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Bioequivalence and Food Effect Assessment for Vildagliptin/Metformin Fixed-dose Combination Tablets Relative to Free Combination of Vildagliptin and Metformin in Japanese Healthy Subjects

Nozaki, Sachiko and Chitnis, Shripad and Kulmatycki, Kenneth and Salunke, Atish Azad and He, Yan-Ling and Zhou, Wei and Suzuki, Hikoe (2015) Bioequivalence and Food Effect Assessment for Vildagliptin/Metformin Fixed-dose Combination Tablets Relative to Free Combination of Vildagliptin and Metformin in Japanese Healthy Subjects. International Journal of Clinical Pharmacology and Therapeutics.

Abstract

Objective: To assess the bioequivalence of vildagliptin/metformin fixed-dose combination (FDC) tablets (50/250 mg and 50/500 mg) to free combinations of vildagliptin and metformin and the effect of food on the pharmacokinetics (PK) of vildagliptin and metformin following administration of a 50/500 mg FDC tablet.
Methods: Two open label, randomized, single-center, single-dose, 2-period crossover studies were conducted in Japanese male healthy volunteers. Participants were administered vildagliptin/metformin FDC tablet (Study I: 50/250 mg, Study II: 50/500 mg) or their free combination under fasted condition. Food effect (standard Japanese breakfast; composition: 20-30% from fat with approximately 600 kcal in total) was assessed in an additional period in Study II (50/500 mg). PK parameters (AUC, Cmax, Tmax, T1/2) were calculated for vildagliptin and metformin.
Results: For both studies, vildagliptin/metformin FDC tablets were bioequivalent to their respective free combinations. Administration of FDC tablet following a meal had no effect on vildagliptin PK parameters. The rate of absorption of metformin was decreased when given under fed condition, as reflected by a prolonged Tmax (from 3h in fasted state to 4h in fed state) and reduction in Cmax by 26%, but the extent of absorption (AUClast) was similar to fasted state.
Conclusions: The vildagliptin/metformin FDC tablets were bioequivalent to their free combinations. Food decreased metformin Cmax by 26% while AUClast was unchanged, consistent with previous reports. No food effect on vildagliptin Cmax or AUClast were observed. Therefore, food had no clinically relevant effect of metformin or vildagliptin pharmacokinetics.

Item Type: Article
Keywords: Bioequivalence – vildagliptin – metformin – fixed-dose combination – food effect
Date Deposited: 28 Apr 2016 23:45
Last Modified: 28 Apr 2016 23:45
URI: https://oak.novartis.com/id/eprint/26933

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