口服和静脉给药后isradipine的生物利用度和药代动力学:半衰期比预期短?

H R Christensen, K Antonsen, K Simonsen, A Lindekaer, J Bonde, H R Angelo, J P Kampmann
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引用次数: 20

摘要

以色列地平是一种二氢吡啶型钙通道阻滞剂,用于治疗高血压。在几项药物动力学研究中,口服伊拉西平的终末半衰期为8-9小时。在一项尚未发表的研究中,观察到半衰期要短得多,因此本试验是为了估计静脉注射伊拉西平后的半衰期。并对其生物利用度进行了估计。在一项随机交叉设计中,10名健康的年轻志愿者口服或静脉输注伊拉西平。两个研究期至少间隔3天。给药后10-12小时采集血液样本用于测量伊地平浓度,并估计半衰期和生物利用度。静脉给药后的平均终末半衰期为2.8小时,生物利用度为0.28。这10名受试者都没有出现副作用。在目前的静脉注射研究中,伊拉西平的半衰期似乎比以前的口服研究显示的要短得多。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Bioavailability and pharmacokinetics of isradipine after oral and intravenous administration: half-life shorter than expected?

Isradipine is a calcium channel-blocking agent of the dihydropyridine type, used in the treatment of hypertension. A terminal half-life of 8-9 hr has been reported, in several pharmacokinetic studies after oral administration of isradipine. In a yet unpublished study a much shorter half-life was observed, and the present trial was therefore conducted in order to estimate the half-life after intravenous administration of isradipine. The bioavailability was estimated as well. In a randomised cross-over design ten healthy young volunteers were given either isradipine orally or an intravenous infusion. The two study periods were separated by at least 3 days. Blood samples for measurement of isradipine concentration were collected for 10-12 hr after administration and half-life and bioavailability were estimated. Mean terminal half-life after intravenous administration was calculated to be 2.8 hr, and the bioavailability to be 0.28. None of the 10 subjects suffered from side effects. In the present intravenous study the half-life of isradipine seems to be of much shorter than demonstrated in previous oral studies.

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