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Selective preparation of elusive and alternative single component polymorphic solid forms through multi-component

Lynne H Thomas1, Craig Wales2, Chick C Wilson3

  • 1Department of Chemistry, University of Bath, Bath BA2 7AY, UK. C.C.Wilson@bath.ac.uk.

Chemical Communications (Cambridge, England)
|April 16, 2016
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Summary
This summary is machine-generated.

A new method uses nitrogen heterocyclic co-molecules to create novel crystal forms of active pharmaceutical ingredients like paracetamol. This approach also yields previously unknown solvates, advancing pharmaceutical material science.

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Area of Science:

  • Pharmaceutical Science
  • Crystallography
  • Materials Chemistry

Background:

  • Polymorphism in active pharmaceutical ingredients (APIs) significantly impacts drug efficacy and stability.
  • Controlling crystallization to obtain desired polymorphic forms remains a challenge in pharmaceutical development.
  • Novel solvates of APIs can offer unique physicochemical properties.

Purpose of the Study:

  • To demonstrate a simple and transferable method for producing novel polymorphic forms of APIs.
  • To investigate the use of nitrogen heterocyclic co-molecules in controlling API crystallization.
  • To synthesize previously unknown solvates of selected APIs.

Main Methods:

  • Utilizing nitrogen heterocyclic co-molecules as additives.
  • Employing a multi-component environment to influence self-assembly crystallization.
  • Applying the method to active pharmaceutical ingredients such as paracetamol, piroxicam, and piracetam.

Main Results:

  • Successful production of previously elusive polymorphic forms of paracetamol, piroxicam, and piracetam.
  • Demonstration of novel solvates for these APIs.
  • The method proved to be transferable and simple to implement.

Conclusions:

  • Nitrogen heterocyclic co-molecules are effective in directing the crystallization of APIs into novel forms.
  • This method offers a viable strategy for discovering new solid-state forms of pharmaceuticals.
  • The ability to generate novel solvates expands the possibilities for API formulation and development.