Drug‐β‐Cyclodextrin Containing Pellets Prepared with a High‐Shear Mixer

Abstract

This work was aimed at investigating the preparation of β‐cyclodextrin‐microcrystalline cellulose pellets by means of a high‐shear mixer, both in the absence or in the presence of ibuprofen as model drug. Drug loading of pellets was accomplished by means of two alternative techniques: 1) solution layering or 2) powder layering. The prepared pellets were characterised in terms of size distribution, shape factor, friability and dissolution rate. The interaction between ibuprofen and β‐cyclodextrin was monitored by Differential Scanning Calorimetry (DSC). Micro Fourier Transform Infrared spectroscopy (MicroFTIR) was applied to determine the distribution of components within each pellet on a micro scale. Pellets with narrow size distribution and containing up to about 90% of BCD were prepared using water as binder. The process yield resulted around 84 and 63% for drug‐free and medicate pellets respectively. Drug loaded pellets with favourable technological and biopharmaceutical characteristics can be obtained both by powder or solution layering techniques. The latter proved to be more suitable for producing pellets with high drug contents, reduced friability and high drug dissolution rates.

Key Words:

• Pelletization
• High‐shear mixer
• β‐Cyclodextrin
• Ibuprofen
• Shape factor
• Drug crystallinity
• Dissolution
• Multiparticulate drug delivery system