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

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 pharmaceuti...

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Hauptverfasser: VENCL-JONCIC MAJA, DIORIO CHRISTOPHER RICHARD, RAO SRIPRIYA VENKATA RAMANA, SHAH SYED MUZAFAR, MURPHY EUGENE
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creator VENCL-JONCIC MAJA
DIORIO CHRISTOPHER RICHARD
RAO SRIPRIYA VENKATA RAMANA
SHAH SYED MUZAFAR
MURPHY EUGENE
description 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.
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subjects HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title Coated drug spheroids and uses thereof for eliminating or reducing conditions such as emesis and diarrhea
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