Pharmacokinetics of metformin gastric-retentive tablets in healthy volunteers.
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.
Gusler
G
G
DepoMed, Inc., 1360 O'Brien Drive, Menlo Park, CA 94025-1436, USA.
Gorsline
J
J
Levy
G
G
Zhang
S Z
SZ
Weston
I E
IE
Naret
D
D
Berner
B
B
D000328:Adult; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D018592:Cross-Over Studies; D004304:Dosage Forms; D006801:Humans; D007004:Hypoglycemic Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics; D008687:Metformin / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*
D004304:Dosage Forms; D007004:Hypoglycemic Agents; D008687:Metformin