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Synthesis, Characterization and Theoretical Studies of a Novel Salt(Dexmedetomidine: Perchloric Acid = 1:1) and the Investigation of Its Stability 被引量:1

Synthesis, Characterization and Theoretical Studies of a Novel Salt(Dexmedetomidine: Perchloric Acid = 1:1) and the Investigation of Its Stability
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摘要 Dexmedetomidine and its novel salt have been synthesized and characterized by single-crystal XRD and TGA/DSG. Components of the crystalline phase have also been investigated in terms of their corresponding Hirshfeld surface. In the crystal lattice, a three-dimensional hydrogen-bonded network is observed. In this work, the salt strategy has been applied successfully to dexmedetomidine. One important parameter, i.e. stability, has also been significantly improved, which proves to be an important factor for solid dosage formulation. Furthermore, DSC/TGA analysis indicates that the salt maintains its crystallinity up to 300℃, suggesting a higher stability of the salt compared to pure dexmedetomidine. Dexmedetomidine and its novel salt have been synthesized and characterized by single-crystal XRD and TGA/DSG. Components of the crystalline phase have also been investigated in terms of their corresponding Hirshfeld surface. In the crystal lattice, a three-dimensional hydrogen-bonded network is observed. In this work, the salt strategy has been applied successfully to dexmedetomidine. One important parameter, i.e. stability, has also been significantly improved, which proves to be an important factor for solid dosage formulation. Furthermore, DSC/TGA analysis indicates that the salt maintains its crystallinity up to 300℃, suggesting a higher stability of the salt compared to pure dexmedetomidine.
出处 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2015年第8期1179-1186,共8页 结构化学(英文)
基金 supported by the prospective joint research project of Jiangsu province(BY20122193) the Fundamental Research Funds for the Central Universities(CXZZ12_0119)
关键词 single-crystal X-ray diffraction DSC/TGA crystal structure hydrogen bond Hirshfeld surfaces single-crystal X-ray diffraction, DSC/TGA, crystal structure, hydrogen bond, Hirshfeld surfaces
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  • 1Ramon, G.; Davies, K.; Nassimbeni, L. R. Structures of benzoic acids with substituted pyridines and quinolines: salt versus co-crystal formation. CrystEngComm. 2014, 16, 5802-5810.
  • 2Huyskensa, P.; Sobczyk, L.; Majerzb, I. On a hard/soft hydrogen bond interaction. J. MoL Struct. 2002, 615, 61-72.
  • 3Food and Drug Administration. Guidance.for Industry: Regulatory Classification of Pharmaceutical Co-Crystals. Center for Drug Evaluation andResearch. Silver Spring, MD, USA 2013.
  • 4Blagden, N.; Colesb, S. J.; Berry, D. J. Pharmaceutical co-crystals - are we there yet. CrystEngComm. 2014, 16, 5753-5761.
  • 5Seaton, C. C. Proton location in acidpyridine hydrogen bonds of multi-component crystals. CrystEngComm. 2014, 16, 5878-5886.
  • 6Kamibayashi, T.; Maze, M. Clinical uses of alpha 2-adrenergic agonists. Anesthesiology 2000.93, 1345-1349.
  • 7Calzada, B. C.; Artinano, D E.; Alpha, A. A. 2-adrenoreceptorsubtypes. Pharmacol Res. 2001, 44, 195-208.
  • 8Chen, Z. (3.; Cao, D. Q.; Xu, J. M.; Chen, Y. P. The progress of dexmedetomidine clinical application. The Journal of Guangdong Medical 2012, 33, 290-292.
  • 9Turpeinen, U.; Ruotsalainen. H.; Pehkonan, R. Crystal structure, thermal behaviour, protonation and mass spectroscopic studies of racemic 4-[1-(2,3-dimethylphanyl)-ethyl]-lH-imidazole Hydrochlorides. Acta Chemica Scandinavica B 1989, 42, 537-545.
  • 10Kivikoski, J. H.; Rissanen, K. T.; Parhi, S. S. L. Crystal-structures and absolute-configurations of dexanedetomidine and its tosyl derivative. Tetrahedron-Asymmetry 1993, 1, 45-48.

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