Simultaneous micronization and surface modification for improvement of flow and dissolution of drug particles
Document Type
Article
Publication Date
8-30-2011
Abstract
Simultaneous micronization and surface modification of drug particles is considered in order to mitigate disadvantages of micronization, e.g.; agglomeration, poor flowability, marginal increase in surface area and low bulk density. Particles of ibuprofen (102 μm), a model drug, pre-blended with hydrophilic nano-silica, are micronized down to 10 and 5 μm in a continuous fluid energy mill (FEM) to obtain fine surface modified particles. The solid feeding rate and the grinding pressure are shown as critical parameters for achieving the desired particle size and size distribution. The powder properties were characterized via SEM, laser scattering, powder rheometer with shear-cell, and dissolution test. Significant improvement in flow properties and dissolution rate was observed when micronization accompanied surface modification. Additionally, co-grinding with water-soluble polymer during micronization led to further increase in bulk density and more enhanced dissolution rate improvement, which is attributed to improved wettability. XRD, DSC and Raman were used to examine crystallinity, indicating minimal detectable physical transformation with FEM processed ibuprofen. The surface modified, micronized powders also showed improved dispersion, higher bulk densities (>0.4 g/ml), reduced electrostatic, and higher flowability (FFC ≥ 6) compared to just micronized powder (0.19 g/ml, FFC = 1.0), indicating they may be used in high drug loaded formulations amenable to direct compression. © 2011 Elsevier B.V. All rights reserved.
Identifier
79960185799 (Scopus)
Publication Title
International Journal of Pharmaceutics
External Full Text Location
https://doi.org/10.1016/j.ijpharm.2011.05.070
e-ISSN
18733476
ISSN
03785173
PubMed ID
21664954
First Page
185
Last Page
195
Issue
1-2
Volume
415
Grant
EEC-0540855
Fund Ref
National Science Foundation
Recommended Citation
Han, Xi; Ghoroi, Chinmay; To, Daniel; Chen, Yuhua; and Davé, Rajesh, "Simultaneous micronization and surface modification for improvement of flow and dissolution of drug particles" (2011). Faculty Publications. 11209.
https://digitalcommons.njit.edu/fac_pubs/11209
