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

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT01119443

Enrollment

Registered

2010-05-07

Start date

2010-04-30

Completion date

Unknown

Last updated

2014-06-09

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy

Brief summary

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.

Interventions

DRUGPPX ER

PPX ER 0.375mg - 1.5mg for 32 days totally

Study design

Allocation

RANDOMIZED

Intervention model

CROSSOVER

Masking

NONE

Eligibility

Sex/Gender

MALE

Age

20 Years to 40 Years

Healthy volunteers

Yes

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

Design outcomes

Primary

Measure	Time frame	Description
AUCτ,ss (Fed Conditions)	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	Area under the concentration-time curve of the analyte in plasma at steady state over a uniform dosing interval τ
Cmax,ss (Fed Conditions)	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	maximum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ
AUCτ,ss (Fasted Conditions)	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	Area under the concentration-time curve of the analyte in plasma at steady state over a uniform dosing interval τ
Cmax,ss (Fasted Conditions)	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	maximum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ

Secondary

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

Countries

Japan

Participant flow

Participants by arm

Arm	Count
Treatment Sequence A 1.5 mg x 1 tablet q.d. fed -\> 0.375 mg x 4 tablets q.d. fed -\> 1.5 mg x 1 tablet q.d. fasted -\> 0.375 mg x 4 tablets q.d. fasted	14
Treatment Sequence B 0.375 mg x 4 tablets q.d. fed -\> 1.5 mg x 1 tablet q.d. fed -\> 0.375 mg x 4 tablets q.d. fasted -\> 1.5 mg x 1 tablet q.d. fasted	14
Total	28

Withdrawals & dropouts

Period	Reason	FG000	FG001
Crossover Period 1 (5 Days)	Adverse Event	0	1

Baseline characteristics

Characteristic	Treatment Sequence A	Treatment Sequence B	Total
Age, Continuous	29.2 years STANDARD_DEVIATION 4.8	29.1 years STANDARD_DEVIATION 5.4	29.1 years STANDARD_DEVIATION 5
Sex: Female, Male Female	0 Participants	0 Participants	0 Participants
Sex: Female, Male Male	14 Participants	14 Participants	28 Participants

Adverse events

Event type	EG000 affected / at risk	EG001 affected / at risk	EG002 affected / at risk
deaths Total, all-cause mortality	— / —	— / —	— / —
other Total, other adverse events	5 / 28	5 / 28	0 / 27
serious Total, serious adverse events	0 / 28	0 / 28	0 / 27

Outcome results

Primary

AUCτ,ss (Fasted Conditions)

Area under the concentration-time curve of the analyte in plasma at steady state over a uniform dosing interval τ

Time frame: 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

Population: One subject who discontinued the study on Day 1 of Visit 4 (the first day of the first crossover period) was excluded from Pharmacokinetic data set

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Pramipexole ER 1.5 mg x 1 Tablet q.d. in Fed	AUCτ,ss (Fasted Conditions)	31.4 ng/mL	Standard Deviation 7.37
Pramipexole ER 0.375 mg x 4 Tablets q.d. in Fed	AUCτ,ss (Fasted Conditions)	33.6 ng/mL	Standard Deviation 5.8

90% CI: [86.9, 100.8]ANOVA

Primary

AUCτ,ss (Fed Conditions)

Area under the concentration-time curve of the analyte in plasma at steady state over a uniform dosing interval τ

Time frame: 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

Population: One subject who discontinued the study on Day 1 of Visit 4 (the first day of the first crossover period) was excluded from Pharmacokinetic data set

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Pramipexole ER 1.5 mg x 1 Tablet q.d. in Fed	AUCτ,ss (Fed Conditions)	33.7 ng·h/mL	Standard Deviation 5.89
Pramipexole ER 0.375 mg x 4 Tablets q.d. in Fed	AUCτ,ss (Fed Conditions)	32.3 ng·h/mL	Standard Deviation 5.89

90% CI: [98.3, 110.3]ANOVA

Primary

Cmax,ss (Fasted Conditions)

maximum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ

Time frame: 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

Population: One subject who discontinued the study on Day 1 of Visit 4 (the first day of the first crossover period) was excluded from Pharmacokinetic data set

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Pramipexole ER 1.5 mg x 1 Tablet q.d. in Fed	Cmax,ss (Fasted Conditions)	2.13 ng/mL	Standard Deviation 0.359
Pramipexole ER 0.375 mg x 4 Tablets q.d. in Fed	Cmax,ss (Fasted Conditions)	2.12 ng/mL	Standard Deviation 0.305

90% CI: [94, 106.7]ANOVA

Primary

Cmax,ss (Fed Conditions)

maximum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ

Time frame: 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

Population: One subject who discontinued the study on Day 1 of Visit 4 (the first day of the first crossover period) was excluded from Pharmacokinetic data set

