Pharmacokinetics of Metformin Gastric‐Retentive Tablets in Healthy Volunteers

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Abstract
The single‐dose pharmacokinetics of two gastric‐retentive, extended‐release tablet formulations of metformin hydrochloride in fed, healthy volunteers were compared with those of the currently marketed immediate‐release metformin hydrochloride product. The plasma concentration‐time profiles demonstrated extended‐release characteristics from the gastric‐retentive tablets. The mean bioavailability from each gastric‐retentive tablet was approximately 115%, relative to the immediate‐release (IR) product. Cmax values were lower and tmax values were greater for the gastric‐retentive tablets compared with the IR product. In contrast to conventional extended‐release metformin tablets reported in the literature, these gastric‐retentive tablets showed extended‐release plasma concentration profiles of metformin hydrochloride and increased bioavailability compared with the immediate‐release tablet.