This single-center, open-label, randomized, balanced, single-dose, two-treatment, two-period, two-sequence crossover study was conducted under medical supervision in 28 healthy female volunteers.
Food effect bioavailability studies are usually conducted for new drugs and drug products to assess the effect of food on the rate and extent of absorption of a drug when the drug product is administered shortly after a meal (fed conditions), as compared to administration under fasting conditions. Therefore, this study was designed to characterize the effect of a high fat meal on the bioavailability of E4 and DRSP after administration of a single tablet containing 15 mg E4 and 3 mg DRSP. All subjects entered the study site at least 12 hours before each dosing and fasted for at least 10 hours prior to each dose. All subjects were to receive both Treatment A (Reference; a single 15 mg E4/3 mg DRSP tablet without food (fasted)) and Treatment B (Test; a single 15 mg E4/3 mg DRSP tablet with food (fed)) either at the first treatment period (Period 1) or the second treatment period (Period 2). Approximately half of the subjects were randomized to receive either Treatment A followed by Treatment B (Sequence AB), or Treatment B followed by Treatment A (Sequence BA).
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Masking
NONE
Enrollment
28
All subjects received both Treatment A and Treatment B either at the first treatment period (Period 1) or the second treatment period (Period 2). Approximately half of the subjects was randomized to receive either Treatment A followed by Treatment B (Sequence AB), or Treatment B followed by Treatment A (Sequence BA)
Maximum concentration (Cmax) of estetrol in plasma
PK sampling
Time frame: From day 1 to 4 during both period 1 and period 2
Cmax of drospirenone in plasma
PK sampling
Time frame: From day 1 to 4 during both period 1 and period 2
Area under the plasma concentration versus time curve from time 0 to the last determined concentration (AUC0-tdlc) of estetrol
Time frame: From day 1 to 4 during both period 1 and period 2
AUC0-tdlc of drospirenone
Time frame: From day 1 to 4 during both period 1 and period 2
AUC0-inf of estetrol
PK sampling
Time frame: Day 1 to 4 during both period 1 and period 2
AUC0-inf of drospirenone
PK sampling
Time frame: Day 1 to 4 during both period 1 and period 2
Number of subjects with adverse events as a measure of safety and tolerability
Time frame: From up to day 28 before randomization (28 day screening/run-in period) to day 4 of the Period 2
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