Phase 1
Completed N=40
Relative Bioavailability of Two Different Batches of a Linagliptin / Metformin Combination Tablet in Healthy Volunteers
Healthy
Source: ClinicalTrials.gov NCT01216397 ↗
Enrolled (actual)
40
Serious AEs
0.0%
Results posted
Apr 2012
Primary outcomePrimary: Linagliptin: Maximum Measured Concentration (Cmax) — 5.36; 5.39 nmol/L
Summary
The objective of the current study is to investigate the relative bioavailability of two different batches of a 2.5 mg linagliptin / 1000 mg metformin fixed dose combination tablet (FDC).
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Linagliptin: Maximum Measured Concentration (Cmax) |
5.36; 5.39 | — |
| PRIMARY Area Under the Concentration-time Curve of Linagliptin in Plasma Over the Time Interval 0 to 72 Hours (AUC0-72) |
179; 179 | — |
| PRIMARY Metformin: Cmax |
1790; 1820 | — |
| PRIMARY Metformin: AUC0-tz |
12100; 12100 | — |
| SECONDARY Linagliptin: AUC0-infinity |
267; 267 | — |
| SECONDARY Linagliptin: Percentage of AUCtz-∞ Obtained by Extrapolation |
32.6; 32.1 | — |
| SECONDARY Linagliptin: Time to Maximum Measured Concentration of the Analyte in Plasma (Tmax) |
3.00; 3.00 | — |
| SECONDARY Linagliptin: λz (Terminal Elimination Rate Constant in Plasma) |
0.0153; 0.0152 | — |
| SECONDARY t1/2 (Terminal Half-life of the Analyte in Plasma) |
45.4; 45.6 | — |
| SECONDARY Linagliptin: MRTpo (Mean Residence Time of the Analyte in the Body After Peroral Administration) |
64.6; 64.5 | — |
| SECONDARY Linagliptin: Apparent Clearance of the Analyte in Plasma After Extravascular Administration (CL/F) |
330; 330 | — |
| SECONDARY Linagliptin: Apparent Volume of Distribution During the Terminal Phase Following an Extravascular Dose (Vz/F) |
1300; 1300 | — |
| SECONDARY Metformin: AUC0-infinity |
12400; 12300 | — |
| SECONDARY Metformin: Percentage of AUCtz-∞ Obtained by Extrapolation |
1.51; 1.52 | — |
| SECONDARY Metformin: Tmax |
1.99; 2.00 | — |
| SECONDARY Metformin: λz (Terminal Elimination Rate Constant in Plasma) |
0.0493; 0.0514 | — |
| SECONDARY Metformin: t1/2 (Terminal Half-life of the Analyte in Plasma) |
14.1; 13.5 | — |
| SECONDARY Metformin: MRTpo (Mean Residence Time of the Analyte in the Body After Peroral Administration) |
8.27; 8.23 | — |
| SECONDARY Metformin: CL/F |
1350; 1350 | — |
| SECONDARY Metformin: Vz/F |
1640; 1580 | — |
| SECONDARY Electrocardiogram (ECG), Vital Signs, Physical Finding or Laboratory Finding Abnormalities |
0; 0; 0; 0; 0; 0 | — |
| SECONDARY Participants With Treatment Emergent Adverse Events |
6; 9; 0; 1; 2; 1 | — |
| SECONDARY Participants Who Discontinued the Trial Because of an Adverse Event |
0; 0 | — |
| SECONDARY Assessment of Tolerability by the Investigator |
39; 40; 1; 0 | — |
Eligibility Criteria
Inclusion criteria
- Healthy males and females according to the following criteria: Based upon a complete medical history, including physical examination, vital signs (blood pressure (BP), pulse rate (PR)), 12-lead electrocardiogram (ECG), clinical laboratory tests
- Age 21 to 50 years (incl.)
- Body Mass Index (BMI) 18.5 to 29.9 kg/m2 (incl.)
- Signed and dated written informed consent prior to admission to the study in accordance with Good Clinical Practice (GCP) and the local legislation
Exclusion criteria
- Any finding of the medical examination (including BP, PR and ECG) deviating from normal and of clinical relevance
- Any evidence of a clinically relevant concomitant disease
- Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
- Surgery of the gastrointestinal tract (except appendectomy)
- Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
- History of relevant orthostatic hypotension, fainting spells or blackouts
- Chronic or relevant acute infections
- History of relevant allergy or hypersensitivity (including allergy to drug or its excipients)
- Intake of drugs within one month or less than 10 half-lives of the respective drug prior to first study drug administration
- Participation in another trial with an investigational drug within 2 months prior to administration or during the trial
- Smoker (more than 10 cigarettes or 3 cigars 3 pipes daily)
- Alcohol abuse (average consumption of more than 20 g/day in females and 30 g/day in males)
- Drug abuse
- Blood donation (more than 100 mL within four weeks prior to day 1 of visit 2)
- Any laboratory value outside the reference range that is of clinical relevance
- Inability to comply with dietary regimen of trial site
For female subjects of childbearing potential only:
- Positive pregnancy test, pregnancy or planning to become pregnant 1 month before study or within 2 months after study completion
- No adequate contraception 1 month before study and until 2 month after study completion, e.g. not any of the following: implants, injectables, combined hormonal contraceptives, hormonal IUD (intrauterine device), sexual abstinence for at least 1 month prior to first study drug administration, vasectomised partner (vasectomy performed at least 1 year prior to enrolment), or surgical sterilisation (including hysterectomy). Females, who do not have a vasectomised partner, are not sexually abstinent or surgically sterile will be asked to use an additional barrier method (e.g. condom).
- Lactation
Data sourced from ClinicalTrials.gov (NCT01216397). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.