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口服活性炭对静脉注射给家兔的奎尼丁和奎宁药代动力学的影响。

Effect of oral activated charcoal on the pharmacokinetics of quinidine and quinine administered intravenously to rabbits.

作者信息

Hasan M M, Hassan M A, Rawashdeh N M

机构信息

Department of Pharmacology, Faculty of Medicine, Jordan University of Science and Technology, Irbid.

出版信息

Pharmacol Toxicol. 1990 Jul;67(1):73-6. doi: 10.1111/j.1600-0773.1990.tb00785.x.

Abstract

The pharmacokinetics of quinidine and quinine following intravenous administration (10 mg/kg) with and without concurrent treatment with oral activated charcoal was studied in the rabbit. Marked differences were observed in the pharmacokinetic parameters. Compared to quinidine, quinine was characterized by larger volume of distribution (Vd), systemic clearance (Cl) and elimination rate constant (Kel), and smaller half-life of elimination (t1/2), mean residence time (MRT) and area under the curve (AUC). Activated charcoal administered orally (15 g) significantly decreased the serum concentrations of quinidine but not quinine. Furthermore, charcoal treatment significantly enhanced the systemic elimination of quinidine as indicated by the significant increase in Cl and decrease in t1/2, MRT and AUC. By contrast, activated charcoal had no significant effect on the pharmacokinetic parameters of quinine. Differences between quinidine and quinine in respect to the effect of activated charcoal on the systemic elimination of these drugs seem at least, in part, dependent on dispositional factors. The high Cl and Vd of quinine in the rabbit are probably factors that mask the effect of charcoal on the elimination of this drug.

摘要

在兔子身上研究了静脉注射(10毫克/千克)奎尼丁和奎宁后,同时口服活性炭和不口服活性炭时它们的药代动力学。观察到药代动力学参数存在显著差异。与奎尼丁相比,奎宁的特点是分布容积(Vd)、全身清除率(Cl)和消除速率常数(Kel)更大,消除半衰期(t1/2)、平均驻留时间(MRT)和曲线下面积(AUC)更小。口服活性炭(15克)显著降低了奎尼丁的血清浓度,但对奎宁没有影响。此外,活性炭治疗显著增强了奎尼丁的全身消除,表现为Cl显著增加,t1/2、MRT和AUC降低。相比之下,活性炭对奎宁的药代动力学参数没有显著影响。活性炭对这些药物全身消除作用方面,奎尼丁和奎宁之间的差异似乎至少部分取决于处置因素。兔子体内奎宁的高Cl和Vd可能是掩盖活性炭对该药物消除作用的因素。

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