发明名称 STABILIZED AMOXICILLIN INCLUSION COMPLEX
摘要 PROBLEM TO BE SOLVED: To obtain an amoxicillin preparation which is stabilized, namely controls decomposition at a low pH and maintains antimicrobial activity by using an inclusion complex of amoxicillin with a cyclodextrin (derivative). SOLUTION: An inclusion complex of amoxicillin with a cyclodextrin, preferablyβ-cyclodextrin,γ-cyclodextrin or a cyclodextrin derivative, preferably dimethyl-β-cyclodextrin is used. The inclusion complex is obtained by formulating an aqueous solution containing a fixed amount of a cyclodextrin (derivative) with amoxicillin in an amount of corresponding molar ratio directly as powder or as a solution dissolved in an organic solvent such as ethanol, acetone, etc., stirring and, if required, removing impurities. In the case of obtaining as a solid substance, a small amount of water is added to the mixture and may be lyophilized. The formulating molar ratio of amoxicillin to the cyclodextrin (derivative) is preferably 1:0.3-3.
申请公布号 JP2001058994(A) 申请公布日期 2001.03.06
申请号 JP19990232488 申请日期 1999.08.19
申请人 EISAI CO LTD 发明人 TOMONO KAZUO;UEDA HARUHISA;NAGAI TSUNEJI;GOTO HIROKO;SUZUKI TOYOJI
分类号 C07D499/68;A61K31/43;A61P1/04;A61P31/00;C08B37/16;(IPC1-7):C07D499/68 主分类号 C07D499/68
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