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卡米诺霉素在人体中的药代动力学:双周给药方案与每三周单剂量给药方案的对比

Pharmacokinetics of carminomycin in man: biweekly schedule vs single dose every three weeks.

作者信息

Weenen H, Pinedo H M, de Planque M M, Ten Bokkel Huinink W W, McVie J G, Lankelma J

出版信息

Eur J Cancer Clin Oncol. 1984 Jul;20(7):915-8. doi: 10.1016/0277-5379(84)90164-0.

Abstract

Carminomycin was administered to five patients at a dose of 7.5 mg/m2 twice weekly. Plasma and urine samples were obtained during two subsequent 72-hr periods following drug administration, and assayed for carminomycin (C) and carminomycinol (Col) by HPLC with fluorescence detection. Distribution of carminomycin was rapid and drug levels decreased below the detection limit (5 X 10(-9)M) within 24 hr. Carminomycinol appeared very quickly and surpassed carminomycin levels in 10 min-4 hr, disappearing very slowly, with a half-life of 40-98 hr. No major differences in pharmacokinetic behavior were found when comparing the five patients in this study with patients who received 18 mg/m2, as described in a previous report. After the second dose of carminomycin in the 7.5 mg/m2 twice weekly schedule, however, carminomycin pharmacokinetics were found to be altered in comparison with the first dose, the most pronounced difference being an increase in the t1/2 for Col from 65 +/- 28 to 173 +/- 81 hr.

摘要

向5名患者施用卡米诺霉素,剂量为7.5毫克/平方米,每周两次。在给药后的两个连续72小时期间采集血浆和尿液样本,并通过带荧光检测的高效液相色谱法测定卡米诺霉素(C)和卡米诺霉素醇(Col)。卡米诺霉素分布迅速,药物水平在24小时内降至检测限(5×10⁻⁹M)以下。卡米诺霉素醇出现得非常快,在10分钟至4小时内超过卡米诺霉素水平,消失非常缓慢,半衰期为40至98小时。将本研究中的5名患者与先前报告中描述的接受18毫克/平方米的患者进行比较时,未发现药代动力学行为有重大差异。然而,在每周两次、每次7.5毫克/平方米的给药方案中,第二次给予卡米诺霉素后,发现卡米诺霉素的药代动力学与第一次给药相比有所改变,最明显的差异是Col的t1/2从65±28小时增加到173±81小时。

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