Abstract
The aim of the present study was to develop an alternative process to spray granulation in order to prepare high loaded spherical nicotinamide (NAM) pellets by wet extrusion and spheronisation. Therefore, a quality by design approach was implemented to model the effect of the process parameters of the extrusion-spheronisation process on the roundness, roughness and useable yield of the obtained pellets. The obtained results were compared to spray granulated NAM particles regarding their characteristics and their release profile in vitro after the application of an ileocolon targeted shellac coating. The wet extrusion-spheronisation process was able to form highly loaded NAM pellets (80%) with a spherical shape and a high useable yield of about 90%. However, the water content range was rather narrow between 24.7% and 21.3%. The design of experiments (DoE), showed that the spheronisation conditions speed, time and load had a greater impact on the quality attributes of the pellets than the extrusion conditions screw design, screw speed and solid feed rate (hopper speed). The best results were obtained using a low load (15 g) combined with a high rotation speed (900 m/min) and a low time (3–3.5 min). In comparison to spray granulated NAM pellets, the extruded NAM pellets resulted in a higher roughness and a higher useable yield (63% vs. 92%). Finally, the coating and dissolution test showed that the extruded and spheronised pellets are also suitable for a protective coating with an ileocolonic release profile. Due to its lower specific surface area, the required shellac concentration could be reduced while maintaining the release profile.
Highlights
Advancements in drug delivery systems were and are highly present in the pharmaceutical and food research area
Shellac can be used for food as edible coatings [18,19,20] and/or nutraceuticals because of its generally recognized as safe (GRAS) status and its legal approval as a food additive [21]
A quality by design (QbD) approach, which is often applied in the pharmaceutical industry to guarantee the product quality [22,23] was used to define the quality target product profile (QTPP) with its critical quality attributes (CQAs)
Summary
Advancements in drug delivery systems were and are highly present in the pharmaceutical and food research area. Fluid-bed processes and wet extrusion-spheronisation provide high drug load capacity and uniformity of pellets [1,9,10] including moderate to highly water-soluble compounds such as nicotinamide (NAM). The topical delivery to the colon area of NAM was achieved by application of an adapted shellac coating. NAM cores produced by wet extrusion-spheronisation process will be compared to the spray granulated cores in this study as an alternative process. The aim of the present study was to modulate the extrusion/spheronisation process in order to produce highly loaded NAM pellets and to compare their properties to spray granulated NAM pellets. For the wet extrusion-spheronisation process a high drug load of 80% NAM combined with 20% MCC (Avicel PH101) was used. The release profile of the coated extrudates were compared with coated spray granulates
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