BIOAVAILABILITY OF A CONTROLLED-RELEASE FORMULATION OF URSODEOXYCHOLIC ACID IN MAN

Several controlled release formulations of ursodeoxycholic acid (UDCA) are currently available. However, none of these results in an optimal bioavailability oi the active ingredient as a function of the absorpt ion windows for bile acids found at the gastroduodenal level. Nonsatur ated passive absorption of bile acids occurs at these sites, while abs orption in the rest of the intestinal tract is less consistent as it i s limited by the presence of carriers. These considerations led to the development of an original delayed-release formulation of UDCA using the bioadhesive technique. This allows a longer residence time at the appropriate sites and hence a higher passive absorption of UDCA. The r esults of this pharmacokinetic study, which compared the new formulati on with a traditional PH-dependent sequential release formulation, dem onstrated that the new formulation had a greater area under the curve (AUG) during a 24 h period, when compared with that oi the reference d rug, reaching statistically significant values (p <0.01) within the fi rst 12h.