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本文报道用高效液相色谱法(HPLC)检测尿中异喹胍(Debrisoquine,D)及其在体内的代谢产物4-羟异喹胍(4-hydroxydebrisoquine,HD)排泄量的新方法。并依此计算人体对D的代谢比值,进行志愿者药物羟化代谢的初步研究。胍生(G)为内标,样本用乙酰丙酮衍生化后,经碱化-酸化-碱化溶剂提取。流动相为甲醇:水73:27(v/v),pH3.5,分析柱ODS C_(18),紫外检测波长248nm。尿中D和HD的浓度在0.1～20μg/ml范围内直线相关,r=0.9998,最低检测浓度为0.01μg/ml,四个浓度的方法回收率为97％～103％,天内精密度(CV)1.4％～3.3％,天间精密度(CV)3.0％～5.2％,10例健康志愿者一次口服10 mg D,测算服药后8h内尿中D和HD的含量,代谢比值在0.16—7.95间,均属快代谢型者。
This paper reports a new method for the determination of urinary release of 4-hydroxydebrisoquine (HD) by using high performance liquid chromatography (HPLC) in the urine of Debrisoquine (D) and its metabolites. Based on this, the metabolic ratio of human body to D was calculated and the preliminary study of hydroxylation metabolism of volunteers was carried out. Guanidine (G) as an internal standard, the sample is derivatized with acetylacetone, the alkalization - acidification - alkalinization solvent extraction. Mobile phase methanol: water 73:27 (v / v), pH3.5, analytical column ODS C_ (18), UV detection wavelength of 248nm. The concentration of urine D and HD in the range of 0.1 ~ 20μg / ml linear correlation, r = 0.9998, the minimum detection concentration of 0.01μg / ml, four concentrations of the method recovery was 97% to 103%, intraday precision ) 1.4% ~ 3.3%, intrauterine densities (CV) 3.0% ~ 5.2%, 10 healthy volunteers orally 10 mg D, measured within 8h after taking the urine D and HD in the urine, the metabolic ratio of 0.16-7.95 Room, are fast metabolism type.