Metastable Racemic Ibuprofen Supercooled Liquid
Amorphous solid dispersions are good candidates for improving solubility in water and the oral bioavailability of poorly water-soluble active pharmaceutical ingredients (APIs). Amorphous solids become supercooled liquids when the temperature reaches the glass transition temperature (T<sub>g<...
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2024-11-01
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| author | Tuanjia Li Wangchuan Xiao Shizhao Ren Rongrong Xue Fenghua Chen |
| author_facet | Tuanjia Li Wangchuan Xiao Shizhao Ren Rongrong Xue Fenghua Chen |
| author_sort | Tuanjia Li |
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| description | Amorphous solid dispersions are good candidates for improving solubility in water and the oral bioavailability of poorly water-soluble active pharmaceutical ingredients (APIs). Amorphous solids become supercooled liquids when the temperature reaches the glass transition temperature (T<sub>g</sub>). For APIs with low melting points, T<sub>g</sub> can be below room temperature, which makes it difficult to prepare long-term stable amorphous solids. Studies on the physicochemical properties of supercooled liquids shed light on the design of ASDs for APIs with low melting points. Racemic ibuprofen (IBU) supercooled liquid has been detected using differential scanning calorimetry and powder X-ray diffraction during the melt-quenching of IBU at a low temperature (0 °C). In this work, gram-scaled IBU supercooled liquid was prepared using the melt-quenching method, maintaining a liquid state for minutes at room temperature and for hours at 10 °C, as confirmed by visual observation. The Raman spectra, IR spectra, and UV-vis spectra results indicate that the structure of the IBU supercooled liquid is similar to that of an IBU solution instead of IBU Form I. The rate of recrystallization into Form I can be adjusted by controlling the temperature and additives, as confirmed by visual observation. Moreover, long-term stable IBU dispersions, with improved aqueous solubility, were inspired by the IBU supercooled liquid. The IBU supercooled liquid model can guide the preparation of ASDs for low melting point drugs. |
| format | Article |
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| institution | Kabale University |
| issn | 2073-4352 |
| language | English |
| publishDate | 2024-11-01 |
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| spelling | doaj-art-b3c96fd713ea42bd9c6742a7458cb2da2024-12-27T14:19:41ZengMDPI AGCrystals2073-43522024-11-011412103710.3390/cryst14121037Metastable Racemic Ibuprofen Supercooled LiquidTuanjia Li0Wangchuan Xiao1Shizhao Ren2Rongrong Xue3Fenghua Chen4College of Material Engineering, Fujian Agriculture and Forestry University, Fuzhou 350100, ChinaSchool of Resources and Chemical Engineering, Sanming University, Sanming 365004, ChinaSchool of Resources and Chemical Engineering, Sanming University, Sanming 365004, ChinaSchool of Resources and Chemical Engineering, Sanming University, Sanming 365004, ChinaSchool of Resources and Chemical Engineering, Sanming University, Sanming 365004, ChinaAmorphous solid dispersions are good candidates for improving solubility in water and the oral bioavailability of poorly water-soluble active pharmaceutical ingredients (APIs). Amorphous solids become supercooled liquids when the temperature reaches the glass transition temperature (T<sub>g</sub>). For APIs with low melting points, T<sub>g</sub> can be below room temperature, which makes it difficult to prepare long-term stable amorphous solids. Studies on the physicochemical properties of supercooled liquids shed light on the design of ASDs for APIs with low melting points. Racemic ibuprofen (IBU) supercooled liquid has been detected using differential scanning calorimetry and powder X-ray diffraction during the melt-quenching of IBU at a low temperature (0 °C). In this work, gram-scaled IBU supercooled liquid was prepared using the melt-quenching method, maintaining a liquid state for minutes at room temperature and for hours at 10 °C, as confirmed by visual observation. The Raman spectra, IR spectra, and UV-vis spectra results indicate that the structure of the IBU supercooled liquid is similar to that of an IBU solution instead of IBU Form I. The rate of recrystallization into Form I can be adjusted by controlling the temperature and additives, as confirmed by visual observation. Moreover, long-term stable IBU dispersions, with improved aqueous solubility, were inspired by the IBU supercooled liquid. The IBU supercooled liquid model can guide the preparation of ASDs for low melting point drugs.https://www.mdpi.com/2073-4352/14/12/1037ibuprofensupercooled liquidstabilitydissolutionamorphous solid dispersions |
| spellingShingle | Tuanjia Li Wangchuan Xiao Shizhao Ren Rongrong Xue Fenghua Chen Metastable Racemic Ibuprofen Supercooled Liquid Crystals ibuprofen supercooled liquid stability dissolution amorphous solid dispersions |
| title | Metastable Racemic Ibuprofen Supercooled Liquid |
| title_full | Metastable Racemic Ibuprofen Supercooled Liquid |
| title_fullStr | Metastable Racemic Ibuprofen Supercooled Liquid |
| title_full_unstemmed | Metastable Racemic Ibuprofen Supercooled Liquid |
| title_short | Metastable Racemic Ibuprofen Supercooled Liquid |
| title_sort | metastable racemic ibuprofen supercooled liquid |
| topic | ibuprofen supercooled liquid stability dissolution amorphous solid dispersions |
| url | https://www.mdpi.com/2073-4352/14/12/1037 |
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