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Related Experiment Videos

General principles of pharmaceutical solid polymorphism: a supramolecular perspective.

Barbara Rodríguez-Spong1, Christopher P Price, Adivaraha Jayasankar

  • 1Department of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, 428 Church Street, Ann Arbor, MI 48109-1065, USA.

Advanced Drug Delivery Reviews
|February 14, 2004
PubMed
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Active pharmaceutical ingredients (APIs) form diverse solid-state structures through molecular interactions. Understanding these supramolecular assemblies is key to designing stable and functional pharmaceutical solids.

Area of Science:

  • Solid-state chemistry
  • Supramolecular chemistry
  • Crystal engineering

Background:

  • The diversity of solid-state forms of active pharmaceutical ingredients (APIs) is governed by non-covalent interactions, molecular assembly, and the thermodynamic balance of entropy and enthalpy.
  • Crystallization involves molecular recognition and self-assembly, influencing pharmaceutical function and stability.
  • Understanding molecular interactions in pharmaceutical solids offers insights into designing ordered and disordered solid forms.

Purpose of the Study:

  • To review pharmaceutical solids using supramolecular chemistry and crystal engineering concepts.
  • To discuss factors controlling crystallization and solid-phase transformations.
  • To highlight the path towards supramolecular pharmaceutics through understanding molecular recognition.

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Main Methods:

  • Review of supramolecular chemistry principles applied to pharmaceutical solids.
  • Discussion of crystal engineering concepts in API solid form design.
  • Analysis of molecular recognition and self-assembly in crystallization.

Main Results:

  • Pharmaceutical solid-state diversity arises from non-covalent interactions and molecular assemblies.
  • Molecular recognition and complementarity are crucial for designing single and multi-component solids.
  • Solid phase transformations are controlled by molecular interactions and thermodynamic factors.

Conclusions:

  • Supramolecular chemistry and crystal engineering provide a framework for understanding and designing pharmaceutical solid forms.
  • Insights into molecular recognition advance the field of supramolecular pharmaceutics.
  • Control over crystallization and solid-phase transformations is essential for drug development.