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单次静脉注射和口服给药后氯喹在健康尼日利亚人中的处置情况。

The disposition of chloroquine in healthy Nigerians after single intravenous and oral doses.

作者信息

Walker O, Salako L A, Alván G, Ericsson O, Sjöqvist F

出版信息

Br J Clin Pharmacol. 1987 Mar;23(3):295-301. doi: 10.1111/j.1365-2125.1987.tb03048.x.

Abstract

The pharmacokinetics of chloroquine after single oral (600 mg) and intravenous (2 mg kg-1) doses were studied in healthy black Nigerian students. The plasma concentrations of chloroquine and its desethylmetabolite were determined using a high performance liquid chromatography technique. Concentrations as low as 3 ng ml-1 were reproducibly determined. After i.v. dosage, the half-life ranged between 144 and 298 h; the total plasma clearance was between 282 and 1130 ml min-1 and the volume of distribution between 142 and 398 1 kg-1. Renal clearance was about 52% of plasma clearance. The estimated total urinary recovery of chloroquine and desethylchloroquine was 77% of the oral dose. There was no significant difference in the pharmacokinetics between the oral and the i.v. administration. The pharmacokinetic properties of chloroquine, in these black subjects did not differ from those previously demonstrated in Caucasians.

摘要

在健康的尼日利亚黑人学生中研究了单次口服(600毫克)和静脉注射(2毫克/千克)剂量氯喹后的药代动力学。采用高效液相色谱技术测定血浆中氯喹及其去乙基代谢物的浓度。可重复性地测定低至3纳克/毫升的浓度。静脉给药后,半衰期在144至298小时之间;总血浆清除率在282至1130毫升/分钟之间,分布容积在142至398升/千克之间。肾清除率约为血浆清除率的52%。氯喹和去乙基氯喹的总尿回收率估计为口服剂量的77%。口服和静脉给药的药代动力学无显著差异。在这些黑人受试者中,氯喹的药代动力学特性与先前在白种人中所显示的并无不同。

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Kinetics of the distribution and elimination of chloroquine in the rat.
Gen Pharmacol. 1982;13(5):433-7. doi: 10.1016/0306-3623(82)90110-0.
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Cardiovascular toxicity and distribution kinetics of intravenous chloroquine.
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