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Pramipexole ER 1.5 mg x 1 Tablet q.d. in Fed	Cmax,ss (Fed Conditions)	2.24 ng/mL	Standard Deviation 0.29
Pramipexole ER 0.375 mg x 4 Tablets q.d. in Fed	Cmax,ss (Fed Conditions)	2.13 ng/mL	Standard Deviation 0.255

90% CI: [100.1, 109.8]ANOVA

Secondary

Cmin,ss (Fasted Conditions)

Minimum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ

Time frame: 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

Population: One subject who discontinued the study on Day 1 of Visit 4 (the first day of the first crossover period) was excluded from Pharmacokinetic data set

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Pramipexole ER 1.5 mg x 1 Tablet q.d. in Fed	Cmin,ss (Fasted Conditions)	0.654 ng/mL	Standard Deviation 0.342
Pramipexole ER 0.375 mg x 4 Tablets q.d. in Fed	Cmin,ss (Fasted Conditions)	0.757 ng/mL	Standard Deviation 0.283

90% CI: [73.583, 101.854]ANOVA

Secondary

Cmin,ss (Fed Conditions)

Minimum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ

Time frame: 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

Population: One subject who discontinued the study on Day 1 of Visit 4 (the first day of the first crossover period) was excluded from Pharmacokinetic data set

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Pramipexole ER 1.5 mg x 1 Tablet q.d. in Fed	Cmin,ss (Fed Conditions)	0.676 ng/mL	Standard Deviation 0.195
Pramipexole ER 0.375 mg x 4 Tablets q.d. in Fed	Cmin,ss (Fed Conditions)	0.633 ng/mL	Standard Deviation 0.218

90% CI: [93.189, 122.251]ANOVA

Secondary

Cτ,ss (Fasted Conditions)

Concentration of the analyte in plasma at time τ at steady state

Time frame: pharmacokinetic blood samples collected at τ (23.833 hours) after drug administration

Population: One subject who discontinued the study on Day 1 of Visit 4 (the first day of the first crossover period) was excluded from Pharmacokinetic data set

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Pramipexole ER 1.5 mg x 1 Tablet q.d. in Fed	Cτ,ss (Fasted Conditions)	0.654 ng/mL	Standard Error 0.342
Pramipexole ER 0.375 mg x 4 Tablets q.d. in Fed	Cτ,ss (Fasted Conditions)	0.757 ng/mL	Standard Error 0.283

90% CI: [73.583, 101.854]ANOVA

Secondary

Cτ,ss (Fed Conditions)

Concentration of the analyte in plasma at time τ at steady state

Time frame: pharmacokinetic blood samples collected at τ (23.833 hours) after drug administration

Population: One subject who discontinued the study on Day 1 of Visit 4 (the first day of the first crossover period) was excluded from Pharmacokinetic data set

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Pramipexole ER 1.5 mg x 1 Tablet q.d. in Fed	Cτ,ss (Fed Conditions)	0.711 ng/mL	Standard Error 0.184
Pramipexole ER 0.375 mg x 4 Tablets q.d. in Fed	Cτ,ss (Fed Conditions)	0.656 ng/mL	Standard Error 0.217

90% CI: [95.634, 122.676]ANOVA

Secondary

MRTpo,ss (Fasted Conditions)

Mean residence time of the analyte in the body at steady state after oral administration

Time frame: 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

Population: One subject who discontinued the study on Day 1 of Visit 4 (the first day of the first crossover period) was excluded from Pharmacokinetic data set

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Pramipexole ER 1.5 mg x 1 Tablet q.d. in Fed	MRTpo,ss (Fasted Conditions)	21.2 hour	Standard Deviation 13.1
Pramipexole ER 0.375 mg x 4 Tablets q.d. in Fed	MRTpo,ss (Fasted Conditions)	22.9 hour	Standard Deviation 13.7

90% CI: [77.871, 110.185]ANOVA

Secondary

MRTpo,ss (Fed Conditions)

Mean residence time of the analyte in the body at steady state after oral administration

Time frame: 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

Population: One subject who discontinued the study on Day 1 of Visit 4 (the first day of the first crossover period) was excluded from Pharmacokinetic data set

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Pramipexole ER 1.5 mg x 1 Tablet q.d. in Fed	MRTpo,ss (Fed Conditions)	19.1 hour	Standard Deviation 6.08
Pramipexole ER 0.375 mg x 4 Tablets q.d. in Fed	MRTpo,ss (Fed Conditions)	18.4 hour	Standard Deviation 7.6

90% CI: [91.585, 118.263]ANOVA

Secondary

t1/2,ss (Fasted Conditions)

