The Effects of Impurities on Crystallization of Polymorphs of a Drug Substance AE1-923

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  • Okamoto Masaki
    Department of Applied and Bioapplied Chemistry, Graduate School of Engineering, Osaka City University Fukui Research Institute, Ono Pharmaceutical Co., Ltd.
  • Hamano Masaya
    Fukui Research Institute, Ono Pharmaceutical Co., Ltd.
  • Igarashi Koichi
    Department of Applied and Bioapplied Chemistry, Graduate School of Engineering, Osaka City University
  • Ooshima Hiroshi
    Department of Applied and Bioapplied Chemistry, Graduate School of Engineering, Osaka City University

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  • Effects of Impurities on Crystallization of Polymorphs of a Drug Substance AE1 923

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The effects of seven kinds of impurities on the solvent-mediated transformation of crystal polymorphs of a drug substance AE1-923 were investigated. AE1-923 was developed for an indication of pollakiuria and pain. It has three polymorphs, namely the unstable A-form, the metastable B-form and the stable C-form. The impurities tested were the starting compounds, the reaction reagents and the intermediates in the synthesis of AE1-923. One of the impurities, an intermediate AE1-923ME (methylester of AE1-923), inhibited the solvent-mediated polymorph transformation of the B-form to the C-form, although the transformation of the A-form to the B-form was not inhibited. The other impurities had no effect on the two steps of polymorph transformation. The inhibitory effect of AE1-923ME that was evaluated by the overall transformation rate constant kc exponentially increased with an increase in the concentration of AE1-923ME. AE1-923ME of 0.5 wt% completely suppressed the nucleation of the stable C-form crystals. However, crystal growth of the C-form was not inhibited.

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