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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.

Abstract
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.
AuthorsH Tozaki, T Fujita, T Odoriba, A Terabe, T Suzuki, C Tanaka, S Okabe, S Muranishi, A Yamamoto
JournalLife sciences (Life Sci) Vol. 64 Issue 13 Pg. 1155-62 ( 1999) ISSN: 0024-3205 [Print] Netherlands
PMID10210278 (Publication Type: Journal Article)
Chemical References
  • Capsules
  • Pentanoic Acids
  • Pyridines
  • Chitin
  • Trinitrobenzenesulfonic Acid
  • Chitosan
  • Peroxidase
  • Thromboxane-A Synthase
  • ridogrel
Topics
  • Animals
  • Capsules
  • Chitin (administration & dosage, analogs & derivatives)
  • Chitosan
  • Colitis, Ulcerative (drug therapy)
  • Colon (drug effects)
  • Male
  • Pentanoic Acids (administration & dosage)
  • Peroxidase (metabolism)
  • Pyridines (administration & dosage)
  • Rats
  • Rats, Wistar
  • Thromboxane-A Synthase (antagonists & inhibitors)
  • Trinitrobenzenesulfonic Acid

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