A Relative Bioavailability Study Between Two Formulations Of Sildenafil Citrate

A Relative Bioavailability Study Between Two Formulations Of Sildenafil Citrate In Healthy Male Subjects, Fasting Dosing, Being The Test Formulation Sildenafil Citrate 100 Mg CT , And The Reference Formulation Sildenafil Citrate 100 Mg Film-Coated Tablets (Viagra®), Both Formulations Manufactured By Laboratórios Pfizer Ltda.

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT00904748

Acronym

A1481272

Enrollment

Registered

2009-05-20

Start date

2010-01-31

Completion date

2010-03-31

Last updated

2021-02-01

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

Conditions

Erectile Dysfunction

Keywords

Sildenafil, Bio-equivalence

Brief summary

The purpose of this study is to perform a relative bioavailability study between two formulations of sildenafil citrate.

Detailed description

Bio-equivalence between two formulations of sildenafil citrate

Interventions

DRUGsildenafil citrate 100 mg CT

sildenafil citrate 100 mg CT, single dose without water

DRUGViagra®

sildenafil citrate 100 mg film-coated tablet (Viagra®), single dose

Study design

Allocation

RANDOMIZED

Intervention model

CROSSOVER

Primary purpose

OTHER

Masking

NONE

Eligibility

Sex/Gender

MALE

Age

18 Years to 50 Years

Healthy volunteers

Yes

Inclusion criteria

* Body mass index higher or equal to 18,5 and lower or equal than 29,9 kg/m2. * Good health conditions or without significant disease, at medical discretion, according to the rules defined in the Protocol, and evaluations undergone: clinical history, pulse and blood pressure measurements, physical and psychological examination, ECG and complementary laboratory examination. * Able to understand the study nature and objective, including the risks and adverse effects and willing to cooperate with the investigator and act according to all the trial requirements, which is confirmed by signing the Informed Consent Form.

Exclusion criteria

* Hypersensitivity to the study drug or to the chemically related compounds; history of serious adverse reactions or hypersensitivity to any drug. * History or presence of hepatic or gastrointestinal diseases, or other condition that affects the drug absorption, distribution, excretion or metabolism * History of hepatic, renal, lung, gastrointestinal, epileptic, hematological or psychiatric disease; hypo or hypertension of whatever etiology which demands treatment with drugs; history or occurrence of myocardial infarction, angina and/or cardiac failure;

Design outcomes

Primary

Measure	Time frame	Description
Area Under the Curve (AUC 0-t)	Day 1 (Period 1), Day 8 (Period 2), and Day 15 (Period 3): Pre-dose and 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.5, 3, 4, 5, 6, 8, and 12 hours post-dose	Area under the blood concentration-time profile from time zero to last experimentally determined concentration measured in nanograms\hour/milliliter (ng\hr/mL).
Maximum Plasma Concentration (Cmax)	Day 1 (Period 1), Day 8 (Period 2), and Day 15 (Period 3): Pre-dose and 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.5, 3, 4, 5, 6, 8, and 12 hours post-dose	Maximum plasma concentration measured in nanograms per milliliter (ng/mL).

Secondary

Measure	Time frame	Description
Area Under the Curve From 0 to Infinity (AUC 0-inf )	Day 1 (Period 1), Day 8 (Period 2), and Day 15 (Period 3): Pre-dose and 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.5, 3, 4, 5, 6, 8, and 12 hours post-dose	Area under the blood concentration-time profile from time zero extrapolated to infinite time measured in nanograms \hour/milliliter (ng\hr/mL).
Time to Maximum Plasma Concentration (Tmax)	Day 1 (Period 1), Day 8 (Period 2), and Day 15 (Period 3): Pre-dose and 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.5, 3, 4, 5, 6, 8, and 12 hours post-dose	Time at which maximum plasma concentration (Cmax) occurred.
Half-life (T 1/2)	Day 1 (Period 1), Day 8 (Period 2), and Day 15 (Period 3): Pre-dose and 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.5, 3, 4, 5, 6, 8, and 12 hours post-dose	Terminal elimination half-life.
Number of Participants With Clinically Significant Findings in Vital Signs	Day 1 (Period 1), Day 8 (Period 2), and Day 15 (Period 3): Pre-dose and 0.5, 1, 2, 4, 8 and 12 hours post-dose.	Clinically significant abnormalities in blood pressure (BP), pulse, and temperature reported as an adverse event. Clinically significant = values outside the normal range and/or values judged as significant by the investigator (normal range: systolic BP 100-140 mmHg; diastolic BP 60- 90 mmHg; temperature 35-37°Celsius). Pulse rate based on investigator discretion.

