比,经活性炭治疗的兔子体内普萘洛尔血清浓度显著降低。活性炭治疗显著缩短了普萘洛尔的消除半衰期(16.6%)和平均驻留时间(19%)。还观察到全身清除率增加了17%,曲线下面积减少了14%。给予活性炭并未显著改变分布容积(Vc、V(area)和Vss)或表观分布半衰期。二室模型能充分描述对照和治疗兔子体内的普萘洛尔情况。结果表明,口服活性炭可增强普萘洛尔的全身消除。这可能是由于活性炭阻断了普萘洛尔的肝肠循环所致。

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