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Pharmacokinetic Study of Levosulpiride

Phase 1
Completed
Conditions
Dyspepsia
Interventions
Registration Number
NCT02481583
Lead Sponsor
Wuhan Union Hospital, China
Brief Summary

The aim of this study was to characterise the pharmacokinetic properties and assess the safety of different formulations of levosulpiride in healthy Chinese volunteers.

Detailed Description

Levosulpiride was administered to 42 healthy male and female (1:1) subjects as tablet (orally) and injection (intramuscularly and intravenously) formulations. Blood samples were collected at regular intervals after single and multiple drug administration. The concentration of levosulpiride in plasma was determined using a validated high performance liquid chromatography-tandem mass spectrometry method. Non-compartmental analysis was performed to estimate pharmacokinetic parameters. The analysis of variance was used to test for linearity and assess the effect of gender on the pharmacokinetic properties of the study drug. Adverse effects were monitored using investigators' questionnaires and subjects' spontaneous reports, vital sign measurements, hematology, clinical chemistry, and electrocardiogram.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
42
Inclusion Criteria
  • body mass index between19 and 24 kg/m2
  • negative for HIV and hepatitis B
  • had no clinical important findings on health tests
  • thorax radiography and ECG with no abnormalities
  • normal blood pressure values
  • heart rate
Exclusion Criteria
  • any drug treatment within 2 weeks before starting the study
  • participation in another clinical study within the previous 3 months
  • alcoholism and smoking
  • pregnancy
  • breast-feeding
  • hypocalcemia
  • blood donation or participation in other clinical trials within 3 months before enrollment in the study
  • sitting blood pressure <80/50 mm Hg or >140/100 mm Hg
  • A ventricular rate <60 beats/min or >100 beats/min at rest

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
part 2Levosulpiride30 subjects were randomly assigned to 1 of 3 treatment groups (25, 50, or 75 mg) via i.m. administration, the 50-mg group subjects also received levosulpiride by i.v. route and repeated administration by i.m. route (twice a day for 3 days).
part 1Levosulpiride12 subjects successively received a single dose of levosulpiride tablets 25, 50, or 100 mg via oral administration and 50-mg of levosulpiride tablets 3 times a day for 7 days.
Primary Outcome Measures
NameTimeMethod
Cmaxtwo days

Peak concentration

Area under the curve-AUCtwo days

Area under the curve - plasma concentration

Clearance-CLtwo days

Clearance

Apparent volume of distribution-Vtwo days

The apparent volume of distribution

Secondary Outcome Measures
NameTimeMethod
Safety (adverse events)one month

adverse events

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