Abstract
Pharmacokinetics of metformin extended release (XR) formulation were studied under fasting and fed conditions and compared to those of immediate release (IR) under fasting conditions in humans. 78 healthy human volunteers participated in 3 independent studies (26 subjects per study) were given either 1000 mg oral dose metformin IR or 750 mg metformin XR. Plasma samples were obtained up to 24 hours after dosing. Pharmacokinetic parameters in plasma were calculated by non compartmental analysis using Kinetica program. Results have shown increased XR bioavailability and delayed time to reach the maximum concentration (Cmax ) in the fed state as compared to fasted state, with no significant difference in Cmax and half life values. On the other hand, the IR formulation showed significant differences in all parameters as compared to XR formulation, yet the half life was similar. In conclusion, XR formulation was shown similar to IR formulation with less possible side effects.
Highlights
Metformin is an oral biguanide hypoglycemic agent
Cmax mean value of 1956 ng/ml of immediate release (IR) formulation is close to the upper limit of 2000 ng/ml and prone to increase above the upper limit at steady state
Cmax mean values are close to the effective level of 1000 ng/ml and prone to fall within 1000-2000 ng/ml at steady state
Summary
Metformin is an oral biguanide hypoglycemic agent. It causes an increased peripheral uptake of glucose by increasing the biological efficiency of available exogenous or endogenous insulin. The mode of action of metformin may be linked to an increase of insulin sensitivity. It does not stimulate insulin release but does require the presence of insulin to exert its hypoglycemic effect. Metformin hydrochloride is absorbed along the entire gastrointestinal mucosa. Maximum metformin plasma levels did not generally exceed 5 μg/mL, even at maximum doses. Metformin is excreted unchanged in the urine and does not undergo hepatic metabolism [1,2,3,4,5]
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