Rectal Delivery of Antiinflammatory Drugs. IV. Effect of Amino Acids on the Change in the Rectal Mucosa induced by Diclofenac Sodium

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The effect of the concurrent administration of amino acid (s) with diclofenac sodium on mucosal damage was investigated in rats. An administration of the base alone (Witepsol H-15) induced an only slight desquamation of epithelial cells at the luminal border, without any other changes in the mucosa. However severe histological damage was observed after administration of diclofenac sodium in Witepsol H-15. On the other hand, the concurrent administration of diclofenac sodium with L-form amino acids decreased the damage to the rectal mucosa. The L-forms of methionine and phenylalanine were the most effective, but in the protective effect of their D-forms on the rectal mucosa was much less. Rectal absorption of diclofenac sodium was investigated when it was administered with amino acids in rabbits, dogs and rats. The absorption was not influenced by the concurrent administration of amino acid (s).
社団法人日本薬学会の論文
1982-09-25