Sulpiride

Exposure related observations in humans: other data

Administrative data

Endpoint:

exposure-related observations in humans: other data

Remarks:

pharmacokinetics

Type of information:

experimental study

Adequacy of study:

weight of evidence

Reliability:

4 (not assignable)

Rationale for reliability incl. deficiencies:

abstract

Data source

Reference

Reference Type:

publication

Title:

Absolute bioavailability, rate of absorption, and dose proportionality of sulpiride in humans.

Author:

Bressolle F

Year:

1992

Bibliographic source:

J. Pharm. Sci. 1992; 81: 26-32, (REF 29).

Materials and methods

Endpoint addressed:

basic toxicokinetics

Test guideline

Qualifier:

no guideline followed

GLP compliance:

not specified

Test material

Test material information

Constituent 1

Reference substance name:

Sulpiride

EC Number:

239-753-7

EC Name:

Sulpiride

Cas Number:

15676-16-1

Molecular formula:

C15H23N3O4S

IUPAC Name:

sulpiride

Specific details on test material used for the study:

Sulpiride and sulpiride HCl are expected to be similar for this endpoint.

Method

Ethical approval:

not specified

Exposure assessment:

measured

Details on exposure:

12 healthy subjects received an oral solution of 200 mg drug and an intravenous (IV) and intramuscular (IM) dose of 100 mg drug, in 6 healthy subjects who received an oral capsule of 200, 300, and 400 mg drug, and an IV injection of 100 mg drug, and in 8 healthy male subjects who received an oral capsule and IM dose of 200 mg drug.

Results and discussion

Results:

Drug disposition was best described by a 2-compartment model, with absorption appearing to occur by 2 sequential zero-order processes. The fraction of dose absorbed after oral administration was about 30%, based on plasma and urine data. After the 200 mg dose, mean elimination half-life was 7 h and mean residence time was 8.4 h. For each subject total clearance, corrected for the fraction absorbed, and renal clearance were similar. The dose proportionality study demonstrated linear disposition kinetics.

Applicant's summary and conclusion

Conclusions:

The dose absorbed after oral administration was about 30%. After the 200 mg dose, mean elimination half-life was 7 h and mean residence time was 8.4 h.

Executive summary:

12 Healthy subjects received an oral solution of 200 mg drug and an intravenous (IV) and intramuscular (IM) dose of 100 mg drug, in 6 healthy subjects who received an oral capsule of 200, 300, and 400 mg drug, and an IV injection of 100 mg drug, and in 8 healthy male subjects who received an oral capsule and IM dose of 200 mg drug.

Drug disposition was best described by a 2-compartment model, with absorption appearing to occur by 2 sequential zero-order processes. The fraction of dose absorbed after oral administration was about 30%, based on plasma and urine data. After the 200 mg dose, mean elimination half-life was 7 h and mean residence time was 8.4 h. For each subject total clearance, corrected for the fraction absorbed, and renal clearance were similar. The dose proportionality study demonstrated linear disposition kinetics.