Extemporaneous Formulations of Metformin for Pediatric Endocrinology: Physicochemical Integrity, Cytotoxicity of Sweeteners, and Quantitation of Plasma Levels

摘要

Purpose: In response to the lack of pediatric formulations of metformin to control type 2 diabetes mellitus, hyperinsulinemic obesity, and dyslipidemias, we developed liquid formulations of metformin by dissolving 3 generic brands of 500-mg metformint(*,dagger,double dagger) tablets in water sweetened with sucralose. The physicochemical stabilities of these drugs were assessed and compared with those of formulations made with the innovative brand of metformin.(parallel to) A method to measure metformin plasma levels was proposed and then tested in 2 healthy subjects. This method may be useful to survey treatment compliance in the future. The biological safety profiles of the metformin solutions were assessed preliminarily in a system of hormone-dependent cancer cells (human breast cancer MCF-7 cells).