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醋柳黄酮的药代动力学研究。 (注:原文中的“vincamine teprosilate”常见的中文名是“醋柳黄酮”,但严格来说如果没有更多背景信息可能翻译不够准确,因为“vincamine”也可音译为“长春胺” ,这里按常见译法给出。)

Pharmacokinetic study of vincamine teprosilate.

作者信息

Cadórniga R, Saiz Vadillo M C, Molina I T, Cadórniga L

出版信息

Int J Clin Pharmacol Res. 1984;4(4):281-90.

PMID:6500775
Abstract

The results obtained by the authors in the pharmacokinetic study of vincamine teprosilate after oral and i.v. administration to young healthy volunteers and after oral administration to patients aged 68 to 84 years are presented. The description of the assay for each administration route is reported in the protocol. Plasma levels of vincamine teprosilate were assayed by reverse phase HPLC with spectrofluorimetric detection. The data obtained after i.v. administration made it possible to define the pharmacokinetic model and to estimate parameters. Concentration-time data were adapted to a biocompartmental open model with alpha value of 2.9080 and beta value 0.1047. In oral administration, the overlapping of the fast disposition phase and the absorption phase led to an apparent monocompartmental fit; in both young and aged volunteers, the absorption rate constants as well as the elimination rate constants were calculated. In both groups no significant differences in tmax values were found and no latency period was noticed . Cmax values were similar in both groups of patients; the lower distribution volume in aged volunteers compared to younger ones contributed to this finding. Differences in absorption rate constants in aged and young volunteers (0.53 h-1 and 0.73 h-1 respectively) are analysed. Vincamine teprosilate bioavailability after oral administration was found to be 20 +/- 5%. Possible vincamine teprosilate dose dependence kinetics are suggested.

摘要

本文介绍了作者对年轻健康志愿者口服和静脉注射替普罗西酯长春胺以及对68至84岁患者口服后进行药代动力学研究的结果。每种给药途径的分析方法在方案中有描述。采用反相高效液相色谱-荧光检测法测定血浆中替普罗西酯长春胺的水平。静脉注射给药后获得的数据有助于确定药代动力学模型并估算参数。浓度-时间数据采用双室开放模型拟合,α值为2.9080,β值为0.1047。口服给药时,快速处置相和吸收相重叠导致呈现出明显的单室拟合;在年轻和老年志愿者中,均计算了吸收速率常数和消除速率常数。两组的tmax值均无显著差异,也未观察到潜伏期。两组患者的Cmax值相似;老年志愿者的分布容积低于年轻志愿者,这导致了该结果。分析了老年和年轻志愿者吸收速率常数的差异(分别为0.53 h-1和0.73 h-1)。口服替普罗西酯长春胺后的生物利用度为20±5%。文中还提出了替普罗西酯长春胺可能存在的剂量依赖性动力学。

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