Brès J, Bressolle F
Laboratoire de Pharmacocinétique, Faculté de Pharmacie, Université de Montpellier I, France.
J Pharm Sci. 1991 Dec;80(12):1119-24. doi: 10.1002/jps.2600801206.
The pharmacokinetics of sulpiride in plasma, red blood cells (RBC), and urine were investigated after administration of 100 mg by the iv route to 15 subjects and by the im route to 12 subjects. The concentrations of sulpiride in plasma, RBC, and urine were measured by HPLC. All the data were consistent with a two-compartment, open-body model. After iv administration, the mean +/- SD apparent elimination half-life of sulpiride was 6.47 +/- 1.00 h, and the mean +/- SD volume of distribution at steady state was 0.94 +/- 0.23 L/kg. Renal clearance (119.5 +/- 28.2 mL/min) was very close to total clearance (127.8 +/- 26.2 mL/min). In urine, the mean +/- SD recovery in form of the unchanged drug was 90.0 +/- 9.68% of the administered dose, and the excretion rate versus time showed an elimination half-life similar to that found in plasma. The values of all these parameters were very close to those obtained after im administration. The sulpiride partition coefficient between RBC and plasma did not show any significant change as a function of time and concentration, with a mean value +/- SD of 1.00 +/- 0.043, indicating that sulpiride is evenly distributed between RBC and plasma. The pharmacokinetic parameters determined from the plasma and the RBC data were similar.
对15名受试者静脉注射100毫克舒必利以及对12名受试者肌肉注射100毫克舒必利后，研究了舒必利在血浆、红细胞（RBC）和尿液中的药代动力学。采用高效液相色谱法（HPLC）测定血浆、红细胞和尿液中舒必利的浓度。所有数据均符合二室开放体模型。静脉注射后，舒必利的平均±标准差表观消除半衰期为6.47±1.00小时，稳态分布容积平均±标准差为0.94±0.23升/千克。肾清除率（119.5±28.2毫升/分钟）与总清除率（127.8±26.2毫升/分钟）非常接近。在尿液中，以原形药物形式的平均±标准差回收率为给药剂量的90.0±9.68%，排泄率随时间变化的消除半衰期与血浆中相似。所有这些参数的值与肌肉注射后获得的值非常接近。红细胞与血浆之间的舒必利分配系数未显示随时间和浓度的任何显著变化，平均值±标准差为1.00±0.043，表明舒必利在红细胞和血浆中均匀分布。根据血浆和红细胞数据确定的药代动力学参数相似。
