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Microstructural effects of high-energy grinding on poorly soluble drugs: the case study of efavirenz

Published online by Cambridge University Press:  21 February 2017

Elisa Cappelletto ,
Luca Rebuffi ,
Alberto Flor  and
Paolo Scardi
Elisa Cappelletto*
Affiliation:
Department of Civil, Environmental and Mechanical Engineering, University of Trento, via Mesiano 77, 38123 Trento, Italy
Luca Rebuffi
Affiliation:
Elettra-Sincrotrone Trieste, Area Science Park, Basovizza, 34149 Trieste, Italy
Alberto Flor
Affiliation:
Department of Civil, Environmental and Mechanical Engineering, University of Trento, via Mesiano 77, 38123 Trento, Italy
Paolo Scardi
Affiliation:
Department of Civil, Environmental and Mechanical Engineering, University of Trento, via Mesiano 77, 38123 Trento, Italy
*
a)Author to whom correspondence should be addressed. Electronic mail: [email protected]
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Abstract

In this work, a poorly water-soluble drug (efavirenz) was mechanically activated by ball-milling. The effect of the mechanical activation on the dissolution behavior was investigated considering changes in the particle size and morphology. The powder diffraction was used to follow the comminution process, verifying phase compositions, and crystalline domain size. The interplay between domain and grain size was studied in relation to the solubility rate, through specific dissolution tests. Finally, the morphological characterization has allowed to complete the physical–chemical characterization of the milled powders. This study demonstrated that the mechanical activation of the drug leads the particle size reduction and, with a long milling time, morphological changes. The grain size reduction is not always sufficient to increase the solubility: morphology and agglomeration grade play an important role in the dissolution process.

Keywords

Efavirenznanosizingcrystalline domain sizecomminution processesdissolutionball milling
Type
Technical Articles
Information
Powder Diffraction , Volume 32 , Supplement S1 , September 2017 , pp. S135 - S140
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Copyright
Copyright © International Centre for Diffraction Data 2017 

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