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Controlling Polymorphism in Pharmaceutical Compounds Using Solution Shearing
Crystal Growth & Design ( IF 3.8 ) Pub Date : 2018-01-11 00:00:00 , DOI: 10.1021/acs.cgd.7b01686
Stephanie M. Guthrie 1 , Detlef-M. Smilgies 2 , Gaurav Giri 1
Affiliation  

In this work, two model pharmaceutical compounds, glycine and acetaminophen, were crystallized using a flow coating technique termed solution shearing to create thin films with controllable polymorphism. Controlling polymorphism in pharmaceutical compounds can provide optimized solubility and bioavailability. Thin films of glycine and acetaminophen were obtained using a simple flow coating method, and these films were characterized using cross polarized optical microscopy and grazing incidence X-ray diffraction. Films crystallized as different polymorphs (α and β for glycine and form I and form II for acetaminophen) by controlling processing temperature and shearing speed. The amorphous phase of acetaminophen was also stabilized, and the kinetic transformation to the metastable form II was studied. We show that one-dimensional confinement plays a significant role in stabilizing metastable polymorphs and amorphous phases. Solution shearing has the potential to be used as a high throughput technique to screen polymorphs in industry.

中文翻译:

使用溶液剪切控制药物化合物中的多态性

在这项工作中,使用称为溶液剪切的流涂技术将两种模型药物化合物甘氨酸和对乙酰氨基酚结晶,以产生具有可控多态性的薄膜。控制药物化合物中的多态性可以提供最佳的溶解度和生物利用度。使用简单的流涂方法获得甘氨酸和对乙酰氨基酚薄膜,并使用交叉偏振光学显微镜和掠入射X射线衍射对这些薄膜进行表征。通过控制加工温度和剪切速度,薄膜结晶为不同的多晶型物(甘氨酸为α和β,对乙酰氨基酚为晶型I和晶型II)。对乙酰氨基酚的无定形相也被稳定,并研究了向亚稳态晶型II的动力学转化。我们表明,一维约束在稳定亚稳多晶型物和非晶相中起着重要作用。溶液剪切有潜力用作工业中筛选多晶型物的高通量技术。
更新日期:2018-01-11
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