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采用共研磨法制备非诺贝特环糊精包合物并使用互补分析工具监测该过程

Cyclodextrin Complexation of Fenofibrate by Co-Grinding Method and Monitoring the Process Using Complementary Analytical Tools.

作者信息

Kondoros Balázs Attila, Berkesi Ottó, Tóth Zsolt, Aigner Zoltán, Ambrus Rita, Csóka Ildikó

机构信息

Faculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös Str. 6, H-6720 Szeged, Hungary.

Faculty of Science and Informatics, Department of Physical Chemistry and Materials Science, University of Szeged, Béla Rerrich Square 1, H-6720 Szeged, Hungary.

出版信息

Pharmaceutics. 2022 Jun 23;14(7):1329. doi: 10.3390/pharmaceutics14071329.

Abstract

Solvent-free preparation types for cyclodextrin complexation, such as co-grinding, are technologies desired by the industry. However, in-depth analytical evaluation of the process and detailed characterization of intermediate states of the complexes are still lacking in areas. In our work, we aimed to apply the co-grinding technology and characterize the process. Fenofibrate was used as a model drug and dimethyl-β-cyclodextrin as a complexation excipient. The physical mixture of the two substances was ground for 60 min; meanwhile, samples were taken. A solvent product of the same composition was also prepared. The intermediate samples and the final products were characterized with instrumental analytical tools. The XRPD measurements showed a decrease in the crystallinity of the drug and the DSC results showed the appearance of a new crystal form. Correlation analysis of FTIR spectra suggests a three-step complexation process. In vitro dissolution studies were performed to compare the dissolution properties of the pure drug to the products. Using a solvent-free production method, we succeeded in producing a two-component system with superior solubility properties compared to both the active ingredient and the product prepared by the solvent method. The intermolecular description of complexation was achieved with a detailed analysis of FTIR spectra.

摘要

用于环糊精络合的无溶剂制备类型,如共研磨,是该行业所期望的技术。然而,在该领域仍缺乏对该过程的深入分析评估以及对络合物中间状态的详细表征。在我们的工作中,我们旨在应用共研磨技术并对该过程进行表征。非诺贝特用作模型药物,二甲基-β-环糊精用作络合辅料。将两种物质的物理混合物研磨60分钟;同时,采集样品。还制备了相同组成的溶剂产物。用仪器分析工具对中间样品和最终产物进行表征。X射线粉末衍射(XRPD)测量表明药物的结晶度降低,差示扫描量热法(DSC)结果显示出现了一种新的晶型。傅里叶变换红外光谱(FTIR)的相关分析表明存在三步络合过程。进行体外溶出度研究以比较纯药物与产物的溶出特性。使用无溶剂生产方法,我们成功制备了一种两组分体系,其溶解性优于活性成分和通过溶剂法制备产物。通过对FTIR光谱的详细分析实现了络合的分子间描述。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0007/9319411/67514d8b9141/pharmaceutics-14-01329-g001.jpg

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