Kuhn J G, Balmer C E, Ludden T M, Loesch D M, Von Hoff D D, Bender J F, Grillo-Lopez A J
Cancer Chemother Pharmacol. 1987;19(2):133-7. doi: 10.1007/BF00254565.
Ametantrone is the second anthracene derivative to enter clinical trials. The pharmacokinetic parameters for ametantrone acetate (CI-881) were characterized in six patients concurrently with the phase I clinical trial. Biological samples were assayed by a specific and sensitive high-performance liquid chromatography procedure. Plasma levels of ametantrone declined in a triexponential fashion, with a mean terminal half-life (t 1/2 gamma) of 25 h. The estimated mean total-body plasma clearance was 25.9 +/- 14.7 1 h-1 m-2. The steady-state volume of distribution (Vdss) was large, averaging 568 +/- 630 l/m2. Excretion of unchanged ametantrone in the urine over 48 h averaged 5.7% of the total dose, indicating that there is another major route of elimination.
氨甲蒽醌是进入临床试验的第二种蒽衍生物。在I期临床试验期间，对6名患者同时测定了醋酸氨甲蒽醌（CI - 881）的药代动力学参数。生物样品通过一种特异且灵敏的高效液相色谱法进行测定。氨甲蒽醌的血浆浓度呈三指数方式下降，平均终末半衰期（t 1/2γ）为25小时。估计的平均全身血浆清除率为25.9±14.7 l h-1 m-2。稳态分布容积（Vdss）很大，平均为568±630 l/m2。48小时内尿中未变化的氨甲蒽醌排泄量平均占总剂量的5.7%，表明存在另一条主要消除途径。
