The Absolute Oral Bioavailability and??Population-Based Pharmacokinetic Modelling of a Novel Dipeptidylpeptidase-IV Inhibitor, Vildagliptin, in Healthy Volunteers

• Published in: Clinical pharmacokinetics Vol. 46; no. 9; pp. 787 - 802
• Main Authors: He, Yan-Ling, Sadler, Brian M, Sabo, Ron, Balez, Sebastien, Wang, Yibin, Campestrini, Joelle, Laurent, Aziz, Ligueros-Saylan, Monica, Howard, Dan
• Format: Journal Article
• Language: English
• Published: Auckland Adis international 01.01.2007; Wolters Kluwer Health, Inc; Springer Nature B.V
• Subjects: Adamantane - administration & dosage; Adamantane - analogs & derivatives; Adamantane - pharmacokinetics; Administration, Oral; Adolescent; Adult; Algorithms; Analysis of Variance; Area Under Curve; Biological and medical sciences; Biological Availability; Body Mass Index; Body Weight; Cross-Over Studies; Dipeptidyl Peptidase 4; Dipeptidyl-Peptidase IV Inhibitors; Female; General and cellular metabolism. Vitamins; Half-Life; Humans; Hypoglycemic Agents - administration & dosage; Hypoglycemic Agents - blood; Hypoglycemic Agents - pharmacokinetics; Injections, Intravenous; Male; Medical sciences; Metabolic Clearance Rate; Middle Aged; Nitriles - administration & dosage; Nitriles - pharmacokinetics; Pharmacology. Drug treatments; Pyrrolidines - administration & dosage; Pyrrolidines - pharmacokinetics; Sex Factors; Dipeptidyl-peptidase IV; Human; Population pharmacokinetics; Healthy subject; Enzyme; Oral administration; Enzyme inhibitor; Bioavailability; Peptidases; Hypoglycemic agent; Analog; Hydrolases; Vildagliptin

Vildagliptin is a potent, selective, orally active inhibitor of dipeptidylpeptidase-IV being developed for the treatment of type 2 diabetes mellitus. The objective of this study was to assess the absolute oral bioavailability of vildagliptin by comparing the systemic exposure after oral and intraven...