Colombo T, Broggini M, Garattini S, Donelli M G
Eur J Drug Metab Pharmacokinet. 1981;6(2):115-22. doi: 10.1007/BF03189477.
The differential distribution of doxorubicin (Adriamycin = AM) and daunorubicin (Daunomycin = DM) within the blood components, after an i.v. injection of 10 or 15 mg/kg of body weight, was investigated from its metabolites and quantified by means of the TLC scanning fluorescence technique. AM accumulated in the following order (of decreasing percentages): plasma and red cells (RBC), white cells (WBC), and platelets (PT), but the absolute amount of drug that reached each cell type was related to its relative volume. In the presence of higher blood concentrations (after injection of 15 mg/kg of body weight) the RBCs accumulated much more AM than the plasma, WBC, and PT; suggesting that the RBC fraction has a greater capacity to concentrate the drug. However, if the concentration of AM is expressed per unit volume of each component, a markedly higher value was observed for PT, and this was confirmed by in vitro results obtained by incubating blood in the presence of AM. DM seemed to be distributed on a percent basis to a greater extent than AM in the RBC fraction. Both compounds were taken up by blood cells, particularly platelets, to levels in excess of the extracellular concentration.
静脉注射10或15mg/kg体重后,通过代谢产物研究了阿霉素(阿霉素=AM)和柔红霉素(柔红霉素=DM)在血液成分中的差异分布,并采用薄层色谱扫描荧光技术进行定量。AM按以下顺序积累(百分比递减):血浆和红细胞(RBC)、白细胞(WBC)和血小板(PT),但到达每种细胞类型的药物绝对量与其相对体积有关。在较高血药浓度下(注射15mg/kg体重后),RBC积累的AM比血浆、WBC和PT多得多;这表明RBC部分具有更大的药物浓缩能力。然而,如果按各成分单位体积表示AM浓度,则PT的值明显更高,这一点通过在AM存在下孵育血液获得的体外结果得到证实。DM似乎比AM在RBC部分中按百分比分布的程度更大。两种化合物都被血细胞,特别是血小板摄取,其水平超过细胞外浓度。