Jet-milling co-grounds of APIs with polysorbate 80, lecithin and sucrose esters: Particle characteristics and impacts on agglomeration and dissolution efficiency

Abstract

The jet-milling co-grounds of active pharmaceutical ingredients (APIs) with excipients, including polysorbate 80 (PS), lecithin (LT) and sucrose esters (SEs), were characterized for particle size, specific surface area, scanning electron microscopy (SEM), and dissolution testing. Particle size analysis indicated that increasing proportion of PS or LT in the co-grounds either increased or maintained particle size, while the SEs-API co-grounds exhibited a reduction or no change in size. Specific surface area increased with higher proportions of SEs in the co-grounds but decreased for PS-API and LT-API co-grounds. SEM analysis showed that PS and LT promoted agglomeration in the co-grounds, while SEs reduced agglomeration. Dissolution profiles fluctuated depending on the extent of agglomeration. In conclusion, co-grinding with PS, LT and SEs can enhance the dissolution efficiencies of APIs. SEs, in particularly, demonstrated the ability to reduce agglomeration and improve the dissolution efficiency, suggesting that SEs may aid in simplifying the manufacturing process of poorly water-soluble drugs and enhanced their dissolution performance.