Effect of food on the pharmacokinetics of a vildagliptin/metformin (50/1000 mg) fixed-dose combination tablet in healthy volunteers

He, Yan-Ling; Flannery, Brian; Campestrini, Joelle; Leon, Selene; Zinny, Miguel A.; Ligueros‐Saylan, Monica; Jarugula, Venkateswar

doi:10.1185/03007990802114070

Cited by 19 publications

(12 citation statements)

References 22 publications

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“…This finding is consistent with results of other clinical studies in which co-administration with food of a metformin HCl IR tablet alone [33], or as an IR FDC tablet with other antidiabetic agents [26,27,28], resulted in reduced C max by 15 -39% and delayed t max by 0.5 -1.5 hours. In one study, AUC of 850 mg metformin IR tablet decreased by ~ 25% [33].…”

Section: Discussionsupporting

confidence: 91%

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Effect of food on the pharmacokinetics of canagliflozin/metformin (150/1,000 mg) immediate-release fixed-dose combination tablet in healthy participants

Murphy

Wang

Stieltjes

et al. 2015

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Section: Discussionsupporting

confidence: 91%

“…The highest strength of the FDC tablet manufactured at 150/1,000 mg for twice a day dosing was investigated in accordance with US FDA and EMA guidelines on food-effect bioavailability and fed bioequivalence studies [24,25], and similarly designed food effect studies on other antidiabetic agents formulated as FDC with metformin [26,27,28].…”

Section: Introductionmentioning

confidence: 99%

Effect of food on the pharmacokinetics of canagliflozin/metformin (150/1,000 mg) immediate-release fixed-dose combination tablet in healthy participants

Murphy

Wang

Stieltjes

et al. 2015

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“…No dosage adjustment is necessary based on age, gender, body mass index (BMI), food intake, presence of hepatic impairment, or concomitant use of commonly used drugs (He et al 2008a; He et al 2007d; He et al 2007e; He et al 2007f; Sunkara 2007; He et al 2008b). Bio-equivalence of the fixed-dose combination of vildagliptin and metformin with the individual components has been shown; the effect of food in decreasing metformin exposure was smaller with the metformin component in the fixed-dose combination than has been reported with metformin alone, and the fixed-dose combination can thus be administered in the same manner as metformin alone (He et al 2008c; He et al 2008d). …”

Section: Pharmacologic Overviewmentioning

confidence: 97%

Vildagliptin: a new oral treatment for type 2 diabetes mellitus

Mathieu

Degrande²

2008

VHRM

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Vildagliptin is a new oral antidiabetic agent that enhances pancreatic islet cell responsiveness to glucose. An extensive clinical program involving approximately 22,000 patients and 7000 patient-years of exposure to vildagliptin has shown that the agent is well tolerated and effi cacious in improving glycemic control in patients with type 2 diabetes mellitus (T2DM). Monotherapy trials have shown that signifi cant HbA1c lowering is accompanied by body weight-neutral and lipid-neutral effects, low risk of edema, and low risk of hypoglycemia. These characteristics make vildagliptin a favorable partner for combination therapy. Studies of vildagliptin as an add-on to metformin have shown signifi cant improvements in glycemic control (comparable to that of thiazolidinedione add-on), with the combination being well tolerated and associated with low risks for hypoglycemia and adverse effects on weight or lipid levels. Good tolerability and clinically relevant improvements in glycemic control have also been observed with vildagliptin as an add-on treatment to sulfonylurea, thiazolidinedione, or insulin treatment or in initial combination treatment with pioglitazone. Improved β-cell function and glycemic control have been shown with vildagliptin in subjects with impaired glucose tolerance and in T2DM patients with mild hyperglycemia, with some evidence in the latter suggesting the potential for modifying disease course. Keywords: diabetes, vildagliptin, incretin, metformin, add-on treatment, hypoglycemia Type 2 diabetes mellitus (T2DM) is a dual disease, characterized by islet (beta-and alpha-) cell dysfunction in the setting of insulin resistance. Moreover, ample clinical evidence, such as data from the landmark UK Prospective Diabetes Study (UKPDS), indicates that loss of beta-cell function is progressive. This progressive decline leads to the clinical impression of failure of therapy in T2DM patients and is the main reason why so many patients with T2DM are not within target ranges of glycemic control. Moreover, the clear alpha-cell dysfunction that is also present in T2DM has been disregarded in previous years, mainly because therapeutic interventions were lacking. The need to address this underlying islet cell defi cit led to a search for therapeutic alternatives and has led to the rediscovery of the incretin hormones and their role in glucose homeostasis. Improved understanding of their potential has led in turn to the development of incretin analogs and incretin enhancers for treatment of T2DM (Deacon 2004;Vilsbøll and Holst 2004;Drucker 2006;Deacon et al 2008).The present review will discuss the data available on the incretin enhancer vildagliptin, a potent and selective inhibitor of dipeptidyl peptidase-4 (DPP-4), the enzyme responsible for the rapid degradation of the incretin hormones glucagonlike peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). This activity increases levels of active incretins and enhances pancreatic islet α-and β-cell responsiveness to glucose, thus improving ...

