Cyclodextrin Complexation of Fenofibrate by Co-Grinding Method and Monitoring the Process Using Complementary Analytical Tools
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...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-06-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/7/1329 |
| _version_ | 1797444445542547456 |
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| author | Balázs Attila Kondoros Ottó Berkesi Zsolt Tóth Zoltán Aigner Rita Ambrus Ildikó Csóka |
| author_facet | Balázs Attila Kondoros Ottó Berkesi Zsolt Tóth Zoltán Aigner Rita Ambrus Ildikó Csóka |
| author_sort | Balázs Attila Kondoros |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-03-09T13:11:42Z |
| format | Article |
| id | doaj.art-8306eb5da431455485f2df8e61fd121b |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T13:11:42Z |
| publishDate | 2022-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-8306eb5da431455485f2df8e61fd121b2023-11-30T21:41:03ZengMDPI AGPharmaceutics1999-49232022-06-01147132910.3390/pharmaceutics14071329Cyclodextrin Complexation of Fenofibrate by Co-Grinding Method and Monitoring the Process Using Complementary Analytical ToolsBalázs Attila Kondoros0Ottó Berkesi1Zsolt Tóth2Zoltán Aigner3Rita Ambrus4Ildikó Csóka5Faculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös Str. 6, H-6720 Szeged, HungaryFaculty of Science and Informatics, Department of Physical Chemistry and Materials Science, University of Szeged, Béla Rerrich Square 1, H-6720 Szeged, HungaryDepartment of Medical Physics and Informatics, University of Szeged, Korányi Fasor 9, H-6720 Szeged, HungaryFaculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös Str. 6, H-6720 Szeged, HungaryFaculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös Str. 6, H-6720 Szeged, HungaryFaculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös Str. 6, H-6720 Szeged, HungarySolvent-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.https://www.mdpi.com/1999-4923/14/7/1329DIMEBmolecular complexationsolvent-free methodXRPDDSCFT-IR |
| spellingShingle | Balázs Attila Kondoros Ottó Berkesi Zsolt Tóth Zoltán Aigner Rita Ambrus Ildikó Csóka Cyclodextrin Complexation of Fenofibrate by Co-Grinding Method and Monitoring the Process Using Complementary Analytical Tools Pharmaceutics DIMEB molecular complexation solvent-free method XRPD DSC FT-IR |
| title | Cyclodextrin Complexation of Fenofibrate by Co-Grinding Method and Monitoring the Process Using Complementary Analytical Tools |
| title_full | Cyclodextrin Complexation of Fenofibrate by Co-Grinding Method and Monitoring the Process Using Complementary Analytical Tools |
| title_fullStr | Cyclodextrin Complexation of Fenofibrate by Co-Grinding Method and Monitoring the Process Using Complementary Analytical Tools |
| title_full_unstemmed | Cyclodextrin Complexation of Fenofibrate by Co-Grinding Method and Monitoring the Process Using Complementary Analytical Tools |
| title_short | Cyclodextrin Complexation of Fenofibrate by Co-Grinding Method and Monitoring the Process Using Complementary Analytical Tools |
| title_sort | cyclodextrin complexation of fenofibrate by co grinding method and monitoring the process using complementary analytical tools |
| topic | DIMEB molecular complexation solvent-free method XRPD DSC FT-IR |
| url | https://www.mdpi.com/1999-4923/14/7/1329 |
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