Terminal half-life of the analyte in plasma at steady state

Time frame: 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

Population: One subject who discontinued the study on Day 1 of Visit 4 (the first day of the first crossover period) was excluded from Pharmacokinetic data set

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Pramipexole ER 1.5 mg x 1 Tablet q.d. in Fed	t1/2,ss (Fasted Conditions)	13.3 hour	Standard Deviation 9.82
Pramipexole ER 0.375 mg x 4 Tablets q.d. in Fed	t1/2,ss (Fasted Conditions)	14.6 hour	Standard Deviation 10.8

Secondary

t1/2,ss (Fed Conditions)

Terminal half-life of the analyte in plasma at steady state

Time frame: 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

Population: One subject who discontinued the study on Day 1 of Visit 4 (the first day of the first crossover period) was excluded from Pharmacokinetic data set

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Pramipexole ER 1.5 mg x 1 Tablet q.d. in Fed	t1/2,ss (Fed Conditions)	11.4 hour	Standard Deviation 5.02
Pramipexole ER 0.375 mg x 4 Tablets q.d. in Fed	t1/2,ss (Fed Conditions)	10.8 hour	Standard Deviation 6.01

Secondary

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

Time frame: 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

Population: One subject who discontinued the study on Day 1 of Visit 4 (the first day of the first crossover period) was excluded from Pharmacokinetic data set

Arm	Measure	Value (MEAN)
Pramipexole ER 1.5 mg x 1 Tablet q.d. in Fed	Tmax,ss (Fasted Conditions)	4.24 hour
Pramipexole ER 0.375 mg x 4 Tablets q.d. in Fed	Tmax,ss (Fasted Conditions)	4.28 hour

90% CI: [80.688, 117.45]ANOVA

Secondary

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

Time frame: 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

Population: One subject who discontinued the study on Day 1 of Visit 4 (the first day of the first crossover period) was excluded from Pharmacokinetic data set

Arm	Measure	Value (MEAN)
Pramipexole ER 1.5 mg x 1 Tablet q.d. in Fed	Tmax,ss (Fed Conditions)	5.67 hour
Pramipexole ER 0.375 mg x 4 Tablets q.d. in Fed	Tmax,ss (Fed Conditions)	5.76 hour

90% CI: [84.276, 112.58]ANOVA

Secondary

λz,ss (Fasted Conditions)

Terminal rate constant of the analyte in plasma at steady state

Time frame: 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

Population: One subject who discontinued the study on Day 1 of Visit 4 (the first day of the first crossover period) was excluded from Pharmacokinetic data set

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Pramipexole ER 1.5 mg x 1 Tablet q.d. in Fed	λz,ss (Fasted Conditions)	0.0520 /hour	Standard Deviation 0.0275
Pramipexole ER 0.375 mg x 4 Tablets q.d. in Fed	λz,ss (Fasted Conditions)	0.0474 /hour	Standard Deviation 0.0239

90% CI: [89.571, 133.811]ANOVA

Secondary

λz,ss (Fed Conditions)

Terminal rate constant of the analyte in plasma at steady state

Time frame: 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

Population: One subject who discontinued the study on Day 1 of Visit 4 (the first day of the first crossover period) was excluded from Pharmacokinetic data set

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
Pramipexole ER 1.5 mg x 1 Tablet q.d. in Fed	λz,ss (Fed Conditions)	0.0609 per hour	Standard Deviation 0.017
Pramipexole ER 0.375 mg x 4 Tablets q.d. in Fed	λz,ss (Fed Conditions)	0.0640 per hour	Standard Deviation 0.0169

90% CI: [82.461, 109.698]ANOVA

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026

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

Conditions

Brief summary

Related papers

Interventions

Sponsors

Study design

Eligibility

Inclusion criteria

Exclusion criteria

Design outcomes

Primary

Secondary

Countries

Participant flow

Participants by arm

Withdrawals & dropouts

Baseline characteristics

Adverse events

Outcome results

AUCτ,ss (Fasted Conditions)

AUCτ,ss (Fed Conditions)

Cmax,ss (Fasted Conditions)

Cmax,ss (Fed Conditions)

Cmin,ss (Fasted Conditions)

Cmin,ss (Fed Conditions)

Cτ,ss (Fasted Conditions)

Cτ,ss (Fed Conditions)

MRTpo,ss (Fasted Conditions)

MRTpo,ss (Fed Conditions)

t1/2,ss (Fasted Conditions)

t1/2,ss (Fed Conditions)

Tmax,ss (Fasted Conditions)

Tmax,ss (Fed Conditions)

λz,ss (Fasted Conditions)

λz,ss (Fed Conditions)