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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).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
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Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
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Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
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Study of process induced polymorphic transformations in fluconazole drug.

Satish R Desai1, Sanjiv R Dharwadkar

  • 1Department of Chemistry, The Institute of Science, 15, Madam Cama Road, Mumbai-400 032, India.

Acta Poloniae Pharmaceutica
|September 2, 2009
PubMed
Summary

Fluconazole form-II can transform into form-I through solid-state methods like heating or pressure. These solid-state transformations of fluconazole are confirmed by DSC, XRD, and SEM, impacting drug dissolution.

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Area of Science:

  • Pharmaceutical Sciences
  • Solid-State Chemistry

Background:

  • Fluconazole exists in multiple polymorphic forms, with form-I and form-II being significant.
  • Understanding polymorphic transformations is crucial for drug stability and efficacy.

Purpose of the Study:

  • To investigate the solid-state transformation of fluconazole form-II to form-I.
  • To explore various process parameters that induce this polymorphic transition.

Main Methods:

  • Melting and controlled cooling of fluconazole form-II to form a glassy mass.
  • Ageing of the glassy mass at ambient temperature.
  • Heating the glassy mass at a controlled rate.
  • Application of uniaxial pressure to fluconazole form-II.
  • Differential Scanning Calorimetry (DSC) for phase analysis.
  • X-ray Diffraction (XRD) and Scanning Electron Microscopy (SEM) for structural confirmation.

Main Results:

  • Fluconazole form-II transformed into form-I via melt-recrystallization (glassy mass ageing) and direct heating of the glassy mass.
  • Uniaxial pressure also induced the transformation from form-II to form-I.
  • Ageing of the sample prior to pressure application enhanced the transformation.
  • DSC, XRD, and SEM confirmed the successful polymorphic transformation and characterized the resulting form-I.

Conclusions:

  • Solid-state transformation of fluconazole form-II to form-I is achievable through thermal and mechanical stimuli.
  • Process parameters significantly influence the efficiency of polymorphic conversion.
  • The study provides insights into controlling fluconazole's solid-state properties, potentially affecting its dissolution rate and bioavailability.