Enteric formulations of physiologically active peptides and proteins
OwnerKanji Takadainventor
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Abstract
An enteric formulation for a proteinous drug which protects it from enzymatic degradation and promotes its uptake by the intestinal tract when administered orally, comprises either a solid mass of an intimate mixture of the drug, a nontoxic nonionic surfactant, and an enteric material, or a solid mass of an intimate mixture of the drug with the nonionic surfactant covered by a discrete enteric coating.
Claims20
A solid enteric pharmaceutical formulation consisting of a particulate intimate physical mixture of a (a) physiologically active peptide or protein, (b) a nontoxic nonionic surfactant, (c) a pharmaceutically acceptable solid organic acid selected from the group consisting of tartaric, malonic, maleic, malic, citric and cinnamic acids (d), at least 50 wt. %, based on the weight of the pharmaceutical formulation, of a pharmaceutically acceptable, enteric polymer which is soluble in a volatile organic solvent and which dissolves selectively from the mixture in duodenal juice when the mixture is ingested and, optionally, (e) either or both of a pharmaceutically acceptable solid diluent and an effervescing agent.
A solid ingestible enteric pharmaceutical formulation consisting of a solid particulate mixture of (a) a physiologically active peptide or protein, (b) a nontoxic nonionic surfactant, (c) a pharmaceutically acceptable solid organic acid selected from the group consisting of tartaric, malonic, maleic, malic, citric and cinnamic acids and, optionally, (d) an inert solid diluent;
- the particles of which are covered with at least 50 wt. %, based on the weight of the formulation, of a polymer as a discrete enteric coating which covers the surface of the individual particles of the mixture, which coating is soluble in a volatile organic solvent and dissolves selectively in duodenal juice when the mixture is ingested.
Dependencies are inferred from the claim text.