The purpose of this study is to evaluate bioequivalence parameters of esomeprazole capsules 20 mg (test product) vs. esomeprazole capsules 20 mg (reference product) under fasted conditions.
This will be a single center, single dose, single-blind, randomized, two-sequence, two-period crossover, bioequivalence study in healthy adult participants with at least a 7-day washout period. The study will consist of an ambulant screening day within 28 days prior to first product administration and two study periods.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
OTHER
Masking
DOUBLE
Enrollment
61
Esomeprazole 20 mg delayed-release capsules will be given as one capsule once daily as oral administration.
Esomeprazole 20 mg delayed-release capsules (Nexium 24HR) will be given as one capsule once daily as oral administration.
Syneos health
Québec, Canada
Maximum Observed Post Dose Concentration (Cmax)
Cmax is defined as maximum observed post-dose concentration; obtained without interpolation. Blood samples were collected at the indicated time points for the analysis of Cmax. Pharmacokinetic (PK) parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose (within 1 hour prior to dosing), 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.25, 2.5, 2.75, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8,10, 12, 16, and 24 hours post dose in each treatment period (each period is of 2 days)
Area Under the Plasma Concentration Versus Time Curve Calculated From Time 0 to the Last Measurable Sampling Time Point
AUC(0-t) is defined as area under the plasma concentration versus time curve calculated from time 0 to the last measurable sampling time point t, computed using the linear trapezoidal rule. Blood samples were collected at the indicated time points for the analysis of AUC0-t. PK parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose (within 1 hour prior to dosing), 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.25, 2.5, 2.75, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8,10, 12, 16, and 24 hours post dose in each treatment period (each period is of 2 days)
Area Under the Plasma Concentration Versus Time Curve Calculated From Time 0 to Infinity (AUC0-inf)
AUC(0-inf) is defined as area under the plasma concentration versus time curve calculated from time 0 to infinity. AUC0-inf is equal to (=) AUC0-t plus (+) concentration at the last measurable sampling time point \[C(t)\]/terminal elimination rate constant (λz). Blood samples were collected at the indicated time points for the analysis of AUC0-inf. PK parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose (within 1 hour prior to dosing), 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.25, 2.5, 2.75, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8,10, 12, 16, and 24 hours post dose in each treatment period (each period is of 2 days)
Percentage of AUC(0-inf) Obtained by Extrapolation (%AUCex)
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%AUCex is defined as percentage of AUC(0-inf) obtained by extrapolation, calculated as (1-\[AUC{0-t}/AUC{0-inf}\]) ×100. Blood samples were collected at the indicated time points for the analysis of %AUCex. PK parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose (within 1 hour prior to dosing), 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.25, 2.5, 2.75, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8,10, 12, 16, and 24 hours post dose in each treatment period (each period is of 2 days)
Terminal Elimination Rate Constant
λz is defined as terminal elimination rate constant computed as the slope of the regression line of ln (C\[t\]) on time. The regression should generally involve at least 3 consecutive measurable concentrations that decrease over time. Blood samples were collected at the indicated time points for the analysis of λz. PK parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose (within 1 hour prior to dosing), 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.25, 2.5, 2.75, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8,10, 12, 16, and 24 hours post dose in each treatment period (each period is of 2 days)
Time of the Maximum Observed Post-Dose Concentration (Tmax)
Tmax is defined as the time of the maximum observed post-dose concentration. Blood samples were collected at the indicated time points for the analysis of Tmax. PK parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose (within 1 hour prior to dosing), 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.25, 2.5, 2.75, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8,10, 12, 16, and 24 hours post dose in each treatment period (each period is of 2 days)
Elimination Half-Life (T1/2)
T1/2 is defined as elimination half-life computed as T1/2 = ln(2)/ λz. Blood samples were collected at the indicated time points for the analysis of T1/2. PK parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose (within 1 hour prior to dosing), 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.25, 2.5, 2.75, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8,10, 12, 16, and 24 hours post dose in each treatment period (each period is of 2 days)