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[Polymorph transformation of solid drugs].

Qi Zhang, Xue-feng Mei

    Yao Xue Xue Bao = Acta Pharmaceutica Sinica
    |August 4, 2015
    PubMed
    Summary
    This summary is machine-generated.

    Pharmaceutical solid form selection balances stability and performance. Understanding polymorph and hydrate transformations is crucial for drug development, especially when using metastable forms to enhance solubility and bioavailability.

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    Area of Science:

    • Solid-state chemistry
    • Pharmaceutical sciences
    • Materials science

    Background:

    • The most stable polymorph is typically preferred for minimized phase transformation risk in pharmaceuticals.
    • However, stable polymorphs can exhibit poor solubility, dissolution rates, and bioavailability.
    • Metastable forms, kinetically stable at lower temperatures, may offer improved properties but pose transformation risks.

    Purpose of the Study:

    • To review recent studies on crystal conversion of polymorphs and hydrates.
    • To illustrate cases of crystalline solid transformation.
    • To introduce the types, conditions, and mechanisms of solid form transformations.

    Main Methods:

    • Literature review of recent studies on crystal conversion.
    • Case study analysis of polymorph and hydrate transformations.

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  • Discussion of transformation types, conditions, and mechanisms.

    • Main Results:

    • Crystalline solid transformations involve various types, conditions, and mechanisms.
    • Metastable forms can be advantageous for drug properties but require careful handling.
    • Understanding transformation pathways is essential for preventing undesirable changes.

    Conclusions:

    • Knowledge of solid form transformation is vital for pharmaceutical development.
    • Selection of solid forms requires balancing stability, performance, and processing.
    • Further research into transformation mechanisms can optimize drug formulation and manufacturing.