Some aspects of sorbinicate pharmacokinetics

A derivative of nicotinic acid, D-glucitol hexanicotinate (sorbinicate, SN), was investigated in rats for gastrointestinal absorption, hydrolysis to free nicotinic acid and plasma kinetics of nicotinic acid following oral administration. All the data obtained in several test conditions, suggest that SN is absorbed unhydrolysed in the first segment of the intestinal tract after being rendered at least partially soluble by the gastric HCl and subsequently hydrolysed to free nicotinic acid by several tissues. The hydrolysis is so rapid that the plasma nicotinic acid after a dose of SN is practically all in the free form. There are large species differences in the plasma kinetics of nicotinic acid after an oral dose of SN but in all species the plasma nicotinic acid levels are always much lower and more constant than after an equidose of nicotinic acid.