Pluronic F-127 gels as a novel vehicle for rectal administration of indomethacin.

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Abstract
Polyoxyethylene-polyoxypropylene surface-active block copolymers (Pluronics) were evaluated as a vehicle for rectal administration of indomethacin. The effects of the concentration of Pluronic F-127, temperature, and drug concentration on the drug release were studied by means of an in vitro release method using a cellulose membrane. With increasing concentration of Pluronic F-127 in the vehicle, a corresponding decrease in the apparent release rate of the drug occurred. The apparent release rate increased with increasing temperature from 20 to 44.degree. C. Increase in drug concentration increased the drug release rate. Indomethacin gel preparations made by dissolving the drug in Pluronic F-127 aqueous gel were administered rectally to rabbits and the drug plasma levels were compared with those after rectal administration of commercial suppositories. When a commercial suppository was given to rabbits, the plasma concentration reached the maximum level 30 min after administration. On the other hand, the gel preparation did not show a sharp peak of plasma concentration and produced a sustained plateau level of indomethacin from 15 min to 10 h without a lag time. Thus, it appeared that indomethacin preparations based on Pluronic F-127 aqueous gel may be practically useful as a rectal preparation with prolonged action and with reduced side effects.

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