Indomethacin and indomethacin sustained release—A comparison of their pharmacokinetic profiles

Abstract

The data reviewed here show that INDOCIN ® SR (Indomethacin, MSD) exhibits good sus- tained-release characteristics. It produces more sustained plasma levels and shows no evidence of dose-dumping. Bioavailability is equivalent to that of three consecutive doses of conventional indomethacin capsules. Results of several controlled clinical studies 31–33 are consistent with the pharmacokinetic observations. It is generally believed that an ideal sustained-release product should release its active ingredient in a zero-order fashion similarly to a continuous constant-rate intravenous infusion. Under these conditions, the absorption rate and the resultant plasma levels would appear flat and constant for a specified time interval. Because of the sporadic nature of the enterohepatic recirculation, such an ideal goal cannot be achieved with indomethacin. Nevertheless, clinical data suggest that INDOCIN SR when administered once or twice daily, is comparable to conventional capsules in tolerability and efficacy. 31–33