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阿霉素及阿霉素代谢产物的药代动力学(作者译)

[The pharmacokinetics of adriamycin and adriamycin-metabolites (author's transl)].

作者信息

Ehninger G, Stocker H J, Proksch B, Wilms K

出版信息

Klin Wochenschr. 1980 Sep 15;58(18):927-34. doi: 10.1007/BF01477050.

Abstract

A sensitive reproducible, nondestructive method for the determination of adriamycin and its metabolites in plasma, leukocytes and tissues has been developed. Apolar substances as adriamycinone (adm-one) were extracted at pH 2 with chloroform, polar ones as adriamycin (adm) and adriamycinol (adm-ol) at pH 8.8 with chloroform: methanol, separated by thin-layer-chromatography and quantitated by fluorescence spectrophotometry. The plasma levels of adm-ol and adm-one were lower in all patients compared to those of adm. Further metabolites were found in the bile. Toxic effects were found in patients with prolonged half-lives in the elimination phase. A delayed elimination was observed in a patient with an elevation of the bilirubin level, but also in patients without overt liver disease. The pharmacokinetics of adm showed considerable inter- and intraindividual fluctuations.

摘要

已开发出一种灵敏、可重复、非破坏性的方法,用于测定血浆、白细胞和组织中的阿霉素及其代谢产物。非极性物质如阿霉素酮(adm-one)在pH 2时用氯仿萃取,极性物质如阿霉素(adm)和阿霉素醇(adm-ol)在pH 8.8时用氯仿:甲醇萃取,通过薄层色谱分离并用荧光分光光度法定量。与阿霉素相比,所有患者中阿霉素醇和阿霉素酮的血浆水平较低。在胆汁中发现了进一步的代谢产物。在消除期半衰期延长的患者中发现了毒性作用。在一名胆红素水平升高的患者中观察到消除延迟,在无明显肝病的患者中也观察到了这种情况。阿霉素的药代动力学显示出相当大的个体间和个体内波动。

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