Pharmacokinetic bioequivalence of sitagliptin phosphate tablet formulations: a randomized, open-label, crossover study in healthy volunteers

Category: Review Article
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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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This manuscript has been accepted for publication and undergone full peer review but has not been through the copyediting, typesetting, pagination and proofreading process, which may lead to differences between this version and the Version of Record. 

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