Coated drug spheroids and uses thereof for eliminating or reducing conditions such as emesis and diarrhea

摘要

The disclosure relates to an oral pharmaceutical formulation comprising coated spheroids of a kinase inhibitor such as neratinib, which formulation is designed to reduce or eliminate side effects associated with existing oral formulations of kinase inhibitors. Particularly disclosed is a pharmaceutically acceptable composition of (i) spheroid particles comprising: (a) 30-70 weight percent of an active ingredient selected from the group consisting of neratinib, bosutinib, erlotinib, sutent, tykerb, a 4-mino-3-cyanoquinoline compound and pharmaceutically acceptable salts thereof; (b) 20-30 weight percent of one or more fillers; (c) 5-15 weight percent of one or more wetting agents, said spheroid particles comprising 70-83 weight percent of the total composition; (ii) a sub-coating applied to said spheroid particles further comprising 1-4 weight percent of one or more pharmaceutically acceptable cellulose based polymers and (iii) 16-30 weight percent of one or more pharmaceutically acceptable polymers as an enteric coating applied to said sub-coating, said coating components (ii) and (iii) comprising 17-30 weight percent of the total composition.