DeMarco L C, Budman D R, Lathia C, Amorusi P, Birkhofer M, Lichtman S, Weiselberg L, Vinciguerra V, Lovecchio J, Gal D
Don Monti Division of Medical Oncology, Department of Medicine, North Shore University Hospital/Cornell University Medical College, Manhasset, NY 11030, USA.
Cancer Chemother Pharmacol. 1995;36(1):35-40. doi: 10.1007/BF00685729.
Zeniplatin, a more water-soluble organoplatinum than cisplatin, was evaluated for clinical pharmacology in the context of a phase II trial in previously treated patients with ovarian carcinoma. A total of 12 patients were given zeniplatin at 120 mg/m2 by rapid intravenous infusion over 90 min, with both blood and urine being sampled. All platinum moieties were analyzed in whole blood, plasma, plasma ultrafiltrate, and urine by atomic absorption, and free zeniplatin was analyzed in plasma ultrafiltrate by specific high-performance liquid chromatography (HPLC). In a comparison of the platinum-time concentration curve, AUC (area under the curve) values indicated that approximately 90% of platinum moieties were bound to circulating plasma proteins. There was no evidence of drug accumulation after repetitive dosing. The terminal half-life (t1/2) of this drug in plasma ultrafiltrate (3.7-7.2 h.) as measured by HPLC was slightly longer than that of carboplatin, whereas total platinum moieties in plasma displayed a long t1/2 (124-154 h). Approximately 60% of platinum moieties could be recovered in the urine within 24 h. These findings suggest that zeniplatin has a pharmacokinetic profile similar to that of carboplatin.
泽铂是一种比顺铂水溶性更强的有机铂化合物，在一项针对既往接受过治疗的卵巢癌患者的II期试验中对其进行了临床药理学评估。共有12例患者接受了90分钟内快速静脉输注120mg/m²泽铂的治疗，并采集了血液和尿液样本。通过原子吸收法对全血、血浆、血浆超滤液和尿液中的所有铂部分进行分析，通过特定的高效液相色谱法（HPLC）对血浆超滤液中的游离泽铂进行分析。在铂-时间浓度曲线的比较中，曲线下面积（AUC）值表明约90%的铂部分与循环血浆蛋白结合。重复给药后没有药物蓄积的证据。通过HPLC测定，该药物在血浆超滤液中的终末半衰期（t1/2）（3.7 - 7.2小时）略长于卡铂，而血浆中的总铂部分显示出较长的t1/2（124 - 154小时）。约60%的铂部分可在24小时内从尿液中回收。这些发现表明泽铂具有与卡铂相似的药代动力学特征。
