Recent advances in the characterization of amorphous pharmaceuticals by X-ray diffractometry

Seema Thakral, Maxwell W. Terban, Naveen K. Thakral, Raj Suryanarayanan

Research output: Contribution to journalReview article

35 Scopus citations

Abstract

For poorly water soluble drugs, the amorphous state provides an avenue to enhance oral bioavailability. The preparation method, in addition to sample history, can dictate the nature and the stability of the amorphous phase. Conventionally, X-ray powder diffractometry is of limited utility for characterization, but structural insights into amorphous and nanocrystalline materials have been enabled by coupling X-ray total scattering with the pair distribution function. This has shown great promise for fingerprinting, quantification, and even modeling of amorphous pharmaceutical systems. A consequence of the physical instability of amorphous phases is their crystallization propensity, and recent instrumental advances have substantially enhanced our ability to detect and quantify crystallization in a variety of complex matrices. The International Centre for Diffraction Data has a collection of the X-ray diffraction patterns of amorphous drugs and excipients and, based on the available supporting information, provides a quality mark of the data.

Original languageEnglish (US)
Pages (from-to)183-193
Number of pages11
JournalAdvanced Drug Delivery Reviews
Volume100
DOIs
StatePublished - May 1 2016

Keywords

  • Amorphous
  • Crystallization
  • Solid dispersion
  • Total scattering pair distribution function
  • X-ray diffractometry

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