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Physicochemical and Biological Properties of Drugs Relevant to Controlled Release Formulations

Physicochemical Properties

Physicochemical and Biological Properties of Drugs Relevant to Controlled Release Formulations

Solubility:

  • Drugs should have moderate solubility to ensure consistent release.

  • Extremely soluble drugs may release too quickly; poorly soluble drugs may not release adequately.

Partition Coefficient:

  • Affects drug permeability across biological membranes.

  • Optimal balance between lipophilicity and hydrophilicity is crucial.

Molecular Weight and Size:

  • Smaller molecules diffuse more readily through polymers and membranes.

  • Larger molecules may require specialized systems like nanoparticles.

Stability:

  • Chemical and physical stability in the formulation and biological environment.

  • Sensitivity to pH, enzymes, or other degradation pathways must be considered.

Biological Properties

Physicochemical and Biological Properties of Drugs Relevant to Controlled Release Formulations

Absorption:

  • Consistent and predictable absorption profiles are necessary.

  • Drugs absorbed throughout the GI tract are ideal.

Metabolism:

  • Drugs extensively metabolized in the first pass may not benefit from oral CDDS.

  • Alternative routes or targeted delivery may be required.

Half-life:

  • Drugs with short half-lives are good candidates as CDDS can prolong their action.

  • Extremely long half-life drugs may not need controlled release.

Therapeutic Index:

  • Drugs with a narrow therapeutic window require precise control over release rates.

  • Safety margins must be maintained to prevent toxicity.


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