Effects of meal timing relative to dosing on the pharmacokinetics and pharmacodynamics of vildagliptin in Japanese patients with Type 2 diabetes.
Summary of "Effects of meal timing relative to dosing on the pharmacokinetics and pharmacodynamics of vildagliptin in Japanese patients with Type 2 diabetes."
Objective: To assess the effects of meal timing on the pharmacokinetics and pharmacodynamics of the dipeptidyl peptidase IV (DPP-4) inhibitor vildagliptin in Japanese patients with Type 2 diabetes. Methods: In this open-label, single-center crossover study, 12 Japanese patients with Type 2 diabetes were randomized to twice-daily vildagliptin 50 mg, administered 30 min before or immediately before breakfast and dinner for 7 days. After a 7-day washout period, patients received the other regimen. Blood samples were collected for the determination of vildagliptin, DPP-4, glucagon-like peptide-1 (GLP-1) and glucose. Results: Vildagliptin absorption appeared slower when administered 30 min before rather than immediately before meals (tmax absolute range: 1.00 - 2.00 h vs. 0.33 - 1.58 h). Vildagliptin Cmax and AUC0-8 h were essentially the same irrespective of meal timing (geometric mean ratio: Cmax 1.08 (90% CI; 0.92 - 1.26); AUC0-8 h 0.97 (90% CI; 0.91 - 1.05)). Meal timing did not affect pharmacodynamics; complete DPP-4 inhibition (> 90%) was sustained for 8 h post-dose, and plasma active glucagon-like peptide-1 levels increased 2 - 3-fold from baseline. Fasting plasma glucose (FPG) and postprandial plasma glucose (PPPG) reductions from baseline did not differ significantly with meal timing (30 min before vs. immediately before: FPG, -8.9 vs. -5.8 mg/dl; adjusted AUE0-4 h, -67.0 vs. -51.0 mg×h/dl). Vildagliptin was well tolerated. Conclusions: Dosing 30 min or immediately before meals did not affect vildagliptin pharmacokinetics or pharmacodynamics in Japanese patients with Type 2 diabetes.
Novartis Institutes for BioMedical Research Inc., Cambridge, MA, USA, and Novartis Pharma KK, Tokyo and Kyushu Clinical Pharmacology Research Clinic, Fukuoka, Japan.
This article was published in the following journal.
Name: International journal of clinical pharmacology and therapeutics
Medical and Biotech [MESH] Definitions
Agents that aid or increase the action of the principle drug (DRUG SYNERGISM) or that affect the absorption, mechanism of action, metabolism, or excretion of the primary drug (PHARMACOKINETICS) in such a way as to enhance its effects.
Relative Value Scales
Coded listings of physician or other professional services using units that indicate the relative value of the various services they perform. They take into account time, skill, and overhead cost required for each service, but generally do not consider the relative cost-effectiveness. Appropriate conversion factors can be used to translate the abstract units of the relative value scales into dollar fees for each service based on work expended, practice costs, and training costs.
Measurable biological parameters that serve for drug development, safety and dosing (DRUG MONITORING).
The time frame after a meal or FOOD INTAKE.
A trisaccharide occurring in Australian manna (from Eucalyptus spp, Myrtaceae) and in cottonseed meal.
The pharmacokinetics of lipoyl vildagliptin, a novel dipeptidyl peptidase IV (DPP IV) inhibitor, was studied in rats after oral administration for developing it as an antidiabetic agent. A liquid chro...
A randomized, 2-period, crossover design study to assess the effects of dexlansoprazole, lansoprazole, esomeprazole, and omeprazole on the steady-state pharmacokinetics and pharmacodynamics of clopidogrel in healthy volunteers.
The aim of this study was to assess the effects of different proton pump inhibitors (PPIs) on the steady-state pharmacokinetics and pharmacodynamics of clopidogrel.
The objective of the study was to determine the impact of food and different meal types on the pharmacokinetics of rilpivirine, a nonnucleoside reverse transcriptase inhibitor. In this open-label, ran...
OBJECTIVES: Mycophenolic acid (MPA) is the active form of mycophenolate mofetil (MMF), which is currently used off-label as immunosuppressive therapy in childhood-onset SLE (cSLE). The objectives of t...
The purpose of this study is to assess the safety and effectiveness of vildagliptin, an unapproved drug, compared to placebo in lowering post-meal blood glucose levels in people with pre-d...
This study will evaluate the pharmacokinetics of vildagliptin and its metabolites in patients with mild, moderate or severe renal impairment and healthy volunteers.
CG106 is a Phase I open-label, randomized, multiple-dose, two-way crossover study to characterize the pharmacodynamics and pharmacokinetics of the investigational fixed-dose combination pr...
This study is designed to demonstrate the long-term safety of vildagliptin in patients with type 2 diabetes. This study will study vildagliptin as add-on therapy with metformin, thiazolidi...
The purpose of this study is to determine the effect of a light meal on the pharmacokinetics and pharmacodynamics of aliskiren in patients with mild to moderate hypertension.