Meglumine (DB09415): A Comprehensive Monograph on its Dichotomous Role as a Benign Excipient and a Component of Potent APIs

Executive Summary

Meglumine is a glucose-derived amino sugar with a fundamentally dichotomous identity in medicine and pharmacology. On one hand, it is globally recognized and widely employed as a benign pharmaceutical excipient, valued for its exceptional ability to enhance the aqueous solubility and stability of Active Pharmaceutical Ingredients (APIs).[1] Its physicochemical properties, stemming from a polyol backbone and a basic amino group, make it an ideal solubilizer, pH modifier, and counterion for forming stable, bioavailable salts with poorly soluble drug candidates. In this capacity, it is generally considered pharmacologically inert and possesses a very low toxicity profile.

On the other hand, meglumine serves as an integral component of potent therapeutic and diagnostic agents, where the overall formulation exhibits significant pharmacological activity and, in some cases, severe toxicity. This is most evident in its use in the antiprotozoal drug meglumine antimoniate—a first-line treatment for leishmaniasis—and in a vast array of iodinated and gadolinium-based radiological contrast media.[5] This report establishes a central thesis: the pharmacological and toxicological profile of any meglumine-containing product is dictated not by meglumine itself, but almost exclusively by the API or counterion with which it is paired. The safety of "meglumine" is therefore a meaningless concept without specifying its chemical and clinical context.