Conversion Characteristics of the Conjugates of Mitomycin C with Estradiol and Estradiol Benzoate in Various pH Media
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概要
- 論文の詳細を見る
Novel conjugates of mitomycin C(MMC) with 4-[3-benzoyloxy-1,3,5(10)-estratrien-17β-yloxycarbonyl]butyric acid (EB-glu) and 4-[3-hydroxy-1,3,5(10)-estratrien-17β-yloxycarbonyl]butyric acid (E-glu) at the 1a-N position, abbreviated as EB-glu-MMC and E-Glu-MMC, respectively, were synthesized, and the kinetics on their decomposition and the MMC regeneration in various buffered solutions were investigated. EB-glu was synthesized by the reaction of estradiol benzoate (EB) and glutaric anhydride, and EB-glu-MMC was obtained by the condensation of MMC with EB-glu using N, N'-carbonyldiimidazole. E-glu was obtained by the alkaline hydrolysis of EB-glu, and E-glu-MMC was synthesized by the condensation of MMC with E-glu using N, N'-carbonyldiimidazole. The buffered solutions of pH 4,6,7,7.4,9 and 11 were used as buffered systems. In the stability study, EB-glu-MMC and E-glu-MMC were dissolved in a mixture of the buffer and propylene glycol (1 : 1,v/v) and incubated at 37℃. E-glu-MMC and EB-glu-MMC were subjected to degradation at pH4,and further, their degradation became faster with the increase of pH at the basic condition. MMC was regenerated more easily with the increase of pH, and its regeneraiton was not detected at pH4. The analysis using the pseudo-first order kinetics elucidated the conversion rates. The direct conversion rate from EB-glu-MMC to MMC was found to be close to the regeneration rate from E-glu-MMC to MMC.
- 公益社団法人日本薬学会の論文
- 1997-08-15
著者
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Onishi Hiraku
Department Of Drug Delivery Research Hoshi University
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Onishi Hiraku
Department Of Clinical Pharmacy Hoshi University
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Machida Yoshiharu
Department Of Drug Delivery Research Hoshi University
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Machida Yoshiharu
Dep. Of Drug Delivery Res. Hoshi Univ.
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Machida Yoshiharu
Department Of Clinical Pharmacy Hoshi University
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ISHIKI Nobuyuki
Department of Drug Delivery Research, Hoshi University
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Ishiki Nobuyuki
Department Of Drug Delivery Research Hoshi University
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