Pharmacokinetic Study of Levosulpiride

Tolerability and Pharmacokinetic Comparison of Oral, Intramuscular and Intravenous Administration of Levosulpiride After Single and Multiple Doses in Fasting Healthy Chinese Volunteers

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

Study Overview

• Status: Completed
• Conditions: Dyspepsia
• Intervention / Treatment: Drug: Levosulpiride

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.

• Study Type: Interventional
• Enrollment (Actual): 42
• Phase: Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 19 years to 45 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

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 Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Randomized
• Interventional Model: Parallel Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: part 1; 12 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.	Drug: Levosulpiride; different formulations of levosulpiride
Experimental: part 2; 30 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).	Drug: Levosulpiride; different formulations of levosulpiride

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Cmax	Peak concentration	two days
Area under the curve-AUC	Area under the curve - plasma concentration	two days
Clearance-CL	Clearance	two days
Apparent volume of distribution-V	The apparent volume of distribution	two days

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Safety (adverse events)	adverse events	one month

Collaborators and Investigators

• Sponsor: Wuhan Union Hospital, China
• Investigators: Principal Investigator: Weiyong Li, HUST/Union Hospital

Publications and helpful links

General Publications

• Xu M, Zhou Y, Ni Y, He X, Li H, Sattar H, Chen H, Li W. Tolerability and Pharmacokinetic Comparison of Oral, Intramuscular, and Intravenous Administration of Levosulpiride After Single and Multiple Dosing in Healthy Chinese Volunteers. Clin Ther. 2015 Nov 1;37(11):2458-67. doi: 10.1016/j.clinthera.2015.08.024. Epub 2015 Sep 26.

Study record dates

Study Major Dates

• Study Start: March 1, 2013
• Primary Completion (Actual): May 1, 2013
• Study Completion (Actual): May 1, 2013

Study Registration Dates

• First Submitted: May 9, 2015
• First Submitted That Met QC Criteria: June 24, 2015
• First Posted (Estimate): June 25, 2015

Study Record Updates

• Last Update Posted (Estimate): June 25, 2015
• Last Update Submitted That Met QC Criteria: June 24, 2015
• Last Verified: June 1, 2015

More Information

Terms related to this study

• Keywords: pharmacokinetics; bioavailability; adverse effects; levosulpiride
• Additional Relevant MeSH Terms: Signs and Symptoms, Digestive; Dyspepsia
• Other Study ID Numbers: WHXH-Levosul