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卡米诺霉素在犬类和人类中的药代动力学。初步报告。

Pharmacokinetics of carminomycin in dogs and humans. Preliminary report.

作者信息

Reich S D, Fandrich S E, Finkelstein T T, Schurig J E, Florczyk A P, Comis R L, Crooke S T

出版信息

Cancer Chemother Pharmacol. 1981;6(2):189-93. doi: 10.1007/BF00262341.

Abstract

Carminomycin was administered to four dogs and two human patients as a single intravenous dose. Plasma samples were obtained and assayed for carminomycin and carminomycinol by high pressure liquid chromatography with fluorescence detection. The plasma disappearance of carminomycin could be described by a three-compartment open model. Distribution was rapid and the apparent volume of distribution was greater than 100 l/m2 in both species. The terminal half-life of drug was 86 h in dogs and 20 h in humans. In both dogs and humans carminomycinol concentrations rapidly surpassed carminomycin levels, and terminal half-lives were longer than for the parent compound in the two species. Since carminomycinol has antitumor activity and host toxicity, this metabolite may play an important role in the efficacy and toxicity of carminomycin therapy.

摘要

向四只狗和两名人类患者静脉注射一剂卡米诺霉素。采集血浆样本,采用带荧光检测的高压液相色谱法测定卡米诺霉素和卡米诺霉素醇。卡米诺霉素的血浆消除情况可用三室开放模型描述。分布迅速,两种物种的表观分布容积均大于100 l/m²。药物的终末半衰期在狗中为86小时,在人类中为20小时。在狗和人类中,卡米诺霉素醇的浓度迅速超过卡米诺霉素水平,且两种物种中其终末半衰期均长于母体化合物。由于卡米诺霉素醇具有抗肿瘤活性和宿主毒性,这种代谢产物可能在卡米诺霉素治疗的疗效和毒性中起重要作用。

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