Gikalov I, Kaufmann R, Schuster O
Arzneimittelforschung. 1982;32(4):423-6.
The pharmacokinetic profile of azapropazone (Prolixan), sodium salt of 5-dimethylamino-9,5-dimethylamine-9-methyl-5-propyl-1H-pyrazolol[1,2-a][1,2,4]benzotriazine-1,3(2H)-dione, was established. Six healthy, adult volunteers received a single dose of either 600 mg or 1200 mg azapropazone as sodium salt intravenously. The drug was selectively separated from its metabolites and other plasmatic compounds and it was quantified by measurement of extinction at 254 nm. The kinetic parameters of azapropazone were independent of the applied dose (600 mg and 1200 mg): Biological half-life (t0.5): 16.8 +/- 2.95 h and 17.2 +/- 3.0 h; Total clearance (Cltot): 10.2 +/- 2.1 ml min-1 (both doses); Central volume of distribution (Vc): 3.7 +/- 0.71 and 3.9 +/- 0.91; Apparent volume of distribution (Vd): 12.5 +/- 2.91 and 14.4 +/- 2.41. Initial serum concentrations were 170 +/- 41.5 micrograms ml-1 and 326.3 +/- 84.5 micrograms ml-1, determined by extrapolation (C0 at time t0). The areas under the plasma concentration curves (AUC0 infinity) were calculated to amount 1052.5 +/- 217.4 micrograms ml-1h-1 and 2078.4 +/- 515.9 micrograms ml-1h-1. Three rate constants associated with the elimination of the drug could be calculated.
建立了阿扎丙宗（Prolixan），即5-二甲基氨基-9,5-二甲基胺-9-甲基-5-丙基-1H-吡唑并[1,2-a][1,2,4]苯并三嗪-1,3(2H)-二酮的钠盐的药代动力学特征。六名健康成年志愿者静脉注射了单剂量的600毫克或1200毫克阿扎丙宗钠盐。该药物与其代谢物及其他血浆化合物被选择性分离，并通过测量254纳米处的吸光度进行定量。阿扎丙宗的动力学参数与给药剂量（600毫克和1200毫克）无关：生物半衰期（t0.5）：分别为16.8±2.95小时和17.2±3.0小时；总清除率（Cltot）：均为10.2±2.1毫升/分钟；中央分布容积（Vc）：分别为3.7±0.71和3.9±0.91；表观分布容积（Vd）：分别为12.5±2.91和14.4±2.41。通过外推法（时间t0时的C0）测定的初始血清浓度分别为170±41.5微克/毫升和326.3±84.5微克/毫升。血浆浓度曲线下面积（AUC0至无穷大）经计算分别为1052.5±217.4微克·毫升-1·小时-1和2078.4±515.9微克·毫升-1·小时-1。可以计算出与药物消除相关的三个速率常数。
