Roser R, Martinez L, Pares S, Sagarra R, Esteve J
Eur J Drug Metab Pharmacokinet. 1986 Jan-Mar;11(1):1-7. doi: 10.1007/BF03189768.
Single and multiple oral doses of Sultosilic acid were administered to four healthy volunteers. Plasma and Urine levels of unchanged Sultosilic acid (I) and its major metabolite (II) were measured. I and II were extracted from plasma and urine with chloroform after ion-pair formation and analysed by HPLC using a U.V. detector. Sultosilic acid was well absorbed and the plasma concentrations declined bioexponentially with mean half-lives of 1.9 h (fast disappearance phase, alpha) and 17.6 h (slow disappearance phase, beta) for I and 2.0 h (alpha) and 17.0 h (beta) for II. Renal clearances of I and II were 50.5 ml/min and 74.8 ml/min respectively. 60% of the administered dose was excreted in urine, 28% unchanged (I), the remainder as carboxylic derivative (II). Minimal drug concentrations in plasma in the range of those detected in steady state conditions were already found within the first day of treatment.
对四名健康志愿者单次及多次口服舒托硅酸。测定了未变化的舒托硅酸（I）及其主要代谢产物（II）的血浆和尿液水平。I和II在形成离子对后用氯仿从血浆和尿液中提取，并用配备紫外检测器的高效液相色谱法进行分析。舒托硅酸吸收良好，I的血浆浓度呈双指数下降，快速消除相（α）的平均半衰期为1.9小时，慢速消除相（β）为17.6小时；II的α相半衰期为2.0小时，β相为17.0小时。I和II的肾清除率分别为50.5毫升/分钟和74.8毫升/分钟。给药剂量的60%经尿液排泄，28%为未变化的I，其余为羧酸衍生物（II）。在治疗的第一天内就已发现血浆中的药物浓度处于稳态条件下检测到的最低浓度范围内。
