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Solid state characterization of E2101, a novel antispastic drug.

Ikuo Kushida1, Kazuhide Ashizawa

  • 1Eisai Company, Ltd., Analytical Research Laboratories, 5-1-3 Tokodai, Tsukuba, Ibaraki, 300-2635, Japan. i-kushida@hhc.eisai.co.jp

Journal of Pharmaceutical Sciences
|September 13, 2002
PubMed
Summary

Two polymorphs of the antispastic drug E2101 were identified. Form I, exhibiting higher thermodynamic stability and slower dissolution, is recommended for further drug development.

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Area of Science:

  • Pharmaceutical Sciences
  • Solid-State Chemistry
  • Materials Science

Background:

  • E2101 is a novel antispastic drug.
  • Understanding drug polymorphism is crucial for pharmaceutical development.
  • Polymorphs can significantly impact drug efficacy and stability.

Purpose of the Study:

  • To characterize the polymorphic forms of E2101.
  • To investigate the physicochemical and thermodynamic properties of E2101 polymorphs.
  • To determine the most stable and suitable polymorph for further development.

Main Methods:

  • X-ray powder diffraction (XRD) for polymorph identification.
  • Variable temperature XRD, thermal analysis (DSC), and hygroscopicity measurements for property characterization.

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  • Dissolution studies and solubility measurements at various temperatures to estimate transition temperatures and dissolution rates.

    • Main Results:

    • Two polymorphs of E2101, designated forms I and II, were identified and confirmed by XRD.
    • Both polymorphs are anhydrous with low moisture adsorption.
    • Form I exhibits a higher melting point (148.1°C) and heat of fusion (38.2 kJ/mol) compared to Form II (139.8°C, 35.2 kJ/mol).
    • Form II shows a 1.5-fold faster intrinsic dissolution rate than Form I.
    • Form I is thermodynamically more stable than Form II.

    Conclusions:

    • Form I of E2101 is thermodynamically more stable and suitable for further pharmaceutical development.
    • The polymorphic pair of E2101 exhibits monotropic behavior.
    • Understanding the solid-state properties of E2101 polymorphs is essential for its successful formulation and therapeutic application.