Development of fast disintegrating pellet formulations based on Ludiflash(R)

摘要

The aim of this study was the preparation offast disintegrating pellets. Ludiflash(R) Was combinedwith microcrystalline cellulose (MCC) in differentratios. Two different drugs were used as models:Paracetamol with high water solubility and highpermeability (BCS I) and ibuprofen with low watersolubility and high permeability (BCS II). The drugloading was varied between 20 and 50 % wt.Ethanol/water was used as granulation liquid indifferent concentrations. A mass ratio ofLudiflash/MCC (Avicel PH 101) of 90:10 was foundto be well suited for the pellet preparation byextrusion and spheronisation.A drug loading of 30 % ibuprofen and 50 %paracetamol respectively, yields fast disintegratingand mechanically stable pellets. To evaluate thesurface and cross-sectional area, electronmicroscopy was used. For characterization purposethe moisture contents of the products at each stepwere measured, the particle size distribution of thedried pellets was studied and the disintegrationbehavior and friability were examined. For bothmodel drugs, spherical pellets with a high yield (>78%), low friability (< 0.6%) and acceptablesphericity (AR<1.2) were obtained. All pelletsdisintegrated within 9 minutes.