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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).
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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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Related Experiment Video

Updated: Aug 25, 2025

Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
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Hydroxypropyl-β-cyclodextrin-based solid dispersed granules: A prospective alternative to conventional solid

Jung Suk Kim1, Fakhar Ud Din2, Yoo Jin Choi1

  • 1College of Pharmacy, Hanyang University, 55, Hanyangdaehak-ro, Sangnok-gu, Ansan 15588, South Korea.

International Journal of Pharmaceutics
|October 17, 2022
PubMed
Summary

Hydroxypropyl-β-cyclodextrin (HP-β-CD)-based solid dispersed granules offer improved powder properties and comparable oral bioavailability to solid dispersions for poorly soluble drugs like dexibuprofen.

Keywords:
DexibuprofenFluid bed granulatorHydroxypropyl-β-cyclodextrinOral bioavailabilityPowder propertySolid dispersed granules

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems

Background:

  • Poorly water-soluble drugs present challenges in oral administration.
  • Solid dispersion is a common technique to enhance drug solubility and bioavailability.
  • Developing improved formulations is crucial for effective drug delivery.

Purpose of the Study:

  • To develop hydroxypropyl-β-cyclodextrin (HP-β-CD)-based solid dispersed granules.
  • To evaluate these granules as a superior alternative to traditional solid dispersion.
  • To compare their efficacy in improving solubility, dissolution, and oral bioavailability of dexibuprofen.

Main Methods:

  • Fabrication of solid dispersion (drug/HP-β-CD/Tween80) using a spray-dryer.
  • Fabrication of solid dispersed granules (drug/HP-β-CD/Tween80/Microcrystalline cellulose) using a fluid bed granulator.
  • Comparative analysis of powder properties, solubility, dissolution, and oral bioavailability.

Main Results:

  • HP-β-CD-based solid dispersed granules significantly enhanced dexibuprofen solubility and dissolution.
  • Oral bioavailability of dexibuprofen was maximized to the same extent as solid dispersion.
  • Solid dispersed granules showed considerable improvements in powder and tablet properties compared to solid dispersion.

Conclusions:

  • HP-β-CD-based solid dispersed granules represent a promising advancement over traditional solid dispersions.
  • This formulation offers enhanced drug solubility, dissolution, and bioavailability with improved physical properties.
  • Solid dispersed granules are a prospective alternative for formulating poorly water-soluble drugs.