Production and Characterization of Immediate Release Lansoprazole Pellets Produced by Melt Pelletization Vesna Kroselj, Robert Pisek and Franc Vrecer Krka, d.d., Research and Development Division, Novo mesto (Slovenia) Corresponding author: Vesna Kroselj, KRKA, d.d., Novo mesto, R&D Division, Smarjeska cesta 6, 8501 Novo mesto (Slovenia), e-mail: vesna-kroselj@krka.biz The aim of this study was to evaluate melt pelletization in a high shear mixer as a method for the production of immediate release spherical agglomerates containing lansoprazole (CAS 103577-45-3), thereby increasing the dissolution rate of this poorly soluble model drug.
The pellets were prepared in a laboratory- scale high-shear mixer, using two types of binders: macrogolglycerides (Gelucire 44/14 [MG 1] and Gelucire 50/13 [MG 2]) and poloxamers (poloxamer 188, Lutrol® F 68 [PX 1] and poloxamer 407, Lutrol F 127 [PX 2]).
The particle size analysis showed that the particle size distribution was wide in all cases, regardless of the binder used. Stereomicroscopic and scanning electron microscopic (SEM) analysis revealed the pellets to be round and smooth in case of macrogolglycerides irrespective of the fraction analyzed. For PX 1, the bigger pellets were of more spherical shape. Granules containing PX 2 had an irregular shape and rugged surface regardless of their size. The in vitro dissolution test showed an increase in the dissolution rates of pellets when compared to pure drug and physical mixtures. Further studies of the pellets suggested that the improvement of the dissolution could be explained by the fine distribution of lansoprazole within the pellets and the ability of carriers to prevent reaggregation of drug particles and improve their wettability.
The results of this work suggest that the melt pelletization technique using hydrophilic melting binders is an easy and fast method to produce pellets with lansoprazole with improved dissolution rate. Key words High-shear mixer • Lansoprazole • Macrogolglycerides • Melt pelletization • Poloxamers |
