Physicochemical characterization of YJA20379-8, a new proton pump inhibitor

The physicochemical properties of the potent reversible proton pump inhibitor YJA20379-8, 3-butyryl-4-[(R)-1-methylbenzylamino]-8-ethoxy-1,7-naphthyridine, were studied. YJA20379-8 is essentially nonhygroscopic pale yellowish crystalline powder. It is practically insoluble in water, and its lipid solubility is high. The pH solubility profile exhibits an L-shaped curve, indicating YJA20379-8 is a basic substance having a soluble ionized form in acidic conditions. This is consistent with the result of an experiment to determine pKa. The solid-state stability study shows that YJA20379-8 is stable at various temperatures and humidities, but is decomposed by light.