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Related Concept Videos

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

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Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
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Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
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Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
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Local mobility in amorphous pharmaceuticals--characterization and implications on stability.

Sisir Bhattacharya1, Raj Suryanarayanan

  • 1Department of Pharmaceutics, University of Minnesota, Minneapolis, Minnesota 55455, USA.

Journal of Pharmaceutical Sciences
|June 6, 2009
PubMed
Summary
This summary is machine-generated.

Local molecular mobility, or beta-relaxations, significantly impacts amorphous pharmaceutical stability below the glass transition temperature (T(g)). Understanding these local motions is crucial for predicting drug stability.

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Area of Science:

  • Physical Pharmacy
  • Materials Science
  • Drug Stability

Background:

  • Amorphous pharmaceuticals' stability is linked to molecular mobility.
  • Global mobility (glass transition) is often studied, but doesn't fully explain instability.
  • Local mobility (beta-relaxations) below T(g) is increasingly recognized as critical.

Purpose of the Study:

  • To highlight the pharmaceutical significance of local motions (Johari-Goldstein relaxations) in amorphous systems.
  • To emphasize the impact of local mobility on amorphous phase stability.
  • To review the influence of additives like water on local motions.

Main Methods:

  • Review of existing literature on molecular mobility and amorphous pharmaceutical stability.
  • Discussion of the coupling model relating local and global mobility.
  • Overview of instrumental techniques for characterizing local motions.

Main Results:

  • Global mobility alone is insufficient to explain amorphous pharmaceutical instability.
  • Local mobility significantly influences physical and chemical stability.
  • Additives, such as water, can affect local motions in amorphous matrices.

Conclusions:

  • Local molecular motions are critical for amorphous pharmaceutical stability.
  • Characterizing local mobility, beyond global mobility, is essential for predicting drug behavior.
  • Further research into techniques for measuring local mobility is warranted.