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Related Experiment Videos

Differences in crystallization behavior between quenched and ground amorphous ursodeoxycholic acid.

E Yonemochi1, Y Inoue, G Buckton

  • 1Centre for Materials Science, School of Pharmacy, University of London, UK.

Pharmaceutical Research
|July 9, 1999
PubMed
Summary
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Different preparation methods yield distinct amorphous states of ursodeoxycholic acid (UDCA). Crystallization of amorphous UDCA depends on its molecular disorder and preparation technique.

Area of Science:

  • Pharmaceutical Sciences
  • Materials Science

Background:

  • Ursodeoxycholic acid (UDCA) is a therapeutic bile acid.
  • Amorphous forms of drugs can exhibit different physicochemical properties compared to their crystalline counterparts.
  • Understanding the amorphous states of UDCA is crucial for its formulation and stability.

Purpose of the Study:

  • To investigate the crystallization behavior of ground and quenched amorphous ursodeoxycholic acid (UDCA).
  • To characterize the distinct amorphous states of UDCA prepared by different methods.

Main Methods:

  • Amorphous UDCA was prepared via grinding and melt quenching.
  • Characterization involved powder X-ray diffraction (XRD), near-infrared (NIR) spectroscopy, and dynamic vapor sorption.
  • Crystallization was studied using isothermal microcalorimetry under varying humidity and solvent vapor conditions.

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Main Results:

  • Both ground and quenched methods produced amorphous UDCA, confirmed by XRD.
  • Ground UDCA crystallized around 80°C, while quenched UDCA remained amorphous.
  • Quenched UDCA exhibited higher water sorption at low relative humidity and different surface energy compared to ground UDCA.
  • NIR spectra differentiated between the two amorphous states.

Conclusions:

  • The preparation method significantly influences the molecular state of amorphous UDCA.
  • The degree of molecular disorder in amorphous UDCA correlates with its crystallization propensity.