The relative bioavailability of two formulations containing 10 mg Dapagliflozin assessed under fasting conditions in a randomized crossover study in healthy Caucasian subjects

Monica Oroian 1 , 2 , Diana Ioana Pop 1 , 2 , Ana-Maria Gheldiu 3 , Sandeep Bhardwaj 2 , Adriana Marcovici 2 , Arshad Khuroo 4  and Laurian Vlase 1
  • 1 Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, Cluj-Napoca, Romania
  • 2 Clinical Pharmacology and Pharmacokinetics Department, Cluj-Napoca, Romania
  • 3 Department of Pharmaceutical Botany, Faculty of Pharmacy, Cluj-Napoca, Romania
  • 4 Clinical Pharmacology and Pharmacokinetics Department, Gurugram, India

Abstract

Objective: The aim of the present study was to evaluate the relative bioavailability of two formulations containing 10 mg dapagliflozin in healthy Caucasian subjects under fasting conditions.

Materials and Methods: Forty-eight healthy Caucasian subjects were enrolled in a single-dose, crossover, balanced, open label, randomized clinical trial, with two treatment, two periods and two sequences. The wash-out period was of 7 days and thirty-eight subjects completed both study periods. Each subject received a single dose of 10 mg dapagliflozin as the reference product Farxiga® (AstraZeneca Pharmaceuticals LP, USA) and the test product developed by Sun Pharmaceutical Industries, India. Dapagliflozin plasma levels were determined from blood samples collected in both study periods before and after dosing until 48 hours by using a validated LC-MS/MS method. For pharmacokinetic analysis of data, the non-compartmental method was used (Phoenix® WinNonlin 6.3). The statistical analysis was performed by SAS software 9.1.3 for the logarithmically transformed values of maximum plasma concentration and area under the curve.

Results: The 90% confidence intervals for the evaluated pharmacokinetic parameters were found to be in the accepted interval for bioequivalence (80.00-125.00%).

Conclusion: The 10 mg dapagliflozin immediate release tablet newly developed by Sun Pharmaceutical Industries, India, is bioequivalent with the reference product Farxiga® under fasted state of the subjects.

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