Pharmacokinetics of Metformin Gastric‐Retentive Tablets in Healthy Volunteers

Gusler, G.; Gorsline, J.; Lévy, G.; Zhang, S. Z.; Weston, Irving E.; Naret, Daniel G; Berner, Bret

doi:10.1177/00912700122010546

Cited by 84 publications

(43 citation statements)

References 10 publications

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“…At the end of treatment, mean A1C levels in the 2,000-mg extended-release metformin q.d. and immediate-release metformin groups, respectively, were 6.94 and 7.33% for drug-naïve patients, 6.76 and 7.23% for patients at least 65 years of age, 7.17 and 7.64% for female patients, 7.23 and 7.88% for nonCaucasian patients, and 7.05 and 7.62% for patients with BMI Ն30 kg/m 2 . Significant reductions (P Ͻ 0.001) in mean FPG concentrations were observed Extended-release metformin for type 2 diabetes by the end of week 1 in all treatment groups.…”

Section: Efficacy Resultsmentioning

confidence: 95%

Efficacy, Tolerability, and Safety of a Novel Once-Daily Extended-Release Metformin in Patients With Type 2 Diabetes

et al. 2006

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OBJECTIVE -The purpose of this study was to determine the efficacy and safety of a novel extended-release metformin in patients with type 2 diabetes.RESEARCH DESIGN AND METHODS -Adults with type 2 diabetes (newly diagnosed, treated with diet and exercise only, or previously treated with oral diabetic medications) were randomly assigned to receive one of three extended-release metformin treatment regimens (1,500 mg/day q.d., 1,500 mg/day twice daily, or 2,000 mg/day q.d.) or immediate-release metformin (1,500 mg/day twice daily) in a double-blind 24-week trial.RESULTS -Significant decreases (P Ͻ 0.001) in mean HbA 1c (A1C) levels were observed by week 12 in all treatment groups. The mean changes from baseline to end point in the two groups given 1,500 mg extended-release metformin (Ϫ0.73 and Ϫ0.74%) were not significantly different from the change in the immediate-release metformin group (Ϫ0.70%), whereas the 2,000-mg extended-release metformin group showed a greater decrease in A1C levels (Ϫ1.06%; mean difference [2,000 mg extended-release metformin Ϫ immediate-release metformin]: Ϫ0.36 [98.4% CI Ϫ0.65 to Ϫ0.06]). Rapid decreases in fasting plasma glucose levels were observed by week 1, which continued until week 8, and were maintained for the duration of the study. The overall incidence of adverse events was similar for all treatment groups, but fewer patients in the extended-release metformin groups discontinued treatment due to nausea during the initial dosing period than in the immediate-release metformin group. CONCLUSIONS -Once-or twice-daily extended-release metformin was as safe and effective as twice-daily immediate-release metformin and provided continued glycemic control for up to 24 weeks of treatment. Diabetes Care 29:759 -764, 2006M etformin hydrochloride has been widely used as an effective and generally well-tolerated glucoselowering agent for Ͼ40 years and is the most frequently prescribed first-line therapy for patients with type 2 diabetes (1). Metformin typically reduces basal and postprandial hyperglycemia by ϳ25% in Ͼ90% of patients when given alone or with other therapies during a program of managed care (2). In the U.K. Prospective Diabetes Study, intensive glucose control with metformin appeared to reduce the risk of diabetes-related end points in overweight patients and was associated with less weight gain and fewer hypoglycemic attacks than insulin (3).The objective of this study was to evaluate the efficacy, tolerability, and safety of a novel extended-release oral formulation of metformin compared with conventional immediate-release metformin during 24 weeks of double-blind treatment. When administered with food, the extended-release metformin tablet gradually releases drug over 8 h into the upper gastrointestinal tract (4), where metformin is primarily absorbed (5). Prolonged release of metformin from extended-release metformin tablets has been demonstrated in pharmacokinetic studies (6,7). Extended-release metformin showed slightly lower maximum concentrations, longer times to maxi...

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Section: Efficacy Resultsmentioning

confidence: 95%

Efficacy, Tolerability, and Safety of a Novel Once-Daily Extended-Release Metformin in Patients With Type 2 Diabetes

et al. 2006

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“…Magnetic susceptibilities were measured at room temperature on a Gouy 10 balance using Hg[Co(CNS)] 4 as calibrate. The IR spectra were recorded on a Perkin-Elmer Lamda-983 spectrometer with samples prepared as KBr pellets and UV Visible reflectance spectra were obtained on a Beckman DK-2A spectrophotometer using MgO as reference.…”

Section: Analysis and Physical Measurementsmentioning

confidence: 99%

“…It is an orally administered biguanide that has been widely used in the treatment and management of noninsulin dependent diabetes mellitus (NIDDM). Metformin lowers both basal and postprandial elevated blood glucose in patients with NIDDM, when hyperglycemia cannot be satisfactorily managed on diet alone [1][2][3][4] . Schiff bases offer a versatile and flexible series of ligands capable to bind with various metal ions to give complexes with suitable properties for theoretical and/or practical applications.…”

Section: Introductionmentioning

confidence: 99%

New Ternary Transition Metal Complexes of 2‐{[(2‐aminophenyl)imino] methyl}Phenol and Metformin: Synthesis, Characterization and Antimicrobial Activity

Sharma

Ramani

Dalwadi

et al. 2010

Journal of Chemistry

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Abstract:Complexes of Co(II), Ni(II) and Cu(II) were synthesized from Schiff base 2-{[(2-aminophenyl)imino]methyl}phenol and metformin. The authenticity of the transition metal complexes were characterized by elemental analyses, conductance and magnetic susceptibility measurements, as well as spectroscopic (IR, electronic) and thermal studies. IR spectral studies revealed the existence of the ligands in the amine form in the solid state. The magnetic and electronic spectral studies suggest an octahedral geometry for all the complexes. The metformin acts as a bidentate ligand and Schiff base of o-phynelendiamine and salicylaldehyde acts as a tridentate ligand. Antimicrobial screening of the Schiff base, metformin and transition metal complexes were determined against the bacteria Escherichia coli and Bacillus megaterium.

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“…Metformin HCl is a biguanidine class of antidiabetic drug prescribed orally for the treatment of non-insulin-dependent diabetes mellitus [1][2][3][4]. The assay of metformin HCl in immediate release tablets is usually carried out by UV spectrophotometry as per British Pharmacopoeia (BP) and United States Pharmacopoeia (USP) while HPLC method of assay has been given in the USP monograph for extended release metformin tablets [5][6].…”

Section: Introductionmentioning

confidence: 99%

Quantitative Determination of Metformin Hydrochloride in Tablet Formulation Containing Croscarmellose Sodium as Disintegrant by HPLC and UV Spectrophotometry

Umapathi¹,

Ayyappan²,

Quine³

2012

Trop. J. Pharm Res

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Pharmacokinetics of Metformin Gastric‐Retentive Tablets in Healthy Volunteers

Cited by 84 publications

References 10 publications

Efficacy, Tolerability, and Safety of a Novel Once-Daily Extended-Release Metformin in Patients With Type 2 Diabetes

Efficacy, Tolerability, and Safety of a Novel Once-Daily Extended-Release Metformin in Patients With Type 2 Diabetes

New Ternary Transition Metal Complexes of 2‐{[(2‐aminophenyl)imino] methyl}Phenol and Metformin: Synthesis, Characterization and Antimicrobial Activity

Quantitative Determination of Metformin Hydrochloride in Tablet Formulation Containing Croscarmellose Sodium as Disintegrant by HPLC and UV Spectrophotometry

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