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Publication Number
US-9241969-B2
Publication Date
2016-01-26
Expiration Date
Abstract
Enteric compositions comprising one or more tight junction agonists and/or one or more tight junction antagonists are provided. Compositions of the invention may comprise a delayed-release coating disposed over a tight junction agonist and/or tight junction antagonist layer which may be disposed over an inert core. Delayed-release coatings may be substantially stable in gastric fluid and substantially unstable in intestinal fluid, thus providing for substantial release of the tight junction agonist and/or antagonist from the composition in the duodenum or jejunum of the small intestine.
Core Innovation
The described invention relates to treating a celiac patient by administering a peptide having the amino acid sequence of SEQ ID NO: 1. The peptide is provided as an oral dosage, delayed-release composition that includes peptide-coated beads with a delayed release coating that is a 1:1 co-polymer of methacrylic acid and ethyl acrylate.
The delayed release coating is stable in gastric fluid and unstable in near neutral to alkaline environments so as to release peptide in the duodenum. A performance requirement is specified such that at least 70% of the peptide in the beads is released upon exposure for 90 minutes to simulated intestinal fluid having a pH of greater than 5. The beads contain 0.1 to 0.8% by weight of the peptide.
A further aspect uses two bead populations having the same 1:1 methacrylic acid/ethyl acrylate co-polymer delayed release coating behavior. The first population is configured to release peptide in the duodenum, and the second population is configured to release peptide in the jejunum. At least 70% of the peptide in the second bead population is released about 30 minutes after the first population in simulated intestinal fluid having a pH of greater than 5.
Claims Coverage
The partial content provides two independent claims. Across these claims, the coverage is centered on delayed-release oral peptide-coated beads with a 1:1 methacrylic acid and ethyl acrylate co-polymer coating, gastric stability and near-neutral-to-alkaline instability, specific peptide loading, and simulated intestinal release performance.
Duodenal release with 1:1 methacrylic acid/ethyl acrylate bead coating
Administering a peptide having the amino acid sequence of SEQ ID NO: 1 to the duodenum using an oral dosage delayed-release composition that contains peptide-coated beads with a delayed release coating that is a 1:1 co-polymer of methacrylic acid and ethyl acrylate. The coating is stable in gastric fluid and unstable in near neutral to alkaline environments so as to release peptide in the duodenum, with at least 70% of the peptide released upon exposure for 90 minutes to simulated intestinal fluid having a pH greater than 5. The beads contain 0.1 to 0.8% by weight of said peptide.
Two-stage duodenal-to-jejunal release using first and second bead populations
Administering a peptide having the amino acid sequence of SEQ ID NO: 1 to a patient as an oral dosage delayed-release composition containing a first population of peptide-coated beads configured to release peptide in the duodenum and a second population configured to release peptide in the jejunum. Both bead populations have a delayed release coating that is a 1:1 co-polymer of methacrylic acid and ethyl acrylate, stable in gastric fluid and unstable in near neutral to alkaline environments. The first population meets a requirement of at least 70% peptide release upon exposure for 90 minutes to simulated intestinal fluid having a pH greater than 5, and the second population meets a requirement of at least 70% peptide release about 30 minutes after the first population in the same simulated intestinal fluid condition. The beads contain 0.1 to 0.8% by weight of said peptide.
The independent claims consistently require oral delayed-release peptide-coated beads using a 1:1 methacrylic acid/ethyl acrylate co-polymer coating that is stable in gastric fluid and unstable in near neutral to alkaline environments. Claim coverage further specifies peptide loading and simulated intestinal release thresholds, with one claim focused on duodenal release and the other adding a second bead population for a duodenal-to-jejunal timing sequence.
Stated Advantages
Documented Applications
No documented applications found
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