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Comparative Bioavailability and Pharmacokinetics Between the Solid Form of Metformin vs a Novel Liquid Extemporaneous

Radamés Alemón-Medina1, Nelly Altamirano-Bustamante2, Gustavo Lugo-Goytia3

  • 1Laboratory of Pharmacology, National Institute of Pediatrics (NIP), Mexico City, Mexico.

Dose-Response : a Publication of International Hormesis Society
|October 4, 2021
PubMed

Insights

A new liquid metformin formulation shows similar pharmacokinetics to standard tablets in pediatric patients. This offers a more adaptable and easier-to-administer option for children requiring metformin treatment.

Area of Science:

  • Pharmacology and Pharmaceutical Sciences
  • Clinical Pharmacy
  • Pediatric Medicine

Background:

  • Metformin is a first-line oral antihyperglycemic agent for type 2 diabetes.
  • Accurate and flexible dosing is crucial for effective pediatric pharmacotherapy.
  • Extemporaneous liquid formulations can improve medication adherence and precision in pediatric populations.

Purpose of the Study:

  • To determine the pharmacokinetics of an extemporaneous liquid metformin formulation in pediatric patients.
  • To compare the pharmacokinetic profile of the liquid formulation against standard metformin tablets.
  • To assess the suitability of the liquid formulation for pediatric use.

Main Methods:

  • A randomized, transversal clinical trial involving 34 children and adolescents (7-17 years).
  • Administration of either liquid metformin formulation or standard 500 mg tablet.
  • Blood sample collection on Whatman 903® cards at specified time points (0-24 hours).
  • Ultra-Performance Liquid Chromatography (UPLC) and tandem mass spectrometry for drug detection.

Main Results:

  • The developed UPLC-MS/MS method was accurate, precise, selective, and linear (50-1000 ng/mL).
  • Pharmacokinetic parameters (Cmax, Tmax, half-life) were comparable between the liquid formulation and tablet.
  • Geometric mean ratios (90% CI) for Cmax, AUC0-t, and AUC0-∞ demonstrated bioequivalence.

Conclusions:

  • The liquid extemporaneous formulation of metformin exhibits similar pharmacokinetics to conventional tablets in pediatric patients.
  • This formulation facilitates more precise dose adjustments and enhances ease of administration.
  • The findings support the use of this liquid metformin formulation for improved pediatric diabetes management.

Keywords:
bioavailabilityextemporaneous formulationmetforminpaediatricspharmacokinetics

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