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Pharmaceutical Cocrystals: Regulatory and Strategic Aspects, Design and Development
Dipak Dilip Gadade1, Sanjay Sudhakar Pekamwar1
1School of Pharmacy, S.R.T.M. University, Vishnupuri, Nanded - 431606, India.
Advanced Pharmaceutical Bulletin
|January 20, 2017
Summary
Pharmaceutical cocrystals enhance drug properties like solubility and bioavailability. This supramolecular chemistry approach offers green synthesis and regulatory guidance for drug development.
Area of Science:
- Supramolecular Chemistry
- Pharmaceutical Sciences
- Materials Science
Background:
- Cocrystals are gaining interest for modifying physicochemical properties of active pharmaceutical ingredients (APIs).
- Optimizing API properties like solubility, dissolution, bioavailability, and stability is crucial in pharmaceutical development.
- Pharmaceutical cocrystals offer a green synthesis approach, maintaining therapeutic activity while improving drug characteristics.
Approach:
- Rational design of cocrystals using hydrogen bonding rules, solubility parameters, CSD database screening, and thermodynamic characteristics.
- Selection of appropriate coformers for the synthesis of multi-component cocrystals.
- Investigating synthesis methods and understanding potential polymorphic forms, solvates, and hydrates.
Key Points:
- Cocrystals can significantly improve drug solubility, dissolution rates, and bioavailability.
- They offer a sustainable and green synthesis pathway for pharmaceutical compounds.
- Potential challenges include the formation of various crystalline forms (polymorphs, solvates, hydrates) during synthesis.
- Regulatory agencies in the US and Europe have issued guidance documents for pharmaceutical cocrystal registration.
Conclusions:
- Pharmaceutical cocrystals represent a promising strategy for drug formulation and development.
- Understanding cocrystal design, synthesis, and characterization is vital for successful product registration.
- Consideration of regulatory and intellectual property aspects is essential for advancing cocrystal technology.
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