Surface engineered excipients: I. improved functional properties of fine grade microcrystalline cellulose

Document Type

Article

Publication Date

1-30-2018

Abstract

Excipients with good flowability, bulk density as well as compaction properties are desired for use in tableting since they play important roles in formulation development and processing, including, handling, mixing, feeding and compaction. The objective of this paper is to examine the feasibility of using dry coating based surface modification of microcrystalline cellulose, Avicel PH-105, to produce an engineered fine grade (<30 μm) excipient that has all three desired properties. Using a material sparing high-intensity vibrational mixer, Avciel PH-105 is dry coated with 1 wt% Aerosil 200, selected due to its relatively higher dispersive surface energy and lower particle size amongst other silica choices. The results indicated that as expected, the bulk density and flowability are significantly improved, while there was an appreciable loss of compaction. To minimize the loss of compaction, attributed to decreased surface energy after coating, while maintaining improved bulk density and flowability, the effect of reduced silica amount was examined. Remarkably, at reduced levels (0.5 wt% to 0.7 wt%) of Aerosil 200, significant improvements in bulk density and flowability were attained with only 9%–12% compaction reduction. The properties of the surface-engineered excipients were compared with several other commercially available pharmaceutical excipients using two different processibility or regime maps; tablet tensile strength versus bulk density or flow function coefficient (FFC). The surface engineered excipients exhibited the best overall performance establishing a promising pathway to engineer excipients using dry processing instead of complex processes such as spray drying.

Identifier

85035795714 (Scopus)

Publication Title

International Journal of Pharmaceutics

External Full Text Location

https://doi.org/10.1016/j.ijpharm.2017.11.060

e-ISSN

18733476

ISSN

03785173

PubMed ID

29191481

First Page

127

Last Page

137

Issue

1

Volume

536

Grant

EEC- 0540855

Fund Ref

National Science Foundation

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