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目的探讨国人使用口服 4-去甲氧柔红霉素 (IDA)的药代动力学 ,为临床用药提供理论依据。 方法应用反向高压液相技术 (HPLC)检测 6例初发老年急性白血病患者口服IDA后药物在血浆、单个核细胞和尿液中的药代动力学变化。 结果药物在单个核细胞内有较高的浓度 ,其变化与血浆内浓度变化一致 ;连续 3d用药 ,血浆及细胞内的浓度高峰出现于第 2d用药后的 6 0min ,或第 3d用药后的 2h左右 ;6d后还能测出药物浓度。第 2疗程用药的血浆药物浓度较第 1疗程低。 结论IDA疗效可能与药物进入细胞内及转化为醇式IDA(IDAOL)能力有关 ,药物血浆内浓度与细胞内浓度的关系有个体差异。用药 6d内药物尿排占总量的 0 .4%。
Objective To investigate the pharmacokinetics of oral 4-demethoxyribocin (IDA) in Chinese population and provide a theoretical basis for clinical use. Methods Reverse phase high-pressure liquid chromatography (HPLC) was used to detect the pharmacokinetics of six drug-eluting acute leukemia patients in the plasma, mononuclear cells and urine after oral administration of IDA. Results The drug had a higher concentration in mononuclear cells and the change was consistent with the change of plasma concentration. The peak of plasma and intracellular concentration peaked at 60 min after 2d or 2h after 3d About 6d after the drug concentration can be measured. The second course of treatment of plasma drug concentration lower than the first course of treatment. Conclusion The efficacy of IDA may be related to the ability of drugs to enter into cells and convert to alcohol IDAOL. There is an individual difference in the relationship between drug plasma concentration and intracellular concentration. Drugs 6d drug urine row accounted for 0.4% of the total.