Healthy Participants
Conditions
Keywords
Drug Therapy
Brief summary
The purpose of this study is to determine the bioequivalence of esomeprazole 40 milligram (mg) tablets and capsules.
Detailed description
The drug being tested in this study is called esomeprazole. Esomeprazole is being tested in healthy participants in order to evaluate the bioequivalence between a single oral dose of esomeprazole tablet and capsule. The study will enroll 52 participants. Participants will be randomly assigned (by chance, like flipping a coin) to one of the two treatment sequences: * Esomeprazole 40 mg capsule + Esomeprazole 40 mg tablet * Esomeprazole 40 mg tablet + Esomeprazole 40 mg capsule All participants will be asked to take one capsule or tablet on Day 1 of each Intervention Period based on the treatment sequence to which the participant has been assigned. This single center trial will be conducted in the United States. The overall duration to participate in this study is 36 days. Participants will visit the clinic on Day -1 and remained confined until Day 1 of Intervention Period 1 and 2. A washout period of minimum 6 days will be maintained between the dose in each Intervention Period.
Interventions
DRUGEsomeprazole Capsule
Esomeprazole Capsule
DRUGEsomeprazole Tablet
Esomeprazole Tablet
Sponsors
Takeda
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
OTHER
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
1. Is a healthy adult male or female participant. 2. Is aged 18 to 55 years, inclusive, at the time of informed consent and first study medication dose. 3. Weighs at least 50 kilogram (kg) and has a body mass index (BMI) from 18.5 to 30 kilogram per square meter (kg/m\^2), inclusive at Screening and Day -1.
Exclusion criteria
1. Has uncontrolled, clinically significant neurologic, cardiovascular, pulmonary, hepatic, renal, metabolic, gastrointestinal, or endocrine disease or other abnormality, which may impact the ability of the participant to participate or potentially confound the study results. It is the responsibility of the investigator to assess the clinical significance; however, consultation with the Takeda Medical Monitor may be warranted. 2. Has a history of significant gastro intestinal (GI) disorders manifested with persistent, chronic or intermittent nausea, vomiting, diarrhea, or has a current or recent (within 6 months) GI disease that would influence the absorption of drugs (example, a history of malabsorption, severe esophageal reflux, peptic ulcer disease or erosive esophagitis), or any gastrointestinal-related surgical intervention.. 3. Has a known hypersensitivity to any component of the formulation of esomeprazole capsules or tablets or compounds with the same mechanism of action (dexlansoprazole, lansoprazole, omeprazole, rabeprazole, pantoprazole), or related compounds.
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Esomeprazole | Day 1 pre-dose and at multiple time points (up to 10 hours) post-dose |
| AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for Esomeprazole | Day 1 pre-dose and at multiple time points (up to 10 hours) post-dose |
| Cmax: Maximum Observed Plasma Concentration for Esomeprazole | Day 1 pre-dose and at multiple time points (up to 10 hours) post-dose |
Countries
United States
Participant flow
Recruitment details
Participants took part in the study at 1 investigative site in the United States from 27 March 2017 to 13 May 2017.
Pre-assignment details
Healthy participants were enrolled in this 2-way crossover study and randomized in 1 of the 2 treatment sequences to receive esomeprazole 40 milligram (mg) capsule (Regimen A) or esomeprazole 40 mg tablet (Regimen B) under fasted conditions.
