RPHPLC法测定氨吡酮及其在家兔体内的药代动力学

RPHPLC ESTIMATION OF AMRINCNE IN BIOLOGICAL FLUIDS AND ITS PHARMACOKINETIC APPLICATION IN RABBITS

氨吡酮为一强心类药物,其血、尿药浓度可用反相高效液相色谱法(RPHPLC)测定。氨吡酮及内标安替比林在pH8条件下提取至乙酸乙酯中,再用1 mol/L HCl回提净化后,在YWG-C_(18)H_(87)柱上用流动相甲醇-水-N,N,N′,N′-四甲基乙二胺(37:63:0.3V/V)分离,于UV254nm检测。最低检测浓度为0.1 μg/ml。方法回收率为100.5±0.46％。日内和日间变导系数(CV％)分别为3.78％和1.63％(n=5)。样品的内源性杂质和其他抗心血管病药物不干扰测定。家兔按10 mg/kg单剂量静脉给药后,用本法测定氨吡酮的经时药物浓度,C-T曲线符合二室模型,T_(1/2)(β)=1.99±0.20(p=5),尿中原药24h的排泄率为给药量的38.73％±14.55％。

Amrinone (I) is a new domestically synthesized oardlotonio agent. A method for determination of amrinone in biological fluids by HPLC was developed. Both (I) and antipyrin (I. S.) were extracted from serum with ethyl acetate at pH8, and were back-extraoted into Imol/L HCl. The final extract was chromatographed on an YWG C18H37 column with a mobile phase of methanoi-water-N, N, N'N'-tetramethylethylendiamine (37:63:0.3V/V) and detected at UV 254nm. The minimal detectable level bf (I) in serum was 0.1μg/ml. The relative recovery rate was 100.5±0.4.6%. The CV% of intra-and inter-days were 3.78%. and 1.63%(n = 5) respectively. Endogenous impurities, other oardiotonio agent or potential metabolites didn't cause interference.Five rabbits each received 10mg/kg of I I.V. as a single dose. The C-T curve fitted in with a two-compartment model,t1/2=1.99±0.20h (n=5). The 24 hour's excretion rate of the parent drug in the urine was about 38.73±14.55% of the total amount administered.