European Journal of Clinical Pharmacology

, Volume 17, Issue 5, pp 385–391

The pharmacokinetics of intravenous and oral sulpiride in healthy human subjects

  • F. -A. Wiesel
  • G. Alfredsson
  • M. Ehrnebo
  • G. Sedvall
Originals

Summary

The pharmacokinetics of sulpiride was studied in 6 healthy volunteers after intravenous and oral (tablets) administration of 100 mg. An open two- and in two subjects a three-compartment model was applied following intravenous administration. The average total distribution volume during the terminal slope was 2.72±0.66 l/kg and total systemic clearance was 415±84 ml/min. The serum half-life of the terminal slope following intravenous administration averaged 5.3 h (range 3.7–7.1 h) according to the two-compartment model. In two subjects the half-lives were 11.0 and 13.9 h when the three-compartment model was applied. Determination of urinary excretion rates of unchanged sulpiride indicated a half-life of 7.15 h. Following intravenous administration, 70±9% of the dose was recovered unchanged in urine within 36 h; the mean renal clearance was 310±91 ml/min. Sulpiride was absorbed slowly, with peak concentrations appearing between 3 and 6 h after oral administration. The recovery of unchanged drug in urine following oral administration was 15±5% of the dose, with a mean renal clearance of 223±47 ml/min. The bioavailability determined from combined plasma and urine data was only 27±9%. The low bioavailability was probably due to incomplete absorption.

Key words

sulpiride pharmacokinetics serum clearance renal clearance bioavailability healthy volunteers 

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Copyright information

© Springer-Verlag 1980

Authors and Affiliations

  • F. -A. Wiesel
    • 1
  • G. Alfredsson
    • 1
  • M. Ehrnebo
    • 2
  • G. Sedvall
    • 1
  1. 1.Laboratory of Experimental Psychiatry, Department of PsychiatryKarolinska InstituteStockholmSweden
  2. 2.Karolinska PharmacyKarolinska HospitalStockholmSweden

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