Participants by arm
| Arm | Count |
|---|---|
| Regimen A + Regimen B Esomeprazole 40 mg, capsule, orally, once under fasted conditions on Day 1 of Intervention Period 1, followed by at least 6 days of washout period, further followed by esomeprazole 40 mg, tablet, orally, once under fasted conditions on Day 1 of Intervention Period 2. | 26 |
| Regimen B + Regimen A Esomeprazole 40 mg, tablet, orally, once under fasted conditions on Day 1 of Intervention Period 1, followed by at least 6 days of washout period, further followed by esomeprazole 40 mg, capsule, orally, once under fasted conditions on Day 1 of Intervention Period 2. | 26 |
| Total | 52 |
Withdrawals & dropouts
| Period | Reason | FG000 | FG001 |
|---|---|---|---|
| Washout Period (at Least 6 Days) | Lost to Follow-up | 1 | 0 |
| Washout Period (at Least 6 Days) | Pregnancy | 0 | 1 |
Baseline characteristics
| Characteristic | Regimen B + Regimen A | Regimen A + Regimen B | Total |
|---|---|---|---|
| Age, Continuous | 33.3 years STANDARD_DEVIATION 7.83 | 32.4 years STANDARD_DEVIATION 9.64 | 32.8 years STANDARD_DEVIATION 8.71 |
| Body Mass Index (BMI) | 25.7 kilogram per square meter (kg/m^2) STANDARD_DEVIATION 2.89 | 24.3 kilogram per square meter (kg/m^2) STANDARD_DEVIATION 2.77 | 25.0 kilogram per square meter (kg/m^2) STANDARD_DEVIATION 2.89 |
| Height | 170.7 centimeter STANDARD_DEVIATION 10.95 | 173.4 centimeter STANDARD_DEVIATION 10.36 | 172.0 centimeter STANDARD_DEVIATION 10.65 |
| Race (NIH/OMB) American Indian or Alaska Native | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Asian | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Black or African American | 11 Participants | 8 Participants | 19 Participants |
| Race (NIH/OMB) More than one race | 2 Participants | 0 Participants | 2 Participants |
| Race (NIH/OMB) Native Hawaiian or Other Pacific Islander | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Unknown or Not Reported | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) White | 13 Participants | 18 Participants | 31 Participants |
| Region of Enrollment United States | 26 Participants | 26 Participants | 52 Participants |
| Sex: Female, Male Female | 11 Participants | 9 Participants | 20 Participants |
| Sex: Female, Male Male | 15 Participants | 17 Participants | 32 Participants |
| Smoking Status Ex-smoker | 2 Participants | 8 Participants | 10 Participants |
| Smoking Status Never smoked | 24 Participants | 18 Participants | 42 Participants |
| Weight | 75.3 kilogram STANDARD_DEVIATION 13.37 | 73.3 kilogram STANDARD_DEVIATION 12.83 | 74.3 kilogram STANDARD_DEVIATION 13.01 |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk |
|---|---|---|
| deaths Total, all-cause mortality | 0 / 51 | 0 / 51 |
| other Total, other adverse events | 4 / 51 | 3 / 51 |
| serious Total, serious adverse events | 0 / 51 | 0 / 51 |
Outcome results
Primary
AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Esomeprazole
Time frame: Day 1 pre-dose and at multiple time points (up to 10 hours) post-dose
Population: The pharmacokinetic (PK) set included all participants who received at least 1 dose of study drug and had at least 1 measurable plasma concentration of study drug. The PK set where data at specified timepoints was available for all participants who received at least one dose of Regimen A and Regimen B.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Regimen A | AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Esomeprazole | 1908.0 hour*nanogram per milliliter (h*ng/mL) | Geometric Coefficient of Variation 66 |
| Regimen B | AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Esomeprazole | 1922.2 hour*nanogram per milliliter (h*ng/mL) | Geometric Coefficient of Variation 57.9 |
90% CI: [0.969, 1.07]
Primary
AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for Esomeprazole
Time frame: Day 1 pre-dose and at multiple time points (up to 10 hours) post-dose
Population: The PK set included all participants who received at least 1 dose of study drug and had at least 1 measurable plasma concentration of study drug. The PK set where data at specified timepoints was available for all participants who received at least one dose of Regimen A and Regimen B.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Regimen A | AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for Esomeprazole | 1884.6 h*ng/mL | Geometric Coefficient of Variation 64.3 |
| Regimen B | AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for Esomeprazole | 1882.6 h*ng/mL | Geometric Coefficient of Variation 57.5 |
90% CI: [0.939, 1.05]
Primary
Cmax: Maximum Observed Plasma Concentration for Esomeprazole
Time frame: Day 1 pre-dose and at multiple time points (up to 10 hours) post-dose
Population: The PK set included all participants who received at least 1 dose of study drug and had at least 1 measurable plasma concentration of study drug. The PK set where data at specified timepoints was available for all participants who received at least one dose of Regimen A and Regimen B.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Regimen A | Cmax: Maximum Observed Plasma Concentration for Esomeprazole | 933.29 nanogram per milliliter (ng/mL) | Geometric Coefficient of Variation 44.5 |
| Regimen B | Cmax: Maximum Observed Plasma Concentration for Esomeprazole | 872.38 nanogram per milliliter (ng/mL) | Geometric Coefficient of Variation 43.5 |
90% CI: [0.88, 1.009]