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

• Published in: Chemical & pharmaceutical bulletin Vol. 34; no. 4; pp. 1801 - 1808
• Main Authors: MIYAZAKI, SHOZO, YOKOUCHI, CHIZUKO, NAKAMURA, TSUGUYA, HASHIGUCHI, NORIO, HOU, WEI-MIN, TAKADA, MASAHIKO
• Format: Journal Article
• Language: English
• Published: Tokyo The Pharmaceutical Society of Japan 1986; Maruzen
• Subjects: Animals; Biological and medical sciences; Gels; General pharmacology; Indomethacin - administration & dosage; Indomethacin - blood; Male; Medical sciences; Pharmaceutical technology. Pharmaceutical industry; Pharmaceutical Vehicles; Pharmacology. Drug treatments; Poloxalene; Polyethylene Glycols; Rabbits; rectal delivery system; Suppositories; Rectal form; Controlled release form; Wetting agent; Vehicle(excipient); Rabbit; Lagomorpha; Property formulation relationship; Non steroidal antiinflammatory agent; Ethylene oxide polymer; Colloidal gel; Vertebrata; Mammalia; Absorption; Animal; Propylene oxide polymer
• ISSN: 0009-2363; 1347-5223
• DOI: 10.1248/cpb.34.1801

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°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.