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Related Experiment Videos

Chemical reactivity in solid-state pharmaceuticals: formulation implications.

S R Byrn1, W Xu, A W Newman

  • 1Purdue University, West Lafayette, IN 47907, USA. sbyrn@pharmacy.purdue.edu

Advanced Drug Delivery Reviews
|April 28, 2001
PubMed
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This study explores solid-state chemical reactions in pharmaceuticals, including oxidation and cyclization. Understanding these reactions, influenced by molecular mobility and excipient interactions, is key to improving drug stability.

Area of Science:

  • Pharmaceutical Sciences
  • Solid-State Chemistry
  • Drug Stability

Background:

  • Solid-state reactions in pharmaceuticals encompass phase transformations, dehydration/desolvation, and chemical reactivity.
  • Drug substance instability and reactions with excipients are critical concerns in formulation development.
  • Water absorption can increase molecular mobility, promoting solid-state reactivity.

Purpose of the Study:

  • To focus on chemical reactivity within solid-state pharmaceutical systems.
  • To investigate the influence of molecular mobility on solid-state reactions.
  • To examine drug-excipient interactions and their impact on stability.

Main Methods:

  • Measurement of molecular mobility using techniques like glass transition (Tg) measurements, solid-state NMR, and X-ray crystallography.

Related Experiment Videos

  • Analysis of various solid-state reactions including oxidation, cyclization, hydrolysis, and deamidation.
  • Case studies of drug-excipient interactions such as transacylation, Maillard browning, and acid-base reactions.

    • Main Results:

    • Oxidation studies were conducted on vitamin A, peptides, and steroids.
    • Cyclization reactions of angiotensin-converting enzyme (ACE) inhibitors were investigated in relation to mobility and reactivity.
    • Drug-excipient interactions were exemplified with aspirin, fluoxetine, and ibuprofen.

    Conclusions:

    • Understanding solid-state reactions is crucial for pharmaceutical development.
    • Strategies to prevent reactivity can be implemented based on knowledge of these reactions.
    • Improved stability of drug substances and products can be achieved by controlling solid-state reactivity.