期刊
PHARMACEUTICALS
卷 15, 期 7, 页码 -出版社
MDPI
DOI: 10.3390/ph15070807
关键词
co-crystal; naproxen; stability; solubility; intermolecular interaction
资金
- Key R&D Program of Shan Dong Province [2021ZDSYS26]
- Fundamental Research Funds for the Central Universities [2021-RW350-001]
- Chinese Pharmacopoeia Commission Drug Standard Promoting Fund [2022Y14]
Two novel co-crystals of naproxen, NPX-CPL and NPX-OMT, were designed and evaluated for stability and solubility. NPX-OMT showed significantly improved solubility in various solvent systems, while NPX-CPL was advantageous in acidic solvents. Thermal analysis indicated that NPX-OMT has better thermal stability. Theoretical calculations revealed intermolecular interactions of the co-crystals.
Two novel co-crystals of naproxen (NPX) were designed and prepared at a stoichiometric ratio of 1:1, namely, naproxen-caprolactam (NPX-CPL) and naproxen-oxymatrine (NPX-OMT). The characteristics of the co-crystals were evaluated in terms of stability and solubility studies. In terms of solubility, in four kinds of solvent systems with different pH, the solubility of NPX-OMT was significantly improved compared with that of NPX, whereas the NPX-CPL showed advantages in acidic solvent systems, indicating that the co-crystals can be applied to concoct preparations depending on therapeutic purposes. Furthermore, the experimental results of the thermal analysis showed that the co-crystal NPX-OMT had better thermal stability than the co-crystal NPX-CPL. Finally, as a complement to the single crystal X-ray diffraction (SC XRD) method, the theoretical calculation based on density functional theory (DFT) was also used to reveal the intermolecular interaction of the co-crystals at the molecular level and visually display the difference between them.
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