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Simultaneous oral therapeutic and intravenous ¹⁴C-microdoses to determine the absolute oral bioavailability of saxagliptin and dapagliflozin.
- Source :
-
British journal of clinical pharmacology [Br J Clin Pharmacol] 2013 Mar; Vol. 75 (3), pp. 763-8. - Publication Year :
- 2013
-
Abstract
- Aim: To determine the absolute oral bioavailability (F(p.o.) ) of saxagliptin and dapagliflozin using simultaneous intravenous ¹⁴C-microdose/therapeutic oral dosing (i.v.micro + oraltherap).<br />Methods: The F(p.o.) values of saxagliptin and dapagliflozin were determined in healthy subjects (n = 7 and 8, respectively) following the concomitant administration of single i.v. micro doses with unlabelled oraltherap doses. Accelerator mass spectrometry and liquid chromatography-tandem mass spectrometry were used to quantify the labelled and unlabelled drug, respectively.<br />Results: The geometric mean point estimates (90% confidence interval) F(p.o) . values for saxagliptin and dapagliflozin were 50% (48, 53%) and 78% (73, 83%), respectively. The i.v.micro had similar pharmacokinetics to oraltherap.<br />Conclusions: Simultaneous i.v.micro + oraltherap dosing is a valuable tool to assess human absolute bioavailability.<br /> (© 2012 Bristol-Myers Squibb, Co.. British Journal of Clinical Pharmacology © 2012 The British Pharmacological Society.)
- Subjects :
- Adamantane pharmacokinetics
Administration, Intravenous
Administration, Oral
Adolescent
Adult
Area Under Curve
Benzhydryl Compounds
Biological Availability
Chromatography, Liquid
Dipeptidyl-Peptidase IV Inhibitors pharmacokinetics
Dose-Response Relationship, Drug
Humans
Male
Mass Spectrometry
Middle Aged
Sodium-Glucose Transport Proteins administration & dosage
Sodium-Glucose Transport Proteins pharmacokinetics
White People
Young Adult
Adamantane analogs & derivatives
Dipeptides pharmacokinetics
Dipeptidyl-Peptidase IV Inhibitors administration & dosage
Glucosides pharmacokinetics
Sodium-Glucose Transport Proteins antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1365-2125
- Volume :
- 75
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- British journal of clinical pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 22823746
- Full Text :
- https://doi.org/10.1111/j.1365-2125.2012.04391.x