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7699176 
Journal Article 
Colon-specific delivery of R68070, a new thromboxane synthase inhibitor, using chitosan capsules: therapeutic effects against 2,4,6-trinitrobenzene sulfonic acid-induced ulcerative colitis in rats 
Tozaki, H; Fujita, T; Odoriba, T; Terabe, A; Suzuki, T; Tanaka, C; Okabe, S; Muranishi, S; Yamamoto, A 
1999 
Life Sciences
ISSN: 0024-3205
EISSN: 1879-0631 
PERGAMON-ELSEVIER SCIENCE LTD 
OXFORD 
64 
13 
1155-1162 
English 
The objective of this study was to estimate the therapeutic effects of R68070, a new thromboxane synthase inhibitor, on 2,4,6-trinitrobenzenesulfonic acid sodium salt (TNBS)-induced ulcerative colitis in rats. We also examined the acceleration of the healing effect of R68070 with chitosan capsules to achieve its colon-specific delivery. The colonic injury and inflammation were assessed by measuring the myeloperoxidase (MPO) activities, colon wet weight/body weight (C/B) ratio and the damage score, respectively. These markers were decreased by the oral administration of R68070 with chitosan capsules and carboxymethyl-cellulose (CMC) suspension. The therapeutic effects of R68070 against ulcerative colitis were observed in both dosage forms in a dose dependent manner. In addition, its therapeutic effects were increased by the use of chitosan capsules, compared with CMC suspension. These results suggest that chitosan capsule might be a very useful dosage form for the colon-specific delivery of R68070 as an anti-inflammatory drug and for the therapy of ulcerative colitis.