イソニアジドおよびその関連化合物の安定性(第5報) : イソニアジドの酸化的分解について

概要

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The oxidative degradation of isoniazid (INAH) with Cu^<2+> was investigated. The reaction products were isonicotinic acid, isonicotinamide, 1,2-diisonicotinoylhydrazine, and isonicotinaldehydeisonicotinoylhydrazone. In the low pH region, the sum of the molar concentration of INAH and degradation products in the solution was equal to the initial molar concentration of INAH in a given kinetic run. It was found that INAH forms chelates with Cu^<2+> in the 1 : 1 and 1 : 2 ratio and these chelates are degraded by a first-order process, and that the apparent degradation velocity is determined by the concentration of each chelate compound, INAH-Cu^+ and INAH-Cu-INAH, and each degradation rate constant. The activation energy of the degradation reaction of INAH-Cu^+ and INAH-Cu-INAH was 16.3 and 12.3 kcal/mole, respectively. The degradation of INAH with Cu^<2+> is accomplished by two steps ; first, Cu^<2+> chelates with INAH and pulls the electron and then cleaves C=N or N-N bonds. The effect as stabilizer was investigated with few compounds which can be used as pharmaceutics. It was found that EDTA is the most effective and that citric acid has some effect.
公益社団法人日本薬学会の論文
1971-01-25