Pharmacokinetic bioequivalence of sitagliptin phosphate tablet formulations: a randomized, open-label, crossover study in healthy volunteers
Category: Review Article
63 total, 3 today
Keywords: bioequivalence, new branded generics, pharmacokinetics, sitagliptin
Author byline as per print journal: Chuei Wuei Leong*,1, PhD; Elton Sagim1, BBiomedSc; Kar Ming Yee1, BPharm; Muhammad Shalhadi Saharuddin1, BSc; Nik Mohd Zulhakimi Nik Abdullah1, BSc; Noramirah Farhanah Saberi1, BSc; Rajavikraman Boopathy1, DipSc; Shahnun Ahmad1, MBBS; Atiqah Amran1, BSc; Raman Batheja2, PhD; Rajan Sharma2, MBBS; Kiran Kumar Vuppalavanchu2, MPharm
Study Objectives: The aim of the current study is to assess the rate and extent of absorption of a test and reference formulation containing sitagliptin.
Methods: An open-label, balanced, randomized, two-treatment, two-period, two-sequence crossover study was implemented to investigate the pharmacokinetic bioequivalence of a test and reference tablet products both containing a single dose of sitagliptin 100 mg in 28 healthy volunteers under fasting conditions. A total of twenty blood samples were obtained at pre-dose and multiple time intervals post-dose throughout the 48 hours sampling period. Sitagliptin concentrations were analysed using an LC-MS/MS validated method following a solid phase plasma extraction step. Sitagliptin pharmacokinetic parameters estimated with non-compartmental pharmacokinetic analysis were compared between the test and reference formulations with a multivariate analysis of variance.
Results and Discussion: The differences between the reference and test formulations in terms of area under the curve, 0 to infinity (AUC0‒inf), AUC0‒48, and the maximum concentration (Cmax) were found to be not significant. The 90% confidence intervals of sitagliptin Ln-transformed AUC0‒inf, AUC0‒48, and Cmax, were within the pharmacokinetic bioequivalence acceptance range of 80%‒125%.
Conclusion: The test formulation of sitagliptin was bioequivalent in terms of exposure to the reference formulation in healthy volunteers under fasting conditions.
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