The objective of this study is to investigate the possible effect of multiple oral doses of 25 mg BI 10773 on the steady state pharmacokinetics of ethinylestradiol (EE) and levonogestrel (LNG) (Microgynon®).
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
18
1245.41.1 Boehringer Ingelheim Investigational Site
Biberach, Germany
Ethinylestradiol: Area Under the Curve at Steady State Over the Uniform Dosing Interval τ (AUCτ,ss)
Area under the concentration-time curve of ethinylestradiol in plasma at steady state over the uniform dosing interval τ.
Time frame: Pre-dose, 30 min, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, and 24h after administration of Microgynon on Days 14 and 21. In addition, pre-dose samples were collected on Days 12, 13, 19, and 20.
Levonorgestrel: Area Under the Curve at Steady State Over the Uniform Dosing Interval τ (AUCτ,ss)
Area under the concentration-time curve of levonorgestrel in plasma at steady state over the uniform dosing interval τ.
Time frame: Pre-dose, 30 min, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, and 24h after administration of Microgynon on Days 14 and 21. In addition, pre-dose samples were collected on Days 12, 13, 19, and 20.
Ethinylestradiol: Maximum Measured Concentration (Cmax,ss)
Maximum measured concentration of ethinylestradiol in plasma at steady state over the uniform dosing interval τ.
Time frame: Pre-dose, 30 min, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, and 24h after administration of Microgynon on Days 14 and 21. In addition, pre-dose samples were collected on Days 12, 13, 19, and 20.
Levonorgestrel: Maximum Measured Concentration (Cmax,ss)
Maximum measured concentration of levonorgestrel in plasma at steady state over the uniform dosing interval τ.
Time frame: Pre-dose, 30 min, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, and 24h after administration of Microgynon on Days 14 and 21. In addition, pre-dose samples were collected on Days 12, 13, 19, and 20.
Ethinylestradiol: Time From Last Dosing to Maximum Measured Concentration (Tmax,ss)
Time from last dosing to the maximum measured concentration of ethinylestradiol in plasma at steady state
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multiple doses BI 10773
multiple doses
Time frame: Pre-dose, 30 min, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, and 24h after administration of Microgynon on Days 14 and 21. In addition, pre-dose samples were collected on Days 12, 13, 19, and 20.
Levonorgestrel: Time From Last Dosing to Maximum Measured Concentration (Tmax,ss)
Time from last dosing to the maximum measured concentration of levonorgestrel in plasma at steady state
Time frame: Pre-dose, 30 min, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, and 24h after administration of Microgynon on Days 14 and 21. In addition, pre-dose samples were collected on Days 12, 13, 19, and 20.
Ethinylestradiol: Apparent Clearance at Steady State (CL/Fss)
Apparent clearance of ethinylestradiol in the plasma at steady state after oral administration
Time frame: Pre-dose, 30 min, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, and 24h after administration of Microgynon on Days 14 and 21. In addition, pre-dose samples were collected on Days 12, 13, 19, and 20.
Levonorgestrel: Apparent Clearance at Steady State (CL/Fss)
Apparent clearance of levonorgestrel in the plasma at steady state after oral administration
Time frame: Pre-dose, 30 min, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, and 24h after administration of Microgynon on Days 14 and 21. In addition, pre-dose samples were collected on Days 12, 13, 19, and 20.
Ethinylestradiol: Apparent Volume of Distribution During the Terminal Phase at Steady State (Vz/Fss)
Apparent volume of distribution during the terminal phase at steady state after oral administration
Time frame: Pre-dose, 30 min, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, and 24h after administration of Microgynon on Days 14 and 21. In addition, pre-dose samples were collected on Days 12, 13, 19, and 20.
Levonorgestrel: Apparent Volume of Distribution During the Terminal Phase at Steady State (Vz/Fss)
Apparent volume of distribution during the terminal phase at steady state after oral administration
Time frame: Pre-dose, 30 min, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, and 24h after administration of Microgynon on Days 14 and 21. In addition, pre-dose samples were collected on Days 12, 13, 19, and 20.
Ethinylestradiol: Terminal Half-life at Steady State (t1/2,ss)
Terminal half-life of ethinylestradiol in plasma at steady state
Time frame: Pre-dose, 30 min, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, and 24h after administration of Microgynon on Days 14 and 21. In addition, pre-dose samples were collected on Days 12, 13, 19, and 20.
Levonorgestrel: Terminal Half-life at Steady State (t1/2,ss)
Terminal half-life of levonorgestrel in plasma at steady state
Time frame: Pre-dose, 30 min, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, and 24h after administration of Microgynon on Days 14 and 21. In addition, pre-dose samples were collected on Days 12, 13, 19, and 20.
Ethinylestradiol: Terminal Rate Constant at Steady State (λz,ss)
Terminal rate constant of ethinylestradiol in plasma at steady state
Time frame: Pre-dose, 30 min, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, and 24h after administration of Microgynon on Days 14 and 21. In addition, pre-dose samples were collected on Days 12, 13, 19, and 20.
Levonorgestrel: Terminal Rate Constant at Steady State (λz,ss)
Terminal rate constant of levonorgestrel in plasma at steady state
Time frame: Pre-dose, 30 min, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, and 24h after administration of Microgynon on Days 14 and 21. In addition, pre-dose samples were collected on Days 12, 13, 19, and 20.
Ethinylestradiol: Mean Residence Time at Steady State (MRTpo,ss)
Mean residence time of ethinylestradiol in the body at steady state after oral administration
Time frame: Pre-dose, 30 min, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, and 24h after administration of Microgynon on Days 14 and 21. In addition, pre-dose samples were collected on Days 12, 13, 19, and 20.
Levonorgestrel: Mean Residence Time at Steady State (MRTpo,ss)
Mean residence time of levonorgestrel in the body at steady state after oral administration
Time frame: Pre-dose, 30 min, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, and 24h after administration of Microgynon on Days 14 and 21. In addition, pre-dose samples were collected on Days 12, 13, 19, and 20.
Number of Participants With Clinically Relevant Abnormalities in Physical Examination, Vital Signs, ECG and Clinical Laboratory Tests.
Number of participants with clinically relevant abnormalities in physical examination, vital signs and clinical laboratory tests. Relevant findings or worsenings of baseline conditions were reported as adverse events.
Time frame: Day 1 to day 17
Assessment of Tolerability
Tolerability will be assessed by the investigator according to the categories good, satisfactory, not satisfactory, bad and not assessable.
Time frame: Within Day 24 to Day 31