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2000
Volume 20, Issue 4
  • ISSN: 1573-4110
  • E-ISSN: 1875-6727

Abstract

Background: Metformin is a biguanide derivative utilized as a first-line treatment for type 2 diabetes for people over 60 years. However, it faces certain limitations due to its incomplete absorption, resulting in a 50-60% bioavailability. In addition to its blood glucose-lowering effect, the antiproliferative effect of metformin has been demonstrated . Therefore, it is necessary to consider alternative administration routes that can enhance the bioavailability of metformin, expanding its clinical use beyond its role as an antidiabetic agent. Objective: The aim of the study was to develop a reliable bioanalytical method for the quantitation of metformin in male Sprague-Dawley rat plasma and explore the promising alternative administration route for metformin use. Methods: A robust, high-performance liquid chromatography-tandem mass spectrometry method for the quantification of metformin in rat plasma was developed and validated according to the latest regulatory guidance for bioanalysis. Results: Based on the area under the curves obtained from the rat pharmacokinetic study, subcutaneous injection increased the systemic exposure of metformin by 1.79-fold compared to oral administration in rats. Conclusion: Subcutaneous administration of metformin enhances its bioavailability compared to oral administration, leading to increased antidiabetic effects and potential antitumor activity.

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/content/journals/cac/10.2174/0115734110288849240116045045
2024-05-01
2025-06-18
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