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After filtration, the precipitate is washed to remove coprecipitated impurities and any remaining mother liquor. Colloidal precipitates, such as silver chloride, are washed with an electrolyte (such as dilute nitric acid) to prevent the peptization of the precipitate. In the case of slightly soluble precipitates, the wash solution contains a common ion to reduce solubility. Lead sulfate, which is slightly soluble in water, is washed with dilute sulfuric acid. Similarly, wash solutions may be...
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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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Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
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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).
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Bioequivalence in generic drugs, such as tablets and capsules, refers to their pharmaceutical equivalence to the brand-name counterparts. However, for therapeutic equivalence, manufacturers must also consider physical attributes like size, shape, and weight (FDA Guidance for Industry, December 2003). Discrepancies in these aspects could impact patient compliance and cause medication errors. For instance, swallowing difficulties, often experienced with larger tablets or capsules, can lead to...
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Formulation of ionic liquid APIs via spray drying processes to enable conversion into single and two-phase solid

Evangelia Tsolaki1, Michael W Stocker2, Anne Marie Healy3

  • 1School of Chemical and Bioprocess Engineering, University College Dublin, Dublin 4, Ireland; SSPC, The SFI Research Centre for Pharmaceuticals, School of Chemical and Bioprocess Engineering, University College Dublin, Dublin 4, Ireland; EPSRC-SFI Centre for Doctoral Training in Transformative Pharmaceutical Technologies, Ireland.

International Journal of Pharmaceutics
|May 14, 2021
PubMed
Summary
This summary is machine-generated.

Ionic liquid (IL) drug forms can be solidified into stable solid dosage forms using spray encapsulation or polymer miscibility. These novel methods improve the manufacturability of poorly soluble drugs for oral solid dosage (OSD) applications.

Keywords:
Co-processed APIsIonic liquid APIsSolid dispersionsSpray dryingSpray encapsulation

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Area of Science:

  • Pharmaceutical Science
  • Materials Science
  • Drug Delivery

Background:

  • Ionic liquids (ILs) offer solutions for poorly water-soluble drugs and enhance drug stability.
  • Challenges in handling and manufacturing ILs of active pharmaceutical ingredients (APIs) hinder their use in oral solid dosage forms (OSDs).

Purpose of the Study:

  • To demonstrate the applicability of spray encapsulation for solidifying diverse low glass transition temperature (Tg) API-ILs.
  • To explore a novel polymer-API-IL miscibility approach for API-IL solidification.
  • To overcome the glass transition temperature (Tg) suppression in room temperature ILs for OSD applications.

Main Methods:

  • Spray encapsulation using an immiscible polymer (ethyl cellulose) for phase-separated systems.
  • Spray drying utilizing polymer-API-IL miscibility with a high Tg polymer (maltodextrin) for amorphous solid dispersions (ASDs).
  • Characterization using modulated differential scanning calorimetry (mDSC) and attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR).

Main Results:

  • Successfully produced spray-dried solid materials from low Tg API-ILs at acceptable loadings and yields for OSDs.
  • Demonstrated two solidification approaches: phase-encapsulated systems and amorphous solid dispersions (ASDs).
  • Both methods effectively addressed the Tg suppression associated with room temperature ILs.

Conclusions:

  • The study presents two viable methods for solidifying API-ILs, broadening their application in OSDs.
  • This work lays the foundation for a mechanistic design approach by understanding critical physical attributes of API-IL systems.
  • The findings facilitate the development of advanced drug delivery systems for challenging pharmaceutical compounds.