Lee Y T, Chan K K, Harris P A, Cohen J L
Cancer. 1980 May 1;45(9):2231-9. doi: 10.1002/1097-0142(19800501)45:9<2231::aid-cncr2820450902>3.0.co;2-3.
Twenty patients with solid tumors received 30 mg/M2 of adriamycin. Various tissue samples were intraoperatively obtained from 18 patients, about 1.5--5 hours after an intravenous (IV) bolus dose. Normal liver showed the highest levels of adriamycin uptake (2.3--19.8 micrograms/g); lymph nodes were second; muscle and bone marrow, next; fat and skin had the lowest adriamycin uptake (0.04--0.40 microgram/g). Tumor tissue, excluding that with much necrosis and hemorrhaging, had adriamycin concentrations which approximated those of the liver (1.1--9.2 micrograms/g). Six patients, all with hepatic malignancies, had prolonged plasma concentration studies after IV administration; 5 also had adriamycin administered directly into the hepatic artery catheter. Adriamycin-plasma-time courses were similar, whether the drug was administered by bolus directly into the hepatic artery or peripheral vein. The concentration of metabolites after hepatic intraarterial administration was definitely higher than that after IV administration. Patients with hepatic dysfunction had delayed plasma clearance and secondarily elevated levels approximately 160 and 300 minutes after administration.
20例实体瘤患者接受了30mg/M²的阿霉素治疗。在静脉推注给药后约1.5 - 5小时,从18例患者术中获取了各种组织样本。正常肝脏的阿霉素摄取水平最高(2.3 - 19.8微克/克);淋巴结次之;肌肉和骨髓再次之;脂肪和皮肤的阿霉素摄取最低(0.04 - 0.40微克/克)。除有大量坏死和出血的肿瘤组织外,肿瘤组织的阿霉素浓度与肝脏相近(1.1 - 9.2微克/克)。6例均为肝恶性肿瘤的患者在静脉给药后进行了延长的血浆浓度研究;其中5例还通过肝动脉导管直接给予阿霉素。无论药物是通过直接注入肝动脉还是外周静脉推注给药,阿霉素 - 血浆 - 时间曲线相似。肝动脉内给药后代谢物的浓度明显高于静脉给药后。肝功能不全的患者血浆清除延迟,给药后约160分钟和300分钟时水平继发升高。