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健康受试者单次静脉注射鲁贝唑(Prosynap)后的药代动力学

Pharmacokinetics of lubeluzole (Prosynap) after single intravenous doses in healthy subjects.

作者信息

Van de Velde V, Crabbe R, Van Peer A, Woestenborghs R, Van Osselaer N, Hantson L, Heykants J

机构信息

Janssen Research Foundation, Beerse, Belgium.

出版信息

Int J Clin Pharmacol Ther. 1998 Sep;36(9):490-3.

PMID:9760010
Abstract

The single-dose pharmacokinetics of lubeluzole were investigated in 2 single-blind, placebo-controlled, dose-escalation studies in healthy male subjects. In the first study, 6 subjects received an intravenous infusion of 2.5, 5, and 10 mg lubeluzole. In the second study, a 15 mg dose of lubeluzole was administered to 6 subjects, of whom 5 also received 20 mg and 2 also 25 mg lubeluzole. Following the infusion, plasma lubeluzole concentrations decayed biphasically, with a mean distribution half-life (t1/2alpha) of 30 to 65 minutes and a mean terminal half-life (t1/2beta) of 15 to 24 hours. The results of the 2 studies indicate that lubeluzole exhibits linear kinetics over the dose range tested in healthy male subjects.

摘要

在两项针对健康男性受试者的单盲、安慰剂对照、剂量递增研究中,对鲁贝唑的单剂量药代动力学进行了研究。在第一项研究中,6名受试者接受了2.5毫克、5毫克和10毫克鲁贝唑的静脉输注。在第二项研究中,给6名受试者服用了15毫克剂量的鲁贝唑,其中5名还接受了20毫克鲁贝唑,2名还接受了25毫克鲁贝唑。输注后,血浆鲁贝唑浓度呈双相衰减,平均分布半衰期(t1/2α)为30至65分钟,平均终末半衰期(t1/2β)为15至24小时。两项研究的结果表明,在健康男性受试者测试的剂量范围内,鲁贝唑呈现线性动力学。

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