Hall S W, Yeung K, Benjamin R S, Stewart D, Valdivieso M, Bedikian A Y, Loo T L
Clin Pharmacol Ther. 1979 Jan;25(1):82-7. doi: 10.1002/cpt197925182.
Pharmacokinetic studies were conducted in 8 patients with disseminated neoplasms refractory to conventional chemotherapy, who received gallium nitrate at doses of 300 to 600 mg/m2 intravenously in a phase I clinical trial. Gallium concentrations in biological fluids were determined colorimetrically. In patients with normal renal function, gallium showed a biphasic plasma disappearance with an initial half-life (t1/2) of 0.5 to 1.8 hr (mean 1.0) and a terminal t1/2 of 10.5 to 50.4 hr (mean 25.1). Gallium was distributed in total body water and often localized in some body compartment as evidenced by a volume of distribution ranging from 0.25 to 2.53 L/kg (mean 1.19). The total drug clearance from the plasma was 0.13 to 1.00 ml/kg/min (mean 0.65) in patients with normal renal function. Cumulative urinary excretion of gallium was 15% to 72% (mean 35%) of the administered dose in 24 hr (it fell to 23% in 8 days in a patient with acute oliguric renal failure). Gallium kinetics are altered in patients with acute renal dysfunction and in patients who have received multiple doses of gallium or other metal chemotherapy.
在一项I期临床试验中，对8例常规化疗难治的播散性肿瘤患者进行了药代动力学研究，这些患者静脉注射硝酸镓，剂量为300至600mg/m²。采用比色法测定生物体液中的镓浓度。在肾功能正常的患者中，镓的血浆清除呈双相，初始半衰期（t1/2）为0.5至1.8小时（平均1.0小时），终末t1/2为10.5至50.4小时（平均25.1小时）。镓分布于全身水分中，常定位于某些身体腔室，分布容积范围为0.25至2.53L/kg（平均1.19）。肾功能正常患者的血浆总药物清除率为0.13至1.00ml/kg/min（平均0.65）。镓的24小时累积尿排泄量为给药剂量的15%至72%（平均35%）（急性少尿性肾衰竭患者在8天内降至23%）。急性肾功能不全患者以及接受多剂量镓或其他金属化疗的患者，其镓动力学发生改变。
