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Related Experiment Videos

Increased dissolution rate and bioavailability through comicronization with microcrystalline cellulose.

Julie K Spence1, Shobha N Bhattachar, James A Wesley

  • 1Pharmaceutical Research and Development, World Wide Pharmaceutical Sciences, Pfizer Global Research and Development-Michigan Laboratories, Ann Arbor, Michigan, USA. Julie.Spence@Pfizer.com

Pharmaceutical Development and Technology
|December 24, 2005
PubMed
Summary
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Comicronization, a technique combining drug particles with excipients, enhances dissolution and bioavailability for poorly soluble compounds. This method overcomes particle agglomeration issues common in simple micronization, improving drug delivery.

Area of Science:

  • Pharmaceutical Technology
  • Drug Delivery Systems
  • Physical Pharmacy

Background:

  • Micronization improves bioavailability for dissolution rate-limited compounds.
  • Particle agglomeration due to intermolecular forces negates micronization benefits.
  • Comicronization with excipients offers advantages over neat micronization.

Purpose of the Study:

  • To investigate comicronization of CI-1040 at high drug load.
  • To assess the impact of comicronization on dissolution rate and bioavailability.
  • To characterize comicronized and micronized CI-1040 to explain observed data.

Main Methods:

  • Comicronization of CI-1040 with excipients at high drug load.
  • In-vitro dissolution rate testing.

Related Experiment Videos

  • In-vivo bioavailability studies in male Wistar rats.
  • Physicochemical characterization of drug materials.
  • Main Results:

    • Comicronization significantly increased the dissolution rate of CI-1040.
    • Enhanced bioavailability was observed in male Wistar rats post-comicronization.
    • Physicochemical characterization provided insights into improved performance.

    Conclusions:

    • Comicronization is an effective strategy for enhancing the bioavailability of CI-1040.
    • The approach successfully mitigates particle agglomeration issues.
    • This method holds promise for improving drug delivery of poorly soluble compounds.