Countries

Brazil

Participant flow

Pre-assignment details

Each participant was to receive each of 3 formulations in 3 treatment periods, after being allocated to 1 of 6 treatment sequences. There was to be a minimum interval of 3 days between treatment periods.

Participants by arm

Arm	Count
Entire Study Population Includes all participants who were randomized to any treatment sequence	48
Total	48

Withdrawals & dropouts

Period	Reason	FG000	FG001	FG002	FG003	FG004	FG005
Overall Study	Adverse Event	0	0	0	0	1	0
Overall Study	Withdrawal by Subject	1	1	1	2	0	0

Baseline characteristics

Characteristic	Entire Study Population
Age, Continuous	29.3 years
Sex: Female, Male Female	0 Participants
Sex: Female, Male Male	48 Participants

Adverse events

Event type	EG000 affected / at risk	EG001 affected / at risk	EG002 affected / at risk	EG003 affected / at risk
deaths Total, all-cause mortality	— / —	— / —	— / —	— / —
other Total, other adverse events	3 / 47	3 / 47	3 / 47	18 / 47
serious Total, serious adverse events	0 / 47	0 / 47	0 / 47	0 / 47

Outcome results

Primary

Area Under the Curve (AUC 0-t)

Area under the blood concentration-time profile from time zero to last experimentally determined concentration measured in nanograms\*hour/milliliter (ng\*hr/mL).

Time frame: Day 1 (Period 1), Day 8 (Period 2), and Day 15 (Period 3): Pre-dose and 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.5, 3, 4, 5, 6, 8, and 12 hours post-dose

Population: Participants for pharmacokinetic analysis = participants who completed all of the 3 treatment periods.

Arm	Measure	Value (MEAN)	Dispersion
Test 1: 100 mg Chewable, Without Water	Area Under the Curve (AUC 0-t)	1467.00 ng*hr/mL	Standard Deviation 560.99
Test 2: 100 mg Chewable, With Water	Area Under the Curve (AUC 0-t)	1458.45 ng*hr/mL	Standard Deviation 602.73
Reference: 100 mg Coated, With Water	Area Under the Curve (AUC 0-t)	1493.53 ng*hr/mL	Standard Deviation 615.59

Comparison: Ratio between geometric means of Test 1 study treatment (chewable without water) and reference study treatment (coated with water).90% CI: [92.03, 105.82]ANOVA

Comparison: Ratio between geometric means of Test 2 study treatment (chewable with water) and reference study treatment (coated with water).90% CI: [90.67, 104.26]ANOVA

Primary

Maximum Plasma Concentration (Cmax)

Maximum plasma concentration measured in nanograms per milliliter (ng/mL).

Time frame: Day 1 (Period 1), Day 8 (Period 2), and Day 15 (Period 3): Pre-dose and 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.5, 3, 4, 5, 6, 8, and 12 hours post-dose

Population: Participants for pharmacokinetic analysis = participants who completed all of the 3 treatment periods.

Arm	Measure	Value (MEAN)	Dispersion
Test 1: 100 mg Chewable, Without Water	Maximum Plasma Concentration (Cmax)	439.38 ng/mL	Standard Deviation 198.25
Test 2: 100 mg Chewable, With Water	Maximum Plasma Concentration (Cmax)	434.38 ng/mL	Standard Deviation 211.53
Reference: 100 mg Coated, With Water	Maximum Plasma Concentration (Cmax)	532.31 ng/mL	Standard Deviation 217.32

Comparison: Ratio between geometric means of Test 1 study treatment (chewable without water) and reference study treatment (coated with water).90% CI: [72.38, 90.26]ANOVA

Comparison: Ratio between geometric means of Test 2 study treatment (chewable with water) and reference study treatment (coated with water).90% CI: [70.53, 87.96]ANOVA

Secondary

Area Under the Curve From 0 to Infinity (AUC 0-inf )

Area under the blood concentration-time profile from time zero extrapolated to infinite time measured in nanograms \*hour/milliliter (ng\*hr/mL).

Time frame: Day 1 (Period 1), Day 8 (Period 2), and Day 15 (Period 3): Pre-dose and 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.5, 3, 4, 5, 6, 8, and 12 hours post-dose

Population: Participants for pharmacokinetic analysis = participants who completed all of the 3 treatment periods.

