title: Relative bioavailability study of linagliptin/metformin tablets in healthy Chinese subjects.
abstract: OBJECTIVE
  To evaluate the relative bioavailability of single pill combination (SPC) tablets of linagliptin and metformin compared with separate tablets co-administered in healthy Chinese subjects.
  
  
  METHODS
  This was an open-label, single-dose, randomized, two-period, crossover study in healthy Chinese subjects with two dose groups: linagliptin 2.5 mg/metformin 850 mg and linagliptin 2.5 mg/metformin 500 mg. Within each group (n=24), subjects received one dose of the SPC tablet in one period and one dose of the separate tablets in the other. Primary endpoints were area under the plasma concentration-time curve from 0 to 72 hours (AUC0-72) and maximum plasma concentration (Cmax) for linagliptin, and AUC from 0 to the last quantifiable concentration (AUC0-tz) and Cmax for metformin.
  
  
  RESULTS
  With the linagliptin 2.5 mg/metformin 850 mg dose, the adjusted geometric mean ratio of the SPC to the separate tablets for linagliptin was 99.53% (90% confidence interval (CI): 94.75-104.55) for AUC0-72 and 101.93% (90% CI: 95.36-108.95) for Cmax; for metformin the ratio was 96.99% (90% CI: 90.62-103.81) for AUC0-tz and 94.64% (90% CI: 85.43-104.84) for Cmax. With the linagliptin 2.5 mg/metformin 500 mg dose, the ratio with linagliptin for AUC0-72 and Cmax was 100.81% (90% CI: 95.14-106.82) and 111.37% (90% CI: 100.40-123.54), respectively; the same statistical parameters with metformin for AUC0-tz and Cmax were 102.95% (90% CI: 96.24-110.12) and 102.46% (90% CI: 92.20-113.87), respectively.
  
  
  CONCLUSIONS
  SPC tablets of linagliptin and metformin were bioequivalent to separate tablets co-administered in healthy Chinese subjects.
authors.forename: Solen
authors.initials: S
authors.lastname: Pichereau
authors.forename: Xia
authors.initials: X
authors.lastname: Zhao
authors.forename: Yimin
authors.initials: Y
authors.lastname: Cui
authors.forename: Shuai
authors.initials: S
authors.lastname: Zhao
authors.forename: Kathrin
authors.initials: K
authors.lastname: Hohl
authors.forename: Thomas
authors.initials: T
authors.lastname: Meinicke
authors.forename: Christian
authors.initials: C
authors.lastname: Friedrich
mesh_terms: D000284:Administration, Oral; D000328:Adult; D019540:Area Under Curve; D044466:Asian People; D001682:Biological Availability; D002681:China; D018592:Cross-Over Studies; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D004338:Drug Combinations; D005260:Female; D006207:Half-Life; D064368:Healthy Volunteers; D006801:Humans; D007004:Hypoglycemic Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D000069476:Linagliptin; D008297:Male; D008657:Metabolic Clearance Rate; D008687:Metformin / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D011687:Purines / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D011799:Quinazolines / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D013607:Tablets; D055815:Young Adult
chemical_list: D054873:Dipeptidyl-Peptidase IV Inhibitors; D004338:Drug Combinations; D007004:Hypoglycemic Agents; D011687:Purines; D011799:Quinazolines; D013607:Tablets; D000069476:Linagliptin; D008687:Metformin