Hall S W, Strong J E, Broughton A, Frazier M L, Benjamin R S
Cancer Chemother Pharmacol. 1982;9(1):22-5. doi: 10.1007/BF00296756.
Bleomycin pharmacokinetics were studied by radioimmunoassay in 11 patients who received 7-30 U intravenously (IV) and eight patients who received 4-30 U subcutaneously (SC). For patients who received IV bleomycin plasma disappearance was biphasic, with a mean initial half-life of 0.26 h and a terminal half-life of 2.3 h. Mean plasma drug clearance was 67.8 ml/min/m2 and the volume of distribution was 13.2 l/m2. Urinary excretion accounted for 63.9% of the drug in 24 h. After SC administration peak plasma levels occurred in 1.1 h, with a mean elimination half-life of 4.3 h. Mean plasma drug clearance was 60.5 ml/min/m2 and the volume of distribution was 19.2 l/m2. Bleomycin plasma clearance correlated well with serum creatinine (r2 = 0.72). Bleomycin has a rapid plasma elimination and urinary excretion. Bleomycin bioavailability after SC administration appears comparable to that seen after IV administration as determined by the areas under the plasma disappearance curves. Prolonged plasma levels are seen after SC injection, suggesting this route of administration can produce plasma concentrations comparable to those attained with continuous IV infusions.
采用放射免疫分析法对11例静脉注射（IV）7 - 30 U博来霉素的患者和8例皮下注射（SC）4 - 30 U博来霉素的患者进行了博来霉素药代动力学研究。接受静脉注射博来霉素的患者，其血浆药物消除呈双相，平均初始半衰期为0.26小时，终末半衰期为2.3小时。平均血浆药物清除率为67.8 ml/min/m²，分布容积为13.2 l/m²。24小时内尿液排泄占药物的63.9%。皮下注射后，血浆峰浓度在1.1小时出现，平均消除半衰期为4.3小时。平均血浆药物清除率为60.5 ml/min/m²，分布容积为19.2 l/m²。博来霉素血浆清除率与血清肌酐相关性良好（r² = 0.72）。博来霉素血浆消除迅速且经尿液排泄。根据血浆消除曲线下面积测定，皮下注射后博来霉素的生物利用度与静脉注射后的相当。皮下注射后可见血浆水平延长，提示该给药途径可产生与持续静脉输注相当的血浆浓度。
