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Synthesis of two novel azilsartan cocrystals: Preparation, physicochemical characterization and solubility studies

Crystals, ISSN: 2073-4352, Vol: 10, Issue: 9, Page: 1-11
2020
  • 7
    Citations
  • 0
    Usage
  • 8
    Captures
  • 0
    Mentions
  • 1
    Social Media
Metric Options:   Counts1 Year3 Year

Metrics Details

  • Citations
    7
    • Citation Indexes
      7
  • Captures
    8
  • Social Media
    1
    • Shares, Likes & Comments
      1
      • Facebook
        1

Article Description

Azilsartan is a novel angiotension II receptor blocker primarily used to treat high blood pressure. This is not a formulation-friendly molecule largely due to the inherent water-solubility pitfalls. In this paper, two novel cocrystals of azilsartan (AZ) were studied (AZ-BIP, AZ-BPE; BIP = 4,4-bipyridine, BPE = trans-1,2-bis (4-pyridyl) ethylene) by solution crystallization. The structures of these two cocrystals were characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA), including the single-crystal structure determination of AZ-BIP and AZ-BPE. In the cocrystals AZ-BIP (2:1) and AZ-BPE (2:1), two AZ molecules and one coformer formed a sandwich structure through N-H … N interactions. These sandwich structures were extended into a one-dimensional structure through O-H … N hydrogen bonds. The equilibrium solubility study demonstrated that the AZ-BIP and AZ-BPE cocrystals both showed higher solubility than azilsartan in water.

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