For some time, the pharmaceutical market has been encountering a lack of innovative drugs designed especially for the pediatric population, often the most demanding patients. Therefore, a satisfactory adherence is of key importance.
In the master's thesis, granules that are potentially interesting for further development were developed. Their application is carried out by means of a drinking straw. The granules were filled into a patented straw with two valves preventing reverse water flow. First, various pharmaceutical excipients, such as lactose, sugar, mannitol, isomalt, etc., were filled in the straw, where their behavior was observed during the sipping (potential clogging - formation of plugs), and approximate dissolution time was also determined. Excipients with the best straw behavior were then granulated using a high shear mixer by wet granulation technique. Thus, granules of different particle size distributions were obtained, and their straw behavior was observed (the potential straw clogging and flush volume values of granules). Granules were also evaluated quantitatively using a newly developed instrument capable of measuring the pressure during the straw sipping and enabling a more accurate observation of the required flush volumes of granules. Based on placebo granule straw behavior, granules with 30% of cefprozil content, as a pharmaceutically active ingredient, were also manufactured.
During the experimental work, it was found that the particle size in the straw has the greatest influence on straw behavior, where the particles larger than 710 ?m significantly reduce the chance of straw clogging. It was also found that the best granules for straw filling were sugar based, namely those in which milled sugar was granulated with purified water as a granulating liquid only, granulating water dispersion of PVP K30 and SDS was also good. SDS added in the form of a granulating liquid during granulation can significantly reduce granule flush volumes, but on the other hand, slightly higher sipping pressures were measured. In addition, it was found that granules with a higher citric acid content (15%) had poorer straw behavior compared to those with a lower (5%) citric acid content, and smaller citric acid particles used were more efficient. The effervescent granule is also not suitable for use in this kind of straw, as the straw was completely clogged. It was found that besides the granule composition, particle morphology plays an important role, as the higher amount of granulating liquid added during granulation results in granules having better straw properties. Straw volume filling had also a significant effect on the granule straw behavior.