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“…49 Vildagliptin and metformin exhibit com- Food has no effect on the rate and extent of absorption of vildagliptin from the single-tablet combination. 42 The rate of absorption of metformin is decreased when given with food, but the extent of absorption is not changed. 42 …”

Section: Pharmacokinetics and Metabolismmentioning

confidence: 98%

“…42 The rate of absorption of metformin is decreased when given with food, but the extent of absorption is not changed. 42 …”

Section: Pharmacokinetics and Metabolismmentioning

confidence: 98%

Drug evaluation: Vildagliptin-metformin single-tablet combination

2009

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The single-tablet combination of vildagliptin and metformin addresses key defects of type 2 diabetes for improved glycemic control. By inhibiting the dipeptidyl peptidase-4 (DPP-4) enzyme, vildagliptin raises the levels of the active incretin hormones, glucagon-like peptide 1 and glucose-dependent insulinotropic peptide. This leads to increased synthesis and release of insulin from the pancreatic beta cells and decreased release of glucagon from the pancreatic alpha cells. The combination tablet also contains metformin, which addresses insulin resistance. The complementary mechanisms of action of the two agents in combination have been shown to provide additive and sustained reductions in hemoglobin A(1c) compared with metformin monotherapy. In active-controlled trials, the vildagliptin-metformin combination has been shown to produce equivalent reductions in hemoglobin A(1c) to pioglitazone-metformin and glimepiride-metformin combinations, without significant risk of hypoglycemia and without causing weight gain. In clinical trials, the overall incidence of any adverse event was similar in patients randomized to vildagliptin plus metformin and placebo plus metformin. Available data support the use of vildagliptin in combination with metformin as a promising second-line treatment for the management of type 2 diabetes and this is reflected in the latest UK National Institute for Health and Clinical Excellence draft guideline for consultation on new agents for blood glucose control in type 2 diabetes.

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Effect of food on the pharmacokinetics of a vildagliptin/metformin (50/1000 mg) fixed-dose combination tablet in healthy volunteers

Abstract: The vildagliptin/metformin (50/1000 mg) fixed-dose combination tablet can be administered in the same manner as metformin, and can be recommended to be taken with meals to reduce the gastrointestinal symptoms associated with metformin.

Cited by 19 publications

References 22 publications

Effect of food on the pharmacokinetics of canagliflozin/metformin (150/1,000 mg) immediate-release fixed-dose combination tablet in healthy participants

Effect of food on the pharmacokinetics of canagliflozin/metformin (150/1,000 mg) immediate-release fixed-dose combination tablet in healthy participants

Vildagliptin: a new oral treatment for type 2 diabetes mellitus

Drug evaluation: Vildagliptin-metformin single-tablet combination

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