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Complexation of Baricitinib with β-Cyclodextrin and Its Dimeric Amino-Derivatives

  • A. A. Garibyan,
  • G. I. Kurochkina,
  • N. V. Kutyasheva,
  • M. K. Grachev,
  • I. V. Terekhova

摘要

Abstract

A comparative study of the complexing and solubilizing capacity of β-cyclodextrin and its new dimeric diaminocationic derivatives in relation to baricitinib, a new generation immunomodulator, is performed. Isothermal saturation is used to determine the solubility of baricitinib in the presence of the considered β‑cyclodextrins in a phosphate buffer solution (pH 6.8). Thermodynamic parameters of complex formation are calculated, and a binding mode is proposed on the basis of 1H NMR data. The effect of the structure of β-cyclodextrin on the efficiency of complex formation and the solubilization of baricitinib is analyzed.