Development of potential novel cushioning agents for the compaction of coated multi-particulates by co-processing micronized lactose with polymers.

This work aimed to explore the potential of lactose as novel cushioning agents with suitable physicomechanical properties by micronization and co-spray drying with polymers for protecting coated multi-particulates from rupture when they are compressed into tablets. Several commercially available lactose grades, micronized lactose (ML) produced by jet milling, spray-dried ML (SML), and polymer-co-processed SMLs, were evaluated for their material characteristics and tableting properties. Hydroxypropylcellulose (HPC), hydroxypropylmethylcellulose (HPMC), and polyvinylpyrrolidone (PVP) at three different levels were evaluated as co-processed polymers for spray drying. Sugar multi-particulates layered with chlorpheniramine maleate followed by an ethylcellulose coat were tableted using various lactose types as fillers. Drug release from compacted multi-particulate tablets was used to evaluate the cushioning effect of the fillers. The results showed that the cushioning effect of lactose principally depended on its particle size. Micronization can effectively enhance the protective action of lactose. Although spray drying led to a small reduction in the cushioning effect of ML, it significantly improved the physicomechanical properties of ML. Co-spray drying with suitable polymers improved both the cushioning effect and the physicomechanical properties of SML to a certain degree. Among the three polymers studied, HPC was the most effective in terms of enhancing the cushioning effect of SML. This was achieved by reducing yield pressure, and enhancing compressibility and compactibility. The combination of micronization and co-spray drying with polymers is a promising method with which new applications for lactose can be developed.