An Open-label, Two-period, Fixed-sequence Trial to Evaluate the Effect of Multiple Doses of BI 10773 on the Multiple-dose Pharmacokinetics of a Combination of Ethinylestradiol and Levonorgestrel in Healthy Premenopausal Female Volunteers
Overview
- Phase
- Phase 1
- Intervention
- levonorgestrel
- Conditions
- Healthy
- Sponsor
- Boehringer Ingelheim
- Enrollment
- 18
- Locations
- 1
- Primary Endpoint
- Ethinylestradiol: Area Under the Curve at Steady State Over the Uniform Dosing Interval τ (AUCτ,ss)
- Status
- Completed
- Last Updated
- 11 years ago
Overview
Brief Summary
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®).
Investigators
Eligibility Criteria
Inclusion Criteria
- Not provided
Exclusion Criteria
- Not provided
Arms & Interventions
Reference
multiple doses of Microgynon
Intervention: levonorgestrel
Reference
multiple doses of Microgynon
Intervention: Ethinylestradiol
Test
multiple doses of Microgynon + BI 10773
Intervention: levonorgestrel
Test
multiple doses of Microgynon + BI 10773
Intervention: Ethinylestradiol
Test
multiple doses of Microgynon + BI 10773
Intervention: Microgynon + BI 10773
Outcomes
Primary Outcomes
Ethinylestradiol: Area Under the Curve at Steady State Over the Uniform Dosing Interval τ (AUCτ,ss)
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.
Area under the concentration-time curve of ethinylestradiol in plasma at steady state over the uniform dosing interval τ.
Levonorgestrel: Maximum Measured Concentration (Cmax,ss)
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.
Maximum measured concentration of levonorgestrel in plasma at steady state over the uniform dosing interval τ.
Levonorgestrel: Area Under the Curve at Steady State Over the Uniform Dosing Interval τ (AUCτ,ss)
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.
Area under the concentration-time curve of levonorgestrel in plasma at steady state over the uniform dosing interval τ.
Ethinylestradiol: Maximum Measured Concentration (Cmax,ss)
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.
Maximum measured concentration of ethinylestradiol in plasma at steady state over the uniform dosing interval τ.
Secondary Outcomes
- Levonorgestrel: Apparent Clearance at Steady State (CL/Fss)(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)(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)(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)(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)(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)(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)(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)(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)(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)(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)(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)(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.(Day 1 to day 17)
- Assessment of Tolerability(Within Day 24 to Day 31)