Synthesis of a Glibenclamide Cocrystal: Full Spectroscopic and Thermal Characterization

J Pharm Sci. 2018 Jun;107(6):1597-1604. doi: 10.1016/j.xphs.2018.01.029. Epub 2018 Feb 9.

Abstract

A cocrystal of glibenclamide, an antidiabetic drug classified as type II compound according to the Biopharmaceutics Classification System, has been synthesized using tromethamine as coformer in 1:1 molar ratio, by slow solvent evaporation cocrystalization. The cocrystal obtained was characterized by X-ray powder diffraction, differential scanning calorimetry, Raman, mid infrared, and near-infrared spectroscopy. The results consistently show the formation of a cocrystal between active pharmaceutical ingredients and conformer with the synthons corresponding to hydrogen bonding between hydrogen in amines of tromethamine and carbonyl and sulfonyl groups in glibenclamide.

Keywords: FTIR; Raman spectroscopy; X-ray powder diffractometry; calorimetry (DSC); co-crystals; near-infrared spectroscopy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Calorimetry, Differential Scanning
  • Crystallization / methods*
  • Excipients / chemistry*
  • Glyburide / chemistry*
  • Hydrogen Bonding
  • Hypoglycemic Agents / chemistry*
  • Powder Diffraction
  • Solubility
  • Spectroscopy, Fourier Transform Infrared
  • Spectrum Analysis, Raman
  • Tromethamine / chemistry*
  • X-Ray Diffraction

Substances

  • Excipients
  • Hypoglycemic Agents
  • Tromethamine
  • Glyburide