Controlled indomethacin release from mucoadhesive film: in vitro and clinical evaluations.

Makoto Tanabe, Machiko Watanabe, Mashiho Yanagi, Satoru Nishizawa, Yoshiho Chigono, Juzo Matsuda, Keiko Yamaoka, Keizo Inoue

Division of Medical and Pharmaceutical Sciences-II, Faculty of Pharmaceutical Sciences, Teikyo University, Sagamiko, Sagamihara City, Japan.

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan 2008 Nov

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To develop a film formulation allowing controlled release for long-term analgesia, we selected ethyl cellulose (EC) as a novel additive, prepared a film formulation using indomethacin (IM film), and evaluated it in vitro and clinically. In the in vitro experiments, the effects of the EC concentration on the release rate of IM and on the adhesion force to the mucous membrane were investigated. The addition of 10% EC resulted in more sustained slow release compared with no EC, and the adhesion of the film with 10% EC added was similar to that of films containing carboxyvinyl polymer, which we reported previously showed significantly increased adhesion. A two-layered film consisting of an adhesive layer with 2% or 1% IM and 10% EC and a nonadhesive layer with 2% polyethylene glycol as a softening agent, was investigated for clinical use. Film consisting of an adhesive layer with 2% IM and 10% EC exhibited rapid onset of potent analgesia and was expected to prolong the duration of analgesia. These results suggest that IM film with EC added may be useful clinically, since it shows both immediate analgesic effects and prolonged duration of release.

Citation

Makoto Tanabe, Machiko Watanabe, Mashiho Yanagi, Satoru Nishizawa, Yoshiho Chigono, Juzo Matsuda, Keiko Yamaoka, Keizo Inoue. Controlled indomethacin release from mucoadhesive film: in vitro and clinical evaluations. Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan. 2008 Nov;128(11):1673-9