Gouyette A, Apchin A, Foka M, Richard J M
Eur J Cancer Clin Oncol. 1986 Mar;22(3):257-63. doi: 10.1016/0277-5379(86)90389-5.
After administration of cisplatin (50 mg/m2 on days 1 and 2) by intra-arterial or intravenous infusions over 1 or 6 hr to a total of 24 patients with head and neck cancer, the main pharmacokinetic parameters of platinum were determined according to a multicompartmental analysis. Elimination half-life of total platinum is greater than 3 days, the amount of platinum recovered in the urine over 7 days accounting for 15-50% of the administered dose. The half-life of filterable platinum species was calculated from the urinary excretion data: 39 +/- 17 min (i.a./1 hr), 37 +/- 24 min (i.a./6 hr), 58 +/- 17 min (i.v./1 hr) and 51 +/- 22 min (i.v./6 hr). Biopsies of the tumor were also analyzed on day 3 for their platinum content. The mean concentrations of platinum in biopsies were: 2.72 micrograms/g (i.a./1 hr), 3.89 micrograms/g (i.a./6 hr), 1.27 micrograms/g (i.v./1 hr) and 1.38 micrograms/g (i.v./6 hr). Tumor regression, based upon clinical and histological data, was only moderate after this single chemotherapy course.
对头颈部癌患者24例分别采用动脉内或静脉内输注顺铂（第1天和第2天剂量为50mg/m²），输注时间为1小时或6小时，之后根据多室分析确定铂的主要药代动力学参数。总铂的消除半衰期大于3天，7天内尿中回收的铂量占给药剂量的15%-50%。可滤过铂类的半衰期根据尿排泄数据计算得出：动脉内输注1小时为39±17分钟，动脉内输注6小时为37±24分钟，静脉内输注1小时为58±17分钟，静脉内输注6小时为51±22分钟。在第3天还对肿瘤活检组织进行了铂含量分析。活检组织中铂的平均浓度分别为：动脉内输注1小时为2.72微克/克，动脉内输注6小时为3.89微克/克，静脉内输注1小时为1.27微克/克，静脉内输注6小时为1.38微克/克。根据临床和组织学数据，在这一疗程化疗后肿瘤退缩程度仅为中等。
