Effect of Particle Size and Polymer Loading on Dissolution Behavior of Amorphous Griseofulvin Powder

Kai Zheng, Zhixing Lin, Maxx Capece, Kuriakose Kunnath, Liang Chen, Rajesh N. Davé

Research output: Contribution to journalArticlepeer-review

10 Scopus citations

Abstract

The effect of particle size on the dissolution behavior of the particles of amorphous solid dispersions (ASDs) of griseofulvin (GF), with 0%-50% Kollidon ® VA 64 as a crystallization inhibitor is investigated. Both the final dissolved GF concentration and the dissolution rate of GF ASDs were found to be inversely proportional to the particle size. The solution concentrations for the smallest (45-75 μm) size group with different polymer loadings were significantly higher than those for the largest (250-355 μm) group regardless of the initial GF amount. Specifically, the dissolution rate of GF ASDs with 50% polymer loading for the finest group was 2.7 times higher than for the largest group under supersaturating conditions. The rates of dissolution and recrystallization were assessed through surface concentration (C s ) and Avrami recrystallization rate kinetics, where the solid-state recrystallization was confirmed using Raman spectroscopy. Outcomes indicated that particle size reduction enhanced ASD drug loading by reducing the amount of polymer necessary as finest size ASDs initially dissolve faster, negating their higher recrystallization rate. Kollidon® VA 64 at 30% loading was sufficient to inhibit the GF recrystallization. Overall, the combination of particle size reduction and recrystallization inhibition is effective for improved dissolution behavior of GF ASDs.

Original languageEnglish (US)
Pages (from-to)234-242
Number of pages9
JournalJournal of Pharmaceutical Sciences
Volume108
Issue number1
DOIs
StatePublished - Jan 2019

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Keywords

  • amorphous state
  • dissolution rate
  • particle size
  • solid dispersions

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