Novel submicronized rebamipide liquid with moderate viscosity: significant effects on oral mucositis in animal models.
This study aimed at developing a novel rebamipide liquid for an effective treatment of oral mucositis. The healing effects of a variety of liquids comprising submicronized rebamipide crystals were investigated using a rat cauterization-induced oral ulcer model. Whereas 2% rebamipide liquid comprising micro-crystals did not exhibit significant curative effect, 2% rebamipide liquids comprising submicronized crystals with moderate viscosities exhibited healing effects following intra-oral administration. The 2% and 4% optimized rebamipide liquids showed significant healing effects in the rat oral ulcer model (p<0.01). In addition, in the rat radiation-induced glossitis model, whereby the injury was caused to the tongue by exposing only around the rat's snout to a 15 Gy of X-irradiation, the 2% optimized rebamipide liquid significantly reduced the percent area of ulcerated injury (p<0.05). In conclusion, the submicronized rebamipide liquid with moderate viscosity following intra-oral administration showed better both healing effect in the rat oral ulcer model and preventive effect in the rat irradiation-induced glossitis model.
Department of Pharmacokinetics and Biopharmaceutics, Subdivision of Biopharmaceutical Sciences,  Institute of Health Biosciences, The University of Tokushima.
Takako
T
Nakashima
Nobutomo
N
Sako
Takakuni
T
Matsuda
Naoya
N
Uematsu
Kazushi
K
Sakurai
Tatsuhiro
T
Ishida
D000284:Administration, Oral; D000409:Alanine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000627:therapeutic use; D000818:Animals; D000897:Anti-Ulcer Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000627:therapeutic use*; D002425:Cautery; D004195:Disease Models, Animal; D004337:Drug Carriers / Q000008:administration & dosage; D005928:Glossitis / Q000188:drug therapy*; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage; D019226:Oral Ulcer / Q000188:drug therapy; D015363:Quinolones / Q000008:administration & dosage / Q000737:chemistry* / Q000627:therapeutic use*; D051381:Rats; D013280:Stomatitis / Q000188:drug therapy*; D014783:Viscosity; D014965:X-Rays
D000897:Anti-Ulcer Agents; D004337:Drug Carriers; D015363:Quinolones; C052785:rebamipide; D000409:Alanine