Determination of temelastine and a hydroxymethyl-pyridyl metabolite in biological fluid by high-performance liquid...

A high-performance liquid chromatographic method for the analysis of temelastine (1) and 2-[4-(5-bromo-3-methylpyrid-2-yl)-butylamino]-5-[6-hydroxymethy lpyrid-3- ylmethyl]-pyrimidin-4(1H)-one (1-A) in biological fluid is presented. The method combines the previously reported extraction procedure and new chromatography conditions capable of resolving 1, 1-A, and structurally similar compounds formed by the oxidation of 1. The modified method has been used to measure concentrations of 1 and 1-A in biological fluids taken from the rat and dog, and to look for the presence of 1-A in humans following administration of 1.