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Table 2 Different formulations and the corresponding relevant characteristics of the oral drug metformin (information from [180])

From: Actions of metformin and statins on lipid and glucose metabolism and possible benefit of combination therapy

Metformin formulation Dose Cmax (ng/ml) tmax (h) AUCmean (ng*h/ml) Properties Refs
Immediate release (IR) 1000 mg bid 1328 3.5 18,710 Rapid gut absorption
90% absorption within 30 min
High systemic exposure
GI side effects
High systemic exposure
[180]
Extended release (ER) [181] 2000 mg qd 1688 5.1 16,990 Two-phase approach tablet using polymers
Prolonged gut absorption (duodenum and jejunum)
90% absorption within 10 h
[9, 182]
Delayed release (DR) [183] 500 mg bid/1000 mg bid 905/607 9/9 9010/6160 Enteric coated (polymers) core tablet
Release of metformin by pH of 6.5 (distal small intestine)
Late gut absorption (ileum)
Increased GLP-1 secretion
Less systemic exposure
[10]
  1. qd once a day, bid twice a day
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