Pharmacokinetic modeling of glimepiride plasma concentration in healthy subjects

Rev Med Chir Soc Med Nat Iasi. 2011 Jul-Sep;115(3):949-53.

Abstract

Aim: To determine the pharmacokinetics of glimepiride, a sulfonylurea antidiabetic agent, after single dose administration in healthy subjects.

Material and methods: Pharmacokinetic data for modeling were extracted from a single-center, randomized, single-dose, fasting state, two-way crossover bioequivalence study on 4 mg glimepiride in 24 healthy subjects.

Results: Plasma concentrations of glimepiride were measured using a validated LC/MS/MS method. The pharmacokinetic parameters were calculated using non-compartmental analysis. Different pharmacokinetic models were tested to evaluate pharmacokinetics of glimepiride. The optimal model was chosen based on Akaike's Information Criteria.

Conclusion: Compartmental analysis demonstrated that oral glimepiride tablets obey one compartment open model with rapid absorption following a first order kinetics and a short half-life.

Publication types

  • Randomized Controlled Trial

MeSH terms

  • Administration, Oral
  • Adult
  • Area Under Curve
  • Blood Glucose / drug effects*
  • Cross-Over Studies
  • Fasting
  • Female
  • Half-Life
  • Humans
  • Hypoglycemic Agents / administration & dosage
  • Hypoglycemic Agents / adverse effects
  • Hypoglycemic Agents / pharmacokinetics*
  • Male
  • Mathematical Computing
  • Reference Values
  • Sulfonylurea Compounds / administration & dosage
  • Sulfonylurea Compounds / adverse effects
  • Sulfonylurea Compounds / pharmacokinetics*
  • Tablets

Substances

  • Blood Glucose
  • Hypoglycemic Agents
  • Sulfonylurea Compounds
  • Tablets
  • glimepiride