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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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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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Related Experiment Video

Updated: May 20, 2025

A Package of Established Analytical Tools to Investigate the Solid-State Alteration of Lipid-Based Excipients
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Special Issue "Pharmaceutical Solid Forms: From Crystal Structure to Formulation".

Philippe Espeau1

  • 1Unit of Chemical and Biological Technologies for Health (UTCBS), CNRS, INSERM, Université Paris Cité, 75006 Paris, France.

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|March 27, 2025
PubMed
Summary

Characterizing active pharmaceutical ingredient (API) structure is crucial for successful drug formulation. Understanding API structural properties early streamlines the complex process from discovery to therapeutic product.

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Development
  • Materials Science

Background:

  • Significant effort is needed to transition a therapeutic molecule from discovery to a viable drug product.
  • The structural characteristics of an active pharmaceutical ingredient (API) are fundamental to its successful formulation.
  • Early-stage structural elucidation of APIs is often underestimated in the drug development pipeline.

Discussion:

  • This Special Issue emphasizes the importance of pre-formulation structural characterization of APIs.
  • Investigating API solid-state properties, polymorphism, and degradation pathways is vital.
  • Connecting molecular structure to macroscopic formulation behavior is a key challenge.

Key Insights:

  • Proactive structural analysis of APIs mitigates formulation risks and development delays.
  • Knowledge of API structure informs excipient selection and manufacturing process design.
  • Robust characterization ensures API stability, bioavailability, and therapeutic efficacy.

Outlook:

  • Future research should focus on advanced analytical techniques for rapid API structural assessment.
  • Integrating computational modeling with experimental data can predict formulation outcomes.
  • Standardizing pre-formulation characterization protocols will accelerate drug development timelines.