NCT01447563

Comparative Bioavailability Study of Two Oral Formulations of Clopidogrel

Bioavailability of Two Oral Formulations of Clopidogrel: A Randomized, Open Label, Single Dose, Two-Period, Crossover Comparison in Healthy Mexican Volunteers

• Status: Terminated
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 32 (actual)
• Sponsor: Hospital Universitario Dr. Jose E. Gonzalez · Academic / Other
• Sex: All
• Age: 18 Years – 40 Years
• Healthy volunteers: Accepted

Summary

Background: Clopidogrel, a potent inhibitor of adenosine diphosphate-induced platelet activation, is widely used to prevent and reduce the risk of thrombotic events. Objective: the aim of the present study is to evaluate the bioequivalence of two oral formulations of 75 mg clopidogrel tablets. Method: The study is an open, randomized, single-dose, two-period crossover trial conducted on 32 healthy Mexican volunteers in a fasted state. A single oral dose of the test or reference drug will be followed by a 7 day washout period, after which subjects will receive the alternative formulation. Blood samples were collected up to 24 h after dosing. In order to determine bioequivalence, the plasma concentrations of clopidogrel carboxylic acid metabolite was determined using high-performance liquid chromatography-tandem mass spectrometry area under the plasma concentration time curve from zero to the last quantifiable level (AUC0-t), area under the plasma concentration time curve extrapolated to infinity (AUC0-∞), maximum plasma concentration (Cmax), the plasma elimination half-life (Tmax) and plasma half-life (T1/2) were calculated for both formulations.

Detailed description

Study procedure In each period, the subjects arrived at the clinical/unit site on the day before the commencement of the study and were randomized using Excel® 2007 to receive the test formulation followed by the reference formulation, or viceversa. No food was allowed from 10 h before until at least 4 h after drug administration. On the subsequent morning, a peripheral venous 21G catheter was inserted in the antecubital vein of the subjects and blood samples were collected (zero time). The subjects then received a single 75 mg tablet of either the test or the reference formulation, given with 250 mL water. Blood samples were collected at 0.16, 0.33, 0.5, 0.66, 0.83, 1, 1.5, 1.75, 2, 2.5, 3, 6, 8, 12, 16 and 24 h after drug administration. The blood samples were collected in coded EDTA tubes and plasma was obtained by centrifugation (2,053 g for 10 min at 5 C), after which the plasma was immediately transferred to prelabeled vials and stored at or below -70 After a week of washout, the alternative formulation was administered to the subjects and samples were drawn and analyzed as before.

Conditions

• Comparative Bioavailability of Clopidogrel Tablets

Interventions

Type	Name	Description
DRUG	Clopidogrel bisulfate	subjects received a single 75 mg tablet of the reference formulation, given with 250 mL water
DRUG	Clopidogrel	subjects received a single 75 mg tablet of the test formulation, given with 250 mL water

Timeline

• Start date: 2008-05-01
• Primary completion: 2008-06-01
• Completion: 2008-08-01
• First posted: 2011-10-06
• Last updated: 2011-10-06

Locations

1 site across 1 country: Mexico