シクロデキストリン包接によるチアムリン注射時の局所刺激性の改善

概要

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To reduce the local irritation induced by intramuscular injection of tiamulin (TM), the cyclodextrin complexation was utilized. The inclusion complexations of TM with three cyclodextrins (α-, β-, γ-CyD) in aqueous solution and in solid phase were assessed by ultraviolet, circular dichroism, solubility method, thermal analyses and powder X-ray diffractometry. Effects of CyDs on in vitro hemolysis induced by TM were investigated as a representation of local irritation. The protective effects of CyDs against hemolysis caused by TM increased in the order of γ->β->α-CyD. The irritative effects of TM and its γ-CyD complex on the M. vastus lateralis of rabbits were studied on gross examination. TM showed a distinct discoloration of M. vastus lateralis with surrounding hemorrhagic area. The irritation of γ-CyD complex was found to be milder than that of TM itself.
社団法人日本薬学会の論文
1982-09-25