Pluronic F-127 Gels as a NOvel Vehicle for Rectal Administration of Indomethacin

概要

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Polyoxyethylene-polyoxypropylene surface-active block copolymers (Pluronics^(R)) 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℃. 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.
公益社団法人日本薬学会の論文
1986-04-25