Bioequivalence of Pramipexole Extended Release (PPX ER) 1.5mg x 1 Tablet Once Daily (q.d.) vs. PPX ER 0.375mg x 4 Tablets Under Fasted and Fed Conditions in Japanese Healthy Volunteers

A Multiple Dose Study With Increasing Dose for Pramipexole Extended Release (ER) Tablet (0.375 mg q.d. to 1.5 mg q.d.) in Two-way Cross-over Comparison to Investigate the Bioequivalence of 1.5 mg ER x 1 Tablet q.d. Versus 0.375 mg ER x 4 Tablets q.d. Under Fasted and Fed Conditions in Japanese Healthy Male Volunteers

Bioequivalence between PPX ER 1.5 mg x 1 tablet q.d. and 0.375 mg PPX ER x 4 tablets q.d. under fasted and fed conditions Food effect of 1.5 mg ER x 1 tablet q.d.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: PPX ER

• Study Type: Interventional
• Enrollment (Actual): 28
• Phase: Phase 1

Contacts and Locations

Study Locations

• Japan
  • Sumida-ku, Tokyo, Japan
    • 248.677.001 Boehringer Ingelheim Investigational Site

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 20 years to 40 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion criteria:

• Japanese healthy male
• 20 to 40 years of age
• body mass index (BMI) between 17.6 and 26.4 kg/m2 (BMI calculation: weight in kilograms divided by the square of height in meters)

Exclusion criteria:

1. Any clinical relevance findings of the medical examination as follows

   1. Blood pressure (systolic blood pressure is lower than 110 mmHg and diastolic blood pressure is lower than 60 mmHg at the screening in either a supine or a sitting position),
   2. pulse rate,
   3. electrocardiogram [ECG]
   4. laboratory test parameters) of clinical relevance
2. Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
3. Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
4. History of orthostatic hypotension, fainting spells or blackouts
5. Chronic or acute infections

Study Plan

How is the study designed?

Design Details

• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Other: Treatment sequence A; V4: PPX ER 1.5mg x 1 fed, V5: PPX ER 0.375mg x 4 fed, V6:: PPX ER 1.5mg x 1 fasted, V5: PPX ER 0.375mg x 4 fasted	Drug: PPX ER; PPX ER 0.375mg - 1.5mg for 32 days totally
Other: Treatment sequence B; V4: PPX ER 0.375mg x 4 fed, V5: PPX ER 1.5mg x 1 fed, V6:: PPX ER 0.375mg x 4 fasted, V5: PPX ER 1.5mg x 1 fasted	Drug: PPX ER; PPX ER 0.375mg - 1.5mg for 32 days totally

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
AUCτ,ss (Fed Conditions)	Area under the concentration-time curve of the analyte in plasma at steady state over a uniform dosing interval τ	Serial pharmacokinetic blood samples collected before drug administration, 1, 2, 2.5, 3, 4, 6, 8, 10, 12, and 23.833 hours after drug administration
Cmax,ss (Fed Conditions)	maximum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ	Serial pharmacokinetic blood samples collected before drug administration, 1, 2, 2.5, 3, 4, 6, 8, 10, 12, and 23.833 hours after drug administration
AUCτ,ss (Fasted Conditions)	Area under the concentration-time curve of the analyte in plasma at steady state over a uniform dosing interval τ	Serial pharmacokinetic blood samples collected before drug administration, 1, 2, 2.5, 3, 4, 6, 8, 10, 12, and 23.833 hours after drug administration
Cmax,ss (Fasted Conditions)	maximum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ	Serial pharmacokinetic blood samples collected before drug administration, 1, 2, 2.5, 3, 4, 6, 8, 10, 12, and 23.833 hours after drug administration

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Cτ,ss (Fed Conditions)	Concentration of the analyte in plasma at time τ at steady state	pharmacokinetic blood samples collected at τ (23.833 hours) after drug administration
Cmin,ss (Fed Conditions)	Minimum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ	Serial pharmacokinetic blood samples collected before drug administration, 1, 2, 2.5, 3, 4, 6, 8, 10, 12, and 23.833 hours after drug administration
Tmax,ss (Fed Conditions)	Time from dosing to the maximum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ	Serial pharmacokinetic blood samples collected before drug administration, 1, 2, 2.5, 3, 4, 6, 8, 10, 12, and 23.833 hours after drug administration
λz,ss (Fed Conditions)	Terminal rate constant of the analyte in plasma at steady state	Serial pharmacokinetic blood samples collected before drug administration, 1, 2, 2.5, 3, 4, 6, 8, 10, 12, and 23.833 hours after drug administration
t1/2,ss (Fed Conditions)	Terminal half-life of the analyte in plasma at steady state	Serial pharmacokinetic blood samples collected before drug administration, 1, 2, 2.5, 3, 4, 6, 8, 10, 12, and 23.833 hours after drug administration
MRTpo,ss (Fed Conditions)	Mean residence time of the analyte in the body at steady state after oral administration	Serial pharmacokinetic blood samples collected before drug administration, 1, 2, 2.5, 3, 4, 6, 8, 10, 12, and 23.833 hours after drug administration
Cτ,ss (Fasted Conditions)	Concentration of the analyte in plasma at time τ at steady state	pharmacokinetic blood samples collected at τ (23.833 hours) after drug administration
Cmin,ss (Fasted Conditions)	Minimum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ	Serial pharmacokinetic blood samples collected before drug administration, 1, 2, 2.5, 3, 4, 6, 8, 10, 12, and 23.833 hours after drug administration
Tmax,ss (Fasted Conditions)	Time from dosing to the maximum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ	Serial pharmacokinetic blood samples collected before drug administration, 1, 2, 2.5, 3, 4, 6, 8, 10, 12, and 23.833 hours after drug administration
λz,ss (Fasted Conditions)	Terminal rate constant of the analyte in plasma at steady state	Serial pharmacokinetic blood samples collected before drug administration, 1, 2, 2.5, 3, 4, 6, 8, 10, 12, and 23.833 hours after drug administration
t1/2,ss (Fasted Conditions)	Terminal half-life of the analyte in plasma at steady state	Serial pharmacokinetic blood samples collected before drug administration, 1, 2, 2.5, 3, 4, 6, 8, 10, 12, and 23.833 hours after drug administration
MRTpo,ss (Fasted Conditions)	Mean residence time of the analyte in the body at steady state after oral administration	Serial pharmacokinetic blood samples collected before drug administration, 1, 2, 2.5, 3, 4, 6, 8, 10, 12, and 23.833 hours after drug administration

Collaborators and Investigators

• Sponsor: Boehringer Ingelheim

Publications and helpful links

Helpful Links

• Related Info

Study record dates

Study Major Dates

• Study Start: April 1, 2010
• Primary Completion (Actual): June 1, 2010

Study Registration Dates

• First Submitted: May 5, 2010
• First Submitted That Met QC Criteria: May 6, 2010
• First Posted (Estimate): May 7, 2010

Study Record Updates

• Last Update Posted (Estimate): June 9, 2014
• Last Update Submitted That Met QC Criteria: June 3, 2014
• Last Verified: May 1, 2014

More Information

Terms related to this study

• Other Study ID Numbers: 248.677