title: Effect of food on the pharmacokinetics of a vildagliptin/metformin (50/1000 mg) fixed-dose combination tablet in healthy volunteers.
abstract: OBJECTIVE
  Vildagliptin is an orally active, potent and selective DPP-4 inhibitor that improves glycemic control in patients with type 2 diabetes by increasing alpha- and beta-cell responsiveness to glucose.
  
  
  METHODS
  This open-label, single-center, randomized, two-period crossover study in healthy subjects (n=23) ages 18-45 years investigated the effect of food on the pharmacokinetics of vildagliptin and metformin following administration of a vildagliptin/metformin (50/1000 mg) fixed-dose combination tablet.
  
  
  RESULTS
  Administration of the fixed-dose combination tablet following a high-fat meal had no effect on vildagliptin AUC(0-infinity) (ratio of geometric mean for fed:fasted state, 1.10 [90% CI 1.03, 1.18]), C(max) (ratio of means 0.98 [90% CI 0.85, 1.13]) or median t(max) (2.5 h in fed and fasted states). The rate of absorption of metformin was decreased when given with food, as reflected by the prolonged t(max) (2-4 h) and reduction in C(max) (by 26%), but the extent of absorption was not changed. The food effect on the metformin component of the fixed-dose combination tablets was consistent with, but of a lesser magnitude compared with data stated.
  
  
  CONCLUSIONS
  The vildagliptin/metformin (50/1000 mg) fixed-dose combination tablet can be administered in the same manner as metformin, and can be recommended to be taken with meals to reduce the gastrointestinal symptoms associated with metformin.
authors.affiliation: Novartis Institutes for Biomedical Research, Cambridge, MA, USA.
authors.forename: Yan-Ling
authors.initials: YL
authors.lastname: He
authors.forename: Brian
authors.initials: B
authors.lastname: Flannery
authors.forename: Joelle
authors.initials: J
authors.lastname: Campestrini
authors.forename: Selene
authors.initials: S
authors.lastname: Leon
authors.forename: Miguel A
authors.initials: MA
authors.lastname: Zinny
authors.forename: Monica
authors.initials: M
authors.lastname: Ligueros-Saylan
authors.forename: Venkateswar
authors.initials: V
authors.lastname: Jarugula
mesh_terms: D000218:Adamantane / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D000293:Adolescent; D000328:Adult; D018592:Cross-Over Studies; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000008:administration & dosage* / Q000494:pharmacology* / Q000627:therapeutic use; D004338:Drug Combinations; D005260:Female; D018565:Food-Drug Interactions; D006801:Humans; D008297:Male; D008687:Metformin / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D008875:Middle Aged; D009570:Nitriles / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D011759:Pyrrolidines / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D000077597:Vildagliptin
chemical_list: D054873:Dipeptidyl-Peptidase IV Inhibitors; D004338:Drug Combinations; D009570:Nitriles; D011759:Pyrrolidines; D008687:Metformin; D000077597:Vildagliptin; D000218:Adamantane