Arm	Measure	Value (MEAN)	Dispersion
Test 1: 100 mg Chewable, Without Water	Area Under the Curve From 0 to Infinity (AUC 0-inf )	1547.92 ng*hr/mL	Standard Deviation 588.48
Test 2: 100 mg Chewable, With Water	Area Under the Curve From 0 to Infinity (AUC 0-inf )	1534.66 ng*hr/mL	Standard Deviation 618.86
Reference: 100 mg Coated, With Water	Area Under the Curve From 0 to Infinity (AUC 0-inf )	1573.81 ng*hr/mL	Standard Deviation 648.32

Comparison: Ratio between geometric means of Test 1 study treatment (chewable without water) and reference study treatment (coated with water).90% CI: [92.76, 105.93]ANOVA

Comparison: Ratio between geometric means of Test 2 study treatment (chewable with water) and reference study treatment (coated with water).90% CI: [91.56, 104.56]ANOVA

Secondary

Half-life (T 1/2)

Terminal elimination half-life.

Time frame: Day 1 (Period 1), Day 8 (Period 2), and Day 15 (Period 3): Pre-dose and 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.5, 3, 4, 5, 6, 8, and 12 hours post-dose

Population: Participants for pharmacokinetic analysis = participants who completed all of the 3 treatment periods.

Arm	Measure	Value (MEAN)	Dispersion
Test 1: 100 mg Chewable, Without Water	Half-life (T 1/2)	2.96 hours	Standard Deviation 0.63
Test 2: 100 mg Chewable, With Water	Half-life (T 1/2)	2.84 hours	Standard Deviation 0.74
Reference: 100 mg Coated, With Water	Half-life (T 1/2)	2.93 hours	Standard Deviation 0.81

Secondary

Number of Participants With Clinically Significant Findings in Vital Signs

Clinically significant abnormalities in blood pressure (BP), pulse, and temperature reported as an adverse event. Clinically significant = values outside the normal range and/or values judged as significant by the investigator (normal range: systolic BP 100-140 mmHg; diastolic BP 60- 90 mmHg; temperature 35-37°Celsius). Pulse rate based on investigator discretion.

Time frame: Day 1 (Period 1), Day 8 (Period 2), and Day 15 (Period 3): Pre-dose and 0.5, 1, 2, 4, 8 and 12 hours post-dose.

Population: Safety population: all subjects who received at least 1 dose of study medication. Although individual listing data for vital signs were collected, summary statistics were not generated for this outcome measure.

Arm	Measure	Value (NUMBER)
Test 1: 100 mg Chewable, Without Water	Number of Participants With Clinically Significant Findings in Vital Signs	0 participants
Test 2: 100 mg Chewable, With Water	Number of Participants With Clinically Significant Findings in Vital Signs	1 participants
Reference: 100 mg Coated, With Water	Number of Participants With Clinically Significant Findings in Vital Signs	0 participants

Secondary

Time to Maximum Plasma Concentration (Tmax)

Time at which maximum plasma concentration (Cmax) occurred.

Time frame: Day 1 (Period 1), Day 8 (Period 2), and Day 15 (Period 3): Pre-dose and 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.5, 3, 4, 5, 6, 8, and 12 hours post-dose

Population: Participants for pharmacokinetic analysis = participants who completed all of the 3 treatment periods.

Arm	Measure	Value (MEAN)	Dispersion
Test 1: 100 mg Chewable, Without Water	Time to Maximum Plasma Concentration (Tmax)	1.46 hours	Standard Deviation 0.81
Test 2: 100 mg Chewable, With Water	Time to Maximum Plasma Concentration (Tmax)	1.29 hours	Standard Deviation 0.71
Reference: 100 mg Coated, With Water	Time to Maximum Plasma Concentration (Tmax)	1.28 hours	Standard Deviation 0.85

Comparison: Difference in Tmax between Test 1 study treatment (chewable without water) and reference study treatment (coated with water).90% CI: [-0.14, 0.5]ANOVA

Comparison: Difference in Tmax between Test 2 study treatment (chewable with water) and reference study treatment (coated with water).90% CI: [-0.27, 0.28]ANOVA

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

A Relative Bioavailability Study Between Two Formulations Of Sildenafil Citrate

Conditions

Keywords

Brief summary

Detailed description

Related papers

Interventions

Sponsors

Study design

Eligibility

Inclusion criteria

Exclusion criteria

Design outcomes

Primary

Secondary

Countries

Participant flow

Pre-assignment details

Participants by arm

Withdrawals & dropouts

Baseline characteristics

Adverse events

Outcome results

Area Under the Curve (AUC 0-t)

Maximum Plasma Concentration (Cmax)

Area Under the Curve From 0 to Infinity (AUC 0-inf )

Half-life (T 1/2)

Number of Participants With Clinically Significant Findings in Vital Signs

Time to Maximum Plasma Concentration (Tmax)