Robert J, Rigal-Huguet F, Huet S, Pris J, Hurteloup P
Fondation Bergonié, Bordeaux, France.
Leukemia. 1990 Mar;4(3):227-9.
We have studied the plasma pharmacokinetics of idarubicin (4-demethoxy daunorubicin) in 11 elderly patients suffering from acute myeloblastic leukemia receiving orally 30 mg/m2 per day for 3 consecutive days. Idarubicin culminated in plasma 4 hr after administration and followed three similar time courses after the three administrations. Idarubicinol (13-dihydro-4-demethoxy daunorubicin) was the only fluorescent metabolite in plasma and no aglycone could be detected; idarubicinol concentration was always higher than that of unchanged idarubicin. Due to its protracted half-life (64 hr in this study), this metabolite progressively accumulated and the ratio of the areas under the curve (0-24) idarubicinol/idarubicin increased from day to day. By comparison to results obtained after i.v. administration of the drug in another study, the bioavailability of idarubicin alone can be estimated to about 21%, whereas the bioavailability of the sum idarubicin + idarubicinol is about 41%.
我们研究了伊达比星（4-去甲氧基柔红霉素）在11例老年急性髓细胞白血病患者中的血浆药代动力学，这些患者连续3天每天口服30mg/m²。伊达比星在给药后4小时达到血浆峰值，三次给药后呈现三个相似的时间过程。伊达比星醇（13-二氢-4-去甲氧基柔红霉素）是血浆中唯一的荧光代谢产物，未检测到糖苷配基；伊达比星醇的浓度始终高于未代谢的伊达比星。由于其半衰期较长（本研究中为64小时），该代谢产物逐渐蓄积，曲线下面积（0-24）伊达比星醇/伊达比星的比值逐日增加。与另一项研究中静脉给药后的结果相比，伊达比星单独的生物利用度估计约为21%，而伊达比星+伊达比星醇的总生物利用度约为41%。
