Novel Application of the Two-Period Microtracer Approach to Determine Absolute Oral Bioavailability and Fraction Absorbed of Ertugliflozin.

ABSTRACT: Ertugliflozin, a sodium glucose cotransporter-2 inhibitor, is approved in the United States for treatment of type 2 diabetes mellitus. A novel two-period study design with ¹⁴ C microtracer dosing in each period was used to determine absolute oral bioavailability (F) and fraction absorbed (F_a ) of ertugliflozin. Eight healthy adult men received 100-μg i.v. ¹⁴ C-ertugliflozin (400 nCi) dose 1 h after a 15-mg oral unlabeled ertugliflozin dose (period 1), followed by 100 μg ¹⁴ C-ertugliflozin orally along with 15 mg oral unlabeled ertugliflozin (period 2). Unlabeled ertugliflozin plasma concentrations were determined using high-performance liquid-chromatography tandem mass spectrometry (HPLC-MS/MS). ¹⁴ C-ertugliflozin plasma concentrations

SUBMITTER: Raje S 

PROVIDER: S-EPMC6039199 | biostudies-literature | 2018 Jul

REPOSITORIES: biostudies-literature