Fujiwara K, Miyagi Y, Hayase R, Yoshinouchi M, Kobashi Y, Kohno I, Sekiba K
Dept. of Obstetrics and Gynecology, Okayama University Medical School.
Gan To Kagaku Ryoho. 1988 Jun;15(6):1943-8.
A pharmacokinetics and platinum concentration in the gynecologic organs were measured following the intravenous drip infusion of 375 mg/m2 of CBDCA. Total platinum (TP) in plasma decreased biphasically and free platinum (FP) was almost monophasically eliminated. The t 1/2 of FP was about 51 min. and the percentage of FP out of TP at four hours after administration was more than 92%, which was much higher proportion compared with that of cisplatin (CDDP). A cumulative excretion of platinum in the urine within 24 hours was 69%. The platinum concentration in the benign part of portio and endocervix were higher than that of malignant portion, although there were no significant differences in other pelvic organs such as ovary and tubes. However, pelvic lymph-nodes showed less platinum concentration both in metastatic and non-metastatic tissues. Platinum concentration in the tissue did not change significantly with lapse of time. Bone marrow suppression was observed especially in the patients who had received chemotherapy or radiotherapy. No renal toxicity was observed even without any hydration and gastro-intestinal toxicity was much milder than that of CDDP.
在静脉滴注375mg/m²的卡铂后，测量了妇科器官中的药代动力学和铂浓度。血浆中的总铂（TP）呈双相下降，游离铂（FP）几乎呈单相消除。FP的t 1/2约为51分钟，给药后4小时FP占TP的百分比超过92%，与顺铂（CDDP）相比比例高得多。24小时内尿中铂的累积排泄率为69%。虽然在卵巢和输卵管等其他盆腔器官中没有显著差异，但宫颈阴道部和宫颈管良性部分的铂浓度高于恶性部分。然而，盆腔淋巴结在转移组织和非转移组织中的铂浓度均较低。组织中的铂浓度不会随时间显著变化。特别是接受过化疗或放疗的患者出现了骨髓抑制。即使没有任何水化措施也未观察到肾毒性，胃肠道毒性比CDDP轻得多。
