Kleimola T, Leppänen O, Kanto J, Mäntylä R, Syvälahti E
Ann Clin Res. 1976 Apr;8(2):104-10.
A new spectorophotofluorometric method for the determination of sulpiride (S) in the human plasma and urine is described. The plasma concentrations (0--24 hours) and renal excretions (0--48 hours) of sulpiride were measured after Dogmatil forte (Schürholtz), or Sulpiril (Leiras) tablets both containing 200 mg of sulpiride, after two Sulpiril capsules (Leiras) containing 50 mg of sulpiride in each capsule, and after 20 ml Dogmatil saft (Schürholtz) and 20 ml Sulpiril mixt. (Leiras) both containing 5 mg/ml of sulpiride. There were no significant differences in the sulpiride concentrations in plasma or cumulative urinary excretion of sulpiride after Dogmatil forte (200 mg S) or Sulpiril tablet (200 mg S). Two Sulpiril capsules (100 mg S) produced significantly lower plasma concentrations of sulpiride at 3 hours than a Sulpiril tablet (200 mg S) and these were also lower at 4 and 6 hours than with either a Dogmatil forte (200 mg S) or a Sulpiril tablet (200 mg S). Two Sulpiril capsules (100 mg S) gave significantly higher plasma sulpiride concentrations from 1 to 6 hours than 20 ml Sulpiril mixt. (100 mg S) and from 2 to 6 hours higher than 20 ml Dogmatil saft (100 mg S). The plasma half-life of sulpiride measured after two Sulpiril capsules, 20 ml Dogmatil saft and 20 ml Sulpiril mixt., was 9.4 hours, 9.5 hours, and 10.2 hours, respectively. The renal excretion of sulpiride after two Sulpiril capsules (100 mg S) was significantly lower than after a Sulpiril tablet (200 mg S) from 8 to 48 hours, and also significantly lower than after a Dogmatil forte tablet (200 mg S) from 24 to 48 hours. Two Sulpiril capsules (100 mg S) gave significantly higher sulpiride urine concentrations from 8 to 24 hours than 20 ml Sulpiril mixt. (100 mg S) and from 24 to 48 hours than 20 ml Dogmatil saft (100 mg S). There was no significantly differences in this respect between either a Dogmatil forte tablet (200 mg S) and a Sulpiril tablet (200 mg S) or between Dogmatil saft (100 mg S) and Sulpiril mixt. (100 mg S). Comparied with a Dogmatil forte tablet, the bioavailability, calculated by the AUC24 for a Sulpiril tablet was 159%, for a Sulpiril capsule 118%, for Dogmatil saft 77%, and for Sulpiril mixt. 89%. The same values calculated from the sulpiride urine concentrations were 118%, 114%, 71%, and 67%, respectively. There were no significant differences in the blood pressure or heart rate of the volunteers during the experiment. 2 volunteers reported a sedative effect after a Dogmatil forte tablet.
本文描述了一种用于测定人血浆和尿液中舒必利(S)的新的分光光度荧光法。分别测定了服用含200mg舒必利的多马替尔强力片(舒尔霍茨公司)或舒必利片(莱拉斯公司)、服用两粒每粒含50mg舒必利的舒必利胶囊(莱拉斯公司)、服用20ml含5mg/ml舒必利的多马替尔溶液(舒尔霍茨公司)以及20ml含5mg/ml舒必利的舒必利混合液(莱拉斯公司)后舒必利的血浆浓度(0 - 24小时)和肾排泄量(0 - 48小时)。服用多马替尔强力片(200mg S)或舒必利片(200mg S)后,血浆中舒必利浓度或舒必利的累积尿排泄量无显著差异。两粒舒必利胶囊(100mg S)在3小时时产生的舒必利血浆浓度显著低于舒必利片(200mg S),在4小时和6小时时也低于多马替尔强力片(200mg S)或舒必利片(200mg S)。两粒舒必利胶囊(100mg S)在1至6小时的血浆舒必利浓度显著高于20ml舒必利混合液(100mg S),在2至6小时高于20ml多马替尔溶液(100mg S)。两粒舒必利胶囊、20ml多马替尔溶液和20ml舒必利混合液服用后测得的舒必利血浆半衰期分别为9.4小时、9.5小时和10.2小时。两粒舒必利胶囊(100mg S)在8至48小时的舒必利肾排泄量显著低于舒必利片(200mg S),在24至48小时也显著低于多马替尔强力片(200mg S)。两粒舒必利胶囊(100mg S)在8至