title: In-vitro and clinical evaluation of an oral mucosal adhesive film containing indomethacin.
abstract: To develop a new mucoadhesive film containing an analgesic combining clinical efficacy and patient comfort, we prepared and evaluated a two-layered film consisting of an adhesive layer containing indomethacin (IM) as the active ingredient and carboxyvinyl polymer (CP) as a bonding agent and a nonadhesive layer containing polyethylene glycol (PEG) to improve film texture. In in vitro and in vivo adhesive tests, the optimal concentration of CP that could be applied to the mucous membrane was 0.2% or 0.3%. Stability testing determined that the optimal storage conditions and expiration period were 4 degrees C without shade and 4 weeks, respectively. The film was clinically evaluated in patients with oral pain. IM at concentrations of 0.5% and 1% provided optimum analgesic effects, and the effects were the greatest in the 1% IM group. The addition of PEG to the nonadhesive layer reduced the number of patients experiencing discomfort at the site where the film was applied. Therefore this film formulation may be useful for local analgesic application due to its low dose requirement, moderate adhesion, and comfortable texture.
authors.affiliation: Division of Medical and Pharmaceutical Sciences-II, Faculty of Pharmaceutical Sciences, Teikyo University, Sagamihara City, Japan.
authors.forename: Kazuyo
authors.initials: K
authors.lastname: Takeuchi
authors.forename: Machiko
authors.initials: M
authors.lastname: Watanabe
authors.forename: Mashiho
authors.initials: M
authors.lastname: Yanagi
authors.forename: Isao
authors.initials: I
authors.lastname: Murakami
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Hosono
authors.forename: Satoru
authors.initials: S
authors.lastname: Nishizawa
authors.forename: Yoshiho
authors.initials: Y
authors.lastname: Chigono
authors.forename: Shinichi
authors.initials: S
authors.lastname: Hirabayashi
authors.forename: Juzo
authors.initials: J
authors.lastname: Matsuda
authors.forename: Keiko
authors.initials: K
authors.lastname: Yamaoka
authors.forename: Keizo
authors.initials: K
authors.lastname: Inoue
mesh_terms: D000268:Adhesiveness; D000284:Administration, Oral; D000700:Analgesics / Q000008:administration & dosage* / Q000009:adverse effects; D002482:Cellulose / Q000031:analogs & derivatives; D002626:Chemistry, Pharmaceutical; D004304:Dosage Forms; D004355:Drug Stability; D006801:Humans; D007213:Indomethacin / Q000008:administration & dosage* / Q000009:adverse effects; D009061:Mouth Mucosa; D010146:Pain / Q000188:drug therapy*; D011092:Polyethylene Glycols; D012995:Solubility; D016896:Treatment Outcome
chemical_list: D000700:Analgesics; D004304:Dosage Forms; D011092:Polyethylene Glycols; D002482:Cellulose; C008079:hydroxypropylcellulose; D007213:Indomethacin