姚 静, 时念秋, 王杏林. 共无定型药物系统的研究进展J. 药学学报, 2013,48(5): 648-654.
引用本文: 姚 静, 时念秋, 王杏林. 共无定型药物系统的研究进展J. 药学学报, 2013,48(5): 648-654.
YAO Jing, SHI Nian-qiu, WANG Xing-lin. The development of co-amorphous drug systemsJ. 药学学报, 2013,48(5): 648-654.
Citation: YAO Jing, SHI Nian-qiu, WANG Xing-lin. The development of co-amorphous drug systemsJ. 药学学报, 2013,48(5): 648-654.

共无定型药物系统的研究进展

The development of co-amorphous drug systems

  • 摘要:

    将两种水难溶性的晶态药物通过球磨、淬冷或低温研磨的方法制成共无定型药物系统, 既能提高药物的稳定性及溶出速率, 又能减少单一药物不良反应的发生, 从而解决难溶性药物联合用药面临的诸多问题。通 过差示扫描量热法 (differential scanning calorimetry, DSC)X射线粉末衍射法 (X-ray powder diffraction, XRPD)、拉曼光谱 (raman spectroscopy, RS) 和傅里叶转换红外光谱 (fourier transform infrared spectroscopy, FT-IR) 等可以验证共无定型药物系统的形成情况和分子间相互作用。共无定型药物系统的稳定性由它的玻璃化转变温度 (glass transition temperature, Tg) 及分子间相互作用共同决定。依据Gordon-Taylor方程和Flory-Huggins方程可以分别推算理论Tg值和相互作用参数x, 从而在分子水平上对共无定型药物系统进行理论分析。共无定型药物系统的出现为联合用药提供了新的思路。

     

    Abstract:

    Converting two poorly water-soluble crystalline drugs to co-amorphous drug systems by ball milling, quench-cooling, or cryo-milling method can improve stability of the drug, enhance dissolution rates, and reduce adverse reactions of the single drug.  Co-amorphous system has been used to solve problems of co-administration of medicines.  Formation and intermolecular interactions of co-amorphous drug systems may be verified by differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), raman spectroscopy (RS) and fourier transform infrared spectroscopy (FT-IR).  Stability of co-amorphous drug systems is influenced by their glass transition temperature (Tg) and intermolecular interactions.  The theoretical Tg values and the interaction parameter x are calculated by Gordon-Taylor equation and the Flory-Huggins equation, respectively.  Thus, co-amorphous drug systems are analyzed theoretically at molecular level.  Co-amorphous drug systems provide a new sight for the co-administration of medicines.

     

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