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健康志愿者中溴丙胺太林的药代动力学

Pharmacokinetics of prifinium bromide in healthy volunteers.

作者信息

Noguchi H, Tokuma Y, Tamura Y

出版信息

Int J Clin Pharmacol Ther Toxicol. 1983 May;21(5):213-7.

PMID:6134685
Abstract

The pharmacokinetics of prifinium bromide (Riabal), a specific antispasmodic agent, after oral (60 mg) and i.v. (7.5 mg) administration was studied in six healthy male volunteers. After i.v. administration, the drug was rapidly cleared from the serum. Individual serum levels were described by a bi-exponential equation and mean elimination half-life was 2.13 h. The volume of distribution at steady state was about 190% of body weight, and the total serum clearance and renal clearance were 12.5 and 5.80 ml/(min. kg), respectively. The drug reached maximum serum levels (6.76-14.3 ng/ml) within 2-3 h after administration of tablets: the apparent biologic half-life after oral dosing was 2.18 h. The oral bioavailability was low (3.4%), as expected for quaternary ammonium compounds, but the inter-individual variation of bioavailability was small.

摘要

在六名健康男性志愿者中研究了特异性抗痉挛药溴丙胺太林(Riabal)口服(60毫克)和静脉注射(7.5毫克)后的药代动力学。静脉注射后,药物迅速从血清中清除。个体血清水平用双指数方程描述,平均消除半衰期为2.13小时。稳态分布容积约为体重的190%,总血清清除率和肾清除率分别为12.5和5.80毫升/(分钟·千克)。给药片剂后2 - 3小时内药物达到最大血清水平(6.76 - 14.3纳克/毫升):口服给药后的表观生物半衰期为2.18小时。如季铵化合物所预期的那样,口服生物利用度较低(3.4%),但生物利用度的个体间差异较小。

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