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Inhibition of the Vapor-Mediated Phase Transition of the High Temperature Form of Pyrazinamide

机译：抑制吡嗪酰胺的高温形式的蒸汽介导的相转变

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摘要

Tailor-made additives can prove an effective method to prolong the lifetime of metastable forms of pharmaceutical compounds by surface stabilization. Pyrazinamide (PZA) is a pharmaceutical compound with four polymorphic forms. The high temperature γ form, which can be produced by spray drying or sublimation growth, is metastable at room temperature and transforms within days when produced by spray drying, and within several months up to years for single crystals produced by sublimation. However, when PZA is cospray dried with 1,3-dimethylurea (DMU), it has been reported to remain in its γ form for several years. Scanning electron microscopy (SEM) images reveal that the phase transition from γ-PZA to the low temperature forms involves a vapor-mediated recrystallization, while the reverse phase transition upon heating is a nucleation-and-growth solid–solid phase transition. The lifetime-extending effect of DMU on spray-dried PZA has been investigated in more detail and compared with high-energy ball milling of sublimation-grown γ-PZA crystals. Co-ball milling of PZA and DMU is found to extend the lifetime of the high temperature form of PZA to a few months, while separate ball milling leads to an extension of merely a few weeks. DMU acts as an additive that most likely stabilizes the surface of γ-PZA, which would reduce the vapor pressure of PZA, thereby reducing the transition rate. Alternatively, DMU could prevent nucleation of low temperature forms of PZA.
机译：定制的添加剂可以证明通过表面稳定延长亚稳态形式的亚稳态形式的寿命的有效方法。吡嗪酰胺（PZA）是一种具有四种多态性形式的药物化合物。通过喷雾干燥或升华生长可以生产的高温γ形式，在室温下衡量，通过喷雾干燥产生的天数，并且在升华产生的单个晶体的几个月内几个月内变化。然而，当PZA用1,3-二甲基脲（DMU）干燥时，据报道，据报道，持续物质留在几年内。扫描电子显微镜（SEM）图像表明，从γ-PZA到低温形式的相转变涉及蒸汽介导的重结晶，而加热时的反相转变是成核 - 生长固体相转变。 DMU对喷雾干燥PZA的寿命延伸效果已经更详细地研究，并与升华生长的γ-PZA晶体的高能球铣削相比。发现PZA和DMU的共球铣削将PZA的高温形式的寿命延伸到几个月，而单独的球磨导致仅仅几周的延伸。 DMU作为添加剂，最有可能稳定γ-PZA的表面，这将降低PZA的蒸气压，从而降低过渡率。或者，DMU可以防止核细胞的核心的PZA。

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  • 来源
    《Crystal growth & design》 |2018年第2期|共8页
  • 作者

    M. M. H. Smets; G. Baaklini; A. Tijink; L. Sweers; C. H. F. Vossen; C. Brandel; H. Meekes; H. M. Cuppen; G. Coquerel;

  • 作者单位

    Institute for Molecules and Materials Radboud University Heyendaalseweg 135 6525 AJ Nijmegen The Netherlands;

    Normandie Université Laboratoire SMS-EA3233 Université de Rouen F-76821 Mont-Saint-Aignan France;

    Institute for Molecules and Materials Radboud University Heyendaalseweg 135 6525 AJ Nijmegen The Netherlands;

    Institute for Molecules and Materials Radboud University Heyendaalseweg 135 6525 AJ Nijmegen The Netherlands;

    Institute for Molecules and Materials Radboud University Heyendaalseweg 135 6525 AJ Nijmegen The Netherlands;

    Normandie Université Laboratoire SMS-EA3233 Université de Rouen F-76821 Mont-Saint-Aignan France;

    Institute for Molecules and Materials Radboud University Heyendaalseweg 135 6525 AJ Nijmegen The Netherlands;

    Institute for Molecules and Materials Radboud University Heyendaalseweg 135 6525 AJ Nijmegen The Netherlands;

    Normandie Université Laboratoire SMS-EA3233 Université de Rouen F-76821 Mont-Saint-Aignan France;

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