title: Clinical development of metformin extended-release tablets for type 2 diabetes: an overview.
abstract: Glumetz (Depomed, Inc., Menlo Park, CA, USA) is a recently approved gastric retentive extended-release formulation of metformin (M-ER) that provides effective, sustained and well-tolerated glycemic control with once daily administration. Pharmacokinetic studies have demonstrated a similar bioavailability of M-ER administered once daily to immediate-release metformin given twice daily. In addition, M-ER has demonstrated a nearly linear dose proportionality with a relative bioavailability of highest dose to lowest dose of 80%, whereas with immediate-release metformin the relative bioavailability of the highest dose to the lowest dose is only 58%. M-ER demonstrated a positive food effect and should be administered with a meal, preferably the evening meal. Because metformin is only eliminated through renal mechanisms, the use of M-ER, as is the case with other formulations, is contraindicated in patients with renal impairment. Administration of M-ER with sulfonylureas (SUs) had no effect on the pharmacokinetics of metformin. In controlled clinical trials M-ER demonstrated efficacy for 24 weeks as a monotherapy or in combination with SU. Additionally, glycemic control was maintained for an extra 24 weeks in an open-label monotherapy extension study of M-ER. M-ER was well tolerated in all studies.
authors: Diabetes and Glandular Diseases Clinic, San Antonio, TX, USA.
authors: Sherwin L
authors: SL
authors: Schwartz
authors: Toufigh
authors: T
authors: Gordi
authors: Eddie
authors: E
authors: Hou
authors: Marilou
authors: M
authors: Cramer
authors: Michelle
authors: M
authors: Heritier
authors: Verne E
authors: VE
authors: Cowles
mesh_terms: D001682:Biological Availability; D002986:Clinical Trials as Topic; D003692:Delayed-Action Preparations; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy*; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D018565:Food-Drug Interactions; D006801:Humans; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D008687:Metformin / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D051437:Renal Insufficiency / Q000150:complications
chemical_list: D003692:Delayed-Action Preparations; D007004:Hypoglycemic Agents; D008687:Metformin