Kelsen D P, Alcock N, Yeh S, Brown J, Young C
Cancer. 1980 Nov 1;46(9):2009-13. doi: 10.1002/1097-0142(19801101)46:9<2009::aid-cncr2820460919>3.0.co;2-a.
Gallium nitrate is a new antineoplastic agent that has shown activity in a number of in vitro tumor systems. During a Phase I clinical trial, the pharmacokinetics of two methods of administration of gallium nitrate were studied: a seven-day continuous intravenous infusion, and a weekly rapid intravenous infusion. During the continuous infusion of 200 mg/M2 of gallium nitrate, plasma gallium concentrations of 0.9 +/- 0.2 microgram/ml in one patient, and 1.9 +/- 0.4 microgram/ml in a second were noted. Urine excretion of gallium approximated the daily administered dose by day 2-3. Overall, 68-107% of the total administered dose was recovered in the urine. Following a rapid intravenous infusion, a biphasic curve was generated. The T1/2 alpha ranged from 8.3-26 minutes; the T1/2 beta from 6.3-196 hours. From 69-91% of the administered dose was recovered in the urine. The effects of gallium nitrate on tissue localization and body retention of 67Ga are also presented.
硝酸镓是一种新型抗肿瘤药物，已在多种体外肿瘤系统中显示出活性。在一项I期临床试验中，研究了硝酸镓两种给药方法的药代动力学：为期7天的持续静脉输注和每周一次的快速静脉输注。在持续输注200mg/M2硝酸镓的过程中，一名患者的血浆镓浓度为0.9±0.2微克/毫升，另一名患者为1.9±0.4微克/毫升。到第2 - 3天时，镓的尿排泄量接近每日给药剂量。总体而言，尿中回收了总给药剂量的68 - 107%。快速静脉输注后，生成了一条双相曲线。T1/2α范围为8.3 - 26分钟；T1/2β范围为6.3 - 196小时。尿中回收了给药剂量的69 - 91%。还介绍了硝酸镓对67Ga的组织定位和体内潴留的影响。
