一种新型卡马西平共晶的合成及表征
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山东省自然基金;山东省泰山学者研究基金资助项目


A New Pharmaceuticals Cocrystal of Carbamazepine Synthesis and Characterization
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Nature Fund of Shandong Province;Tai-Shan Scholar Research Fund of Shandong Province of China

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    摘要:

    以卡马西平(CBZ)作为药物活性成分(API),以没食子酸甲酯(MTG)作为共晶形成物(CCF),在室温条件下制得一种新的药物共晶CBZ-MTG。通过X-射线单晶衍射测得了其晶体结构,并进行了红外光谱、X-射线粉末衍射、热重分析和差示扫描量热的表征。此外,利用HPLC测得其溶解性质并测试了稳定性,其共晶在溶解性,稳定性和生物利用度上都有了明显的改观。各种结构性质的表征,为其在药物领域的应用提供了基础数据和理论基础,为卡马西平-没食子酸甲酯共晶化合物作为药物应用及在制剂领域提供了新的选择。

    Abstract:

    A new drug cocrystal CBZ-MTG was synthesed by using carbamazepine (CBZ) as a active pharmaceutical ingredient (API) and methyl gallate (MTG) as a cocrystal coformer (CCF) at room temperature. The crystal structure was investigated by X-ray single crystal diffraction, and the cocrystal was characterized by infrared spectroscopy, X-ray powder diffraction, thermogravimetric analysis and differential scanning calorimetry. In addition, the solubility was measured by HPLC and the stability was also tested. The cocrystal have been significantly improved in the aspect of solubility and bioavailability. The characterization of various structural properties provides the basic data and theoretical basis for its application in the field of drugs, and provides a new choice for carbamazepine-methyl gallate cocrystal as drug applications and in the preparation field.

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王冠宇,李大成.一种新型卡马西平共晶的合成及表征[J].精细化工,2018,35(3):

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  • 收稿日期:2017-02-21
  • 最后修改日期:2017-04-12
  • 录用日期:2017-07-27
  • 在线发布日期: 2018-03-15
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