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Control over Polymorph Formation of Polydatin in Binary Solvent System and Structural Characterization.
Journal of Pharmaceutical and Biomedical Analysis ( IF 3.1 ) Pub Date : 2020-03-17 , DOI: 10.1016/j.jpba.2020.113260
Ningbo Gong 1 , Xue Wang 1 , Ying Wang 1 , Shiying Yang 1 , Junke Song 2 , Yang Lu 1 , Guanhua Du 2
Affiliation  

Polydatin is a natural product used for anti-oxidant, anti-inflammatory and anti-tumor purposes, and often added in medicine, nutraceutical, cosmetics, and dietary supplement. Polymorphism is a key feature of solid-state pharmaceutical products. Polymorphic modifications may exhibit different physical and chemical properties. Here we report two different polymorphs, and the amorphous form of Polydatin. Polymorphs were prepared in binary solvent system. The crystal structures of the two forms were revealed for the first time. The structure and 3D packing were determined with single crystal X-ray diffraction analysis. The batch consistency and stability were identified with Powder X-ray diffraction analysis. Various functional groups present in the polymorphs were analyzed with fourier transform infrared spectroscopic method. The thermal properties were investigated with DSC and TGA. HPLC-MS was used for the pharmacokinetic study. Results show that form B has the faster absorption, and can be maintained in animal bodies for a longer time than form A.



中文翻译:

二元体系中多苷的多晶型物形成控制及结构表征。

Polydatin是一种天然产品,用于抗氧化剂,消炎药和抗肿瘤药,通常添加到药物,营养保健品,化妆品和膳食补充剂中。多态性是固态药物产品的关键特征。多晶型修饰可表现出不同的物理和化学性质。在这里,我们报告了两种不同的多晶型物,以及无定形的Polydatin。在二元溶剂系统中制备了多晶型物。首次揭示了两种形式的晶体结构。用单晶X射线衍射分析确定结构和3D堆积。用粉末X射线衍射分析鉴定批料的一致性和稳定性。用傅立叶变换红外光谱法分析了多晶型物中存在的各种官能团。用DSC和TGA研究热性能。HPLC-MS用于药代动力学研究。结果表明,形式B具有比形式​​A更快的吸收,并且可以在动物体内保持更长的时间。

更新日期:2020-03-17
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