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  • 标题:Study of Complex Formation of Carbamazepine with Thiourea
  • 本地全文:下载
  • 作者:Yutaka Inoue ; Sayuri Sato ; Chisa Yamamoto
  • 期刊名称:Chemical and Pharmaceutical Bulletin
  • 印刷版ISSN:0009-2363
  • 电子版ISSN:1347-5223
  • 出版年度:2014
  • 卷号:62
  • 期号:11
  • 页码:1125-1130
  • DOI:10.1248/cpb.c14-00340
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:

    The aim of this study, we evaluated a complex between thiourea (TU) and carbamazepine (CBZ) of a poorly soluble drug by using powder X-ray diffraction (PXRD), Fourier transform infrared (FT-IR) spectroscopy, X-ray crystallography and the solubility test. PXRD of TU/CBZ=2/1, 1/1, and 1/2 prepared by solvent evaporation (EVP) revealed characteristic diffraction peaks at 2θ=6.7°, 8.8°, 13.5°, and 20.4°, therefore molecular interaction between TU and CBZ presumably occurred. Results of the FT-IR spectroscopy, asymmetric and symmetric NH stretching vibration of TU were shifted to high region by TU/CBZ=2/1, 1/1, and 1/2 EVP. TU/CBZ=2/1 and 1/1 EVP had absorption derived from TU. It was considered that complex were formed by TU/CBZ=1/2. X-Ray crystallography of TU and CBZ revealed a crystal structure with one TU molecule arranged near two CBZ molecules. Molecules of the same type overlap in this layer. When doing a solubility test by using CBZ and samples of EVP, physical mixture and crystals in TU/CBZ=1/2 to confirm the solubility in water of TU/CBZ complex, there is no difference with the CBZ. It considered that the structure of a complex differs from the tunnel structure of inclusion complexes that has been previously reported contribute to result it.

  • 关键词:thiourea; carbamazepine; complex; X-ray crystallography; hydrogen bond
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