Solubility and thermodynamics of polymorphic indomethacin in binary solvent mixtures
文献类型：期刊论文
| 作者 | Yang, Li1,2; Zhang, Yan2; Cheng, Jingcai2; Yang, Chao1,2 |
| 刊名 | JOURNAL OF MOLECULAR LIQUIDS
 |
| 出版日期 | 2019-12-01 |
| 卷号 | 295页码:13 |
| ISSN号 | 0167-7322 |
| 关键词 | Indomethacin Binary solvent mixtures Solubility parameter In-situ ATR-FTIR Intermolecular forces |
| DOI | 10.1016/j.molliq.2019.111717 |
| 英文摘要 | The significant effect of solvent mixtures on the dissolution behavior of indomethacin (IMC) was systematically studied. Experimental measurements were carried out using an in-situ attenuated total reflection Fourier transform infrared (ATR-FTIR) spectrometer. Three thermodynamic models were used to correlate the experimental data to determine the solubilities of alpha- and gamma-form IMC in three representative systems, including acetone-heptane, acetone-water and ethanol-water at temperatures ranging from 293 K to 318 K under atmospheric pressure. The acetone-water mixture has the largest dissolving capacity for IMC among the three studied solvent mixtures, and generates "cosolvent effect". This effect is associated with the strong hydrogen-bond interaction between acetone and water. Notably, it is found that solvent-cosolvent mixtures with solubility parameters of 21 MPa0.5-24 MPa0.5 are suitable for solubility improvement in the design of pharmaceutical formulations of IMC. The solvent and antisolvent can be chosen in this order: delta(antisolvent) < delta(solvent) < 21 MPa0.5 or delta(antisolvent) > delta(solvent) > 24 MPa0.5 for the antisolvent crystallization of IMC. Our analysis strongly demonstrates that the solubility parameter can be a simple and efficient tool in preliminary solvent screening. However, the relationship between the solubility parameter and the resulting polymorphic form in antisolvent crystallization requires further study to achieve its potential applicability in polymorphic control. (C) 2019 Elsevier B.V. All fights reserved. |
| WOS关键词 | ANTISOLVENT CRYSTALLIZATION ; LIQUID-EQUILIBRIUM ; PURE ; SPECTROSCOPY ; STABILITY ; BEHAVIOR ; IMPACT ; WATER ; ACID |
| 资助项目 | National Key Research and Development Program[2016YFB0301702] ; National Natural Science Foundation of China[21878294] ; National Natural Science Foundation of China[21776284] ; Major National Scientific Instrument Development Project[21427814] ; Key Research Program of Frontier Sciences, CAS[QYZDJ-SSW-JSC030] ; Instrument Developing Project of the Chinese Academy of Sciences[YZ201641] |
| WOS研究方向 | Chemistry ; Physics |
| 语种 | 英语 |
| 出版者 | ELSEVIER |
| WOS记录号 | WOS:000506728000026 |
| 资助机构 | National Key Research and Development Program ; National Natural Science Foundation of China ; Major National Scientific Instrument Development Project ; Key Research Program of Frontier Sciences, CAS ; Instrument Developing Project of the Chinese Academy of Sciences |
| 源URL | [http://ir.ipe.ac.cn/handle/122111/38761]  |
| 专题 | 中国科学院过程工程研究所 |
| 通讯作者 | Zhang, Yan; Cheng, Jingcai |
| 作者单位 | 1.Univ Chinese Acad Sci, Sch Chem Engn, Beijing 100049, Peoples R China 2.Chinese Acad Sci, Inst Proc Engn, CAS Key Lab Green Proc & Engn, Beijing 100190, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yang, Li,Zhang, Yan,Cheng, Jingcai,et al. Solubility and thermodynamics of polymorphic indomethacin in binary solvent mixtures[J]. JOURNAL OF MOLECULAR LIQUIDS,2019,295:13. |
| APA | Yang, Li,Zhang, Yan,Cheng, Jingcai,&Yang, Chao.(2019).Solubility and thermodynamics of polymorphic indomethacin in binary solvent mixtures.JOURNAL OF MOLECULAR LIQUIDS,295,13. |
| MLA | Yang, Li,et al."Solubility and thermodynamics of polymorphic indomethacin in binary solvent mixtures".JOURNAL OF MOLECULAR LIQUIDS 295(2019):13. |
入库方式： OAI收割
来源：过程工程研究所
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