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[KRN 8602在癌症患者中的药代动力学]

[Pharmacokinetics of KRN 8602 in cancer patients].

作者信息

Majima H, Shinkai H

机构信息

Institute of Microbial Chemistry, Kirin Brewery Co., LTD, Maebashi, Japan.

出版信息

Gan To Kagaku Ryoho. 1991 Dec;18(15):2589-95.

PMID:1746971
Abstract

The pharmacokinetic properties of KRN 8602, an anthracycline compound, was studied by HPLC following intravenous administration of KRN 8602 to cancer patients. The results were as follows. (1) The plasma concentration-time curve declined as a triphasic function (alpha, beta, gamma) (t1/2 (alpha) = 0.02910, +/- 0.0054 hr, t1/2 (beta) = 0.704 +/- 0.319 hr, t1/2 (gamma) 8.37 +/- 1.37 hr). The blood cell concentration was higher than that in plasma. (2) The distribution volumes of the tissue compartment were larger than those of the central compartment. This result suggested that KRN 8602 would be easily transferred into the tissues. (3) The area under the curve (AUC) of KRN 8602 increased in proportion to the increase of dosage. (4) The metabolites of KRN 8602 were detected in plasma, blood cell and urine. (5) Urinary excretion of KRN 8602 and its metabolites were extremely low.

摘要

对蒽环类化合物KRN 8602在癌症患者静脉注射后的药代动力学特性进行了高效液相色谱(HPLC)研究。结果如下:(1)血浆浓度-时间曲线呈三相函数(α、β、γ)下降(t1/2(α) = 0.02910 ± 0.0054小时,t1/2(β) = 0.704 ± 0.319小时,t1/2(γ) = 8.37 ± 1.37小时)。血细胞浓度高于血浆浓度。(2)组织室的分布容积大于中央室。该结果表明KRN 8602易于转移至组织中。(3)KRN 8602的曲线下面积(AUC)随剂量增加而成比例增加。(4)在血浆、血细胞和尿液中检测到KRN 8602的代谢产物。(5)KRN 8602及其代谢产物的尿排泄极低。

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