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Study of Physicochemical Characteristics of Drug Substances

Study of Physicochemical Characteristics

  • Understanding the physicochemical properties of drug substances is paramount in pre-formulation studies.

  • These characteristics influence the drug's behavior during formulation, processing, and storage, as well as its bioavailability and therapeutic performance.

Key Physicochemical Characteristics:

Physical Properties:

  • Physical form (crystalline vs. amorphous)

  • Particle size and shape

  • Flow properties

Chemical Properties:

  • Solubility and dissolution rate

  • pKa (acid dissociation constant)

  • Partition coefficient (log P)

  • Stability and degradation pathways

Thermal Properties:

  • Melting point

  • Glass transition temperature

Spectroscopic Properties:

  • Infrared (IR) spectroscopy

  • Nuclear Magnetic Resonance (NMR)

  • Ultraviolet-visible (UV-Vis) spectroscopy

Polymorphism:

  • Different crystalline forms of the same drug substance.

Importance:

  • Formulation Design: Physicochemical properties determine the choice of dosage forms (e.g., tablets, capsules, injectables) and the selection of excipients.

  • Manufacturability: Properties like flowability and compressibility affect manufacturing processes such as tableting and encapsulation.

  • Stability: Understanding how the drug reacts to environmental factors ensures the formulation remains effective over its shelf life.

  • Bioavailability: Solubility and dissolution rates influence how the drug is absorbed in the body.


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