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Related Experiment Videos

Polymorphism of roxifiban.

Michael B Maurin1, Rodney D Vickery, Shelley R Rabel

  • 1Pharmacy R&D, DuPont Pharmaceuticals Company, Route 141, Henry Clay Road, Building 400, Wilmington, Delaware 19880-0400, USA. michael.maurin@qspharma.com

Journal of Pharmaceutical Sciences
|November 16, 2002
PubMed
Summary
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Roxifiban exhibits two polymorphic forms, detected via X-ray powder diffraction and NMR. Form II is thermodynamically stable, but Form I shows kinetic stability, crucial for pharmaceutical development.

Area of Science:

  • Solid-state chemistry
  • Pharmaceutical sciences
  • Crystallography

Background:

  • Polymorphism is critical in drug development, influencing stability and bioavailability.
  • Understanding crystal forms of active pharmaceutical ingredients (APIs) is essential for consistent drug performance.

Purpose of the Study:

  • To characterize the polymorphic forms of Roxifiban.
  • To determine the thermodynamic relationship between Roxifiban polymorphs.
  • To assess the stability of different Roxifiban crystal forms under storage conditions.

Main Methods:

  • X-ray powder diffraction (XRPD) and solid-state carbon nuclear magnetic resonance (13C NMR) for polymorph detection.
  • Isothermal microcalorimetry (IMC) to detect subtle differences.
  • Solubility studies as a function of temperature to determine thermodynamic parameters.

Related Experiment Videos

  • Differential scanning calorimetry (DSC), infrared (IR), and Raman spectroscopy for comparative analysis.

    • Main Results:

    • Two polymorphic forms of Roxifiban (Form I and Form II) were identified.
    • Enantiotropic relationship confirmed with a thermodynamic transition point at 132°C.
    • Form II is the most thermodynamically stable form.
    • Form I demonstrated kinetic stability for over 36 months at 25°C/60% RH.

    Conclusions:

    • Roxifiban exhibits enantiotropic polymorphism, with Form II being the most stable.
    • Form I's kinetic stability is significant for practical handling and storage, despite Form II's thermodynamic advantage.
    • Characterization of Roxifiban polymorphs is vital for ensuring drug product quality and efficacy.