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Effect of grinding on the solid state stability and particle dissolution of acyclovir polymorphs.

08:00 EDT 7th June 2017 | BioPortfolio

Summary of "Effect of grinding on the solid state stability and particle dissolution of acyclovir polymorphs."

The present work investigated the solid state change of four acyclovir polymorphs when ground at room temperature (Method A) and under cryo-grinding in the presence of liquid nitrogen (Method B). Modifications in particle size and shape (evaluated by scanning electron microscopy) and in the water content (evaluated by thermal analysis) were related to transitions at the solid state, as confirmed by X-ray powder diffractometry. Anhydrous Form I was stable under grinding by both methods A and B. The anhydrous Form II was stable during grinding under Method A, while it was progressively converted to the hydrate Form V during grinding under Method B. The hydrate Form V was stable under Method A, while it was converted to the anhydrous Form I after 15 min and then to the hydrate Form VI after 45 min of grinding. The hydrate Form VI proved to be stable under grinding by both Methods A and B. Thus Form I and VI were the only forms that yielded a sizeable decrease in particle size under grinding, with a consequent increase in particle dissolution rate, while maintaining solid state physicochemical stability. Form I treated under Method B grinding gave the best dissolution rate.

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This article was published in the following journal.

Name: Journal of pharmaceutical sciences
ISSN: 1520-6017
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