Novel Submicronized Rebamipide Liquid with Moderate Viscosity: Significant Effects on Oral Mucositis in Animal Models

被引:10
作者
Nakashima, Takako [1 ,2 ]
Sako, Nobutomo [3 ]
Matsuda, Takakuni [1 ,3 ]
Uematsu, Naoya [2 ]
Sakurai, Kazushi [2 ]
Ishida, Tatsuhiro [1 ]
机构
[1] Univ Tokushima, Inst Hlth Biosci, Subdiv Biopharmaceut Sci, Dept Pharmacokinet & Biopharmaceut, Tokushima 7708503, Japan
[2] Otsuka Pharmaceut Co Ltd, Inst New Drug Discovery 3, Tokushima 7710192, Japan
[3] Otsuka Pharmaceut Co Ltd, Formulat Res Inst, Tokushima 7710182, Japan
关键词
rebamipide; mucositis; submicronized; X-irradiation; liquid; METHIONYL-LEUCYL-PHENYLALANINE; HUMAN NEUTROPHILS; RATS; VOLUNTEERS; CYTOKINES;
D O I
10.1248/bpb.b13-01006
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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.
引用
收藏
页码:671 / 678
页数:8
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