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US 8,524,281 B2Granted
Coated drug spheroids and uses thereof for eliminating or reducing conditions such as emesis and diarrhea
AssigneeWyeth
InventorsSripriya Venkata Ramana Rao, Syed Muzafar Shah, Christopher Richard Diorio, Maja Vencl-Joncic, Eugene James Murphy
Life of this patent
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Abstract
The present invention provides 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.
Claims15
A pharmaceutically acceptable composition of (i) spheroid particles comprising:
- (a) 30-70 weight percent of (E)-N-(4-(3-chloro-4-(pyridin-2-ylmethoxy)phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide or a pharmaceutically acceptable salt thereof as an active ingredient;
- (b) 20-30 weight percent of one or more fillers;
- and (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;
- wherein the enteric coated composition has an AUC/Cmax ratio that is the same as or less than the AUC/Cmax ratio of an immediate release formulation of the active ingredient without enteric coating.
2 more elements
A pharmaceutically acceptable composition of (i) spheroid particles comprising:
- (a) 30-70 weight percent of (E)-N-(4-(3-chloro-4-(pyridin-2-ylmethoxy)phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide maleate as an active ingredient;
- (b) 20-30 weight percent of microcrystalline cellulose;
- and (c) 5-15 weight percent of a polysorbate, said spheroid particles comprising 70-84 weight percent of the total composition;
- (ii) a sub-coating applied to said spheroid particles further comprising 1-4 weight percent of hydroxypropylcellulose and (iii) 16-30 weight percent of a methacrylic acid polymer as an enteric coating applied to said sub-coating, said coating components (ii) and (iii) comprising 16-30 weight percent of the total composition;
- wherein the enteric coated composition has an AUC/Cmax ratio that is the same as or less than the AUC/Cmax ratio of an immediate release formulation of the active ingredient without enteric coating.
2 more elements
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-amino-3-cyanoquinoline compound and pharmaceutically acceptable salts thereof;
- (b) 20-30 weight percent of one or more fillers;
- and (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;
- wherein the enteric coated composition has an AUC/Cmax ratio that is the same as or less than the AUC/Cmax ratio of an immediate release formulation of the active ingredient without enteric coating.
2 more elements
Dependencies are inferred from the claim text.