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- Title
Simultaneous oral therapeutic and intravenous <sup>14</sup>C-microdoses to determine the absolute oral bioavailability of saxagliptin and dapagliflozin.
- Authors
Boulton, David W.; Kasichayanula, Sreeneeranj; Keung, Chi Fung (Anther); Arnold, Mark E.; Christopher, Lisa J.; Xu, Xiaohui (Sophia); LaCreta, Frank
- Abstract
Aim To determine the absolute oral bioavailability ( Fp.o.) of saxagliptin and dapagliflozin using simultaneous intravenous 14C-microdose/therapeutic oral dosing (i.v.micro + oraltherap). Methods The Fp.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. Results The geometric mean point estimates (90% confidence interval) Fp.o. values for saxagliptin and dapagliflozin were 50% (48, 53%) and 78% (73, 83%), respectively. The i.v.micro had similar pharmacokinetics to oraltherap. Conclusions Simultaneous i.v.micro + oraltherap dosing is a valuable tool to assess human absolute bioavailability.
- Subjects
ORAL drug administration; BIOAVAILABILITY; ACCELERATOR mass spectrometry; LIQUID chromatography-mass spectrometry; PHARMACOKINETICS
- Publication
British Journal of Clinical Pharmacology, 2013, Vol 75, Issue 3, p763
- ISSN
0306-5251
- Publication type
Article
- DOI
10.1111/j.1365-2125.2012.04391.x