Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-9265811-B2
Publication Date
2016-02-23
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 invention relates to an oral dosage composition comprising an effective amount of Larazotide acetate (AT1001) and comprising first delayed-release particles and second delayed-release particles. The first delayed-release particles are capable of releasing Larazotide acetate in the duodenum of a patient, and the second delayed-release particles are capable of releasing Larazotide acetate in the jejunum of a patient.
Each delayed-release particle type includes a core particle, a coat comprising Larazotide acetate, and an outer delayed-release coating outside the coat. The outer delayed-release coating comprises a co-polymer of acrylate or methacrylate, is stable in simulated gastric fluid, and triggers release in simulated intestinal fluid having a pH greater than 5.
The described compositions are based on enteric delayed-release pharmaceutical compositions that deliver tight junction effectors to small intestine targets including duodenum and jejunum. The invention includes delayed-release coating materials such as Eudragit-type polymers and multiparticulate systems for staggered release timing.
Claims Coverage
The document provides two independent claim structures focused on oral dosage compositions using delayed-release particles of Larazotide acetate with duodenum-targeting and jejunum-targeting release behavior. The inventive features are centered on particle architecture and on stability and release thresholds in simulated gastric versus simulated intestinal fluid.
Duodenum- and jejunum-selective delayed-release particles for Larazotide acetate
An oral dosage composition comprising an effective amount of Larazotide acetate (AT1001) with first delayed-release particles releasing Larazotide acetate in the duodenum and second delayed-release particles releasing Larazotide acetate in the jejunum, where the first and second delayed-release particles each comprise a core particle, a coat comprising Larazotide acetate, and an outside delayed-release coating comprising a co-polymer of acrylate or methacrylate; the outside delayed-release coating is stable in simulated gastric fluid and releases at least 70% upon exposure to simulated intestinal fluid having a pH greater than 5.
Population of duodenum- and jejunum-targeting delayed-release particles
An oral dosage composition comprising a population of delayed-release particles containing Larazotide acetate (AT1001), where the population consists of first delayed-release particles releasing Larazotide acetate in the duodenum and second delayed-release particles releasing Larazotide acetate in the jejunum; each particle type includes a core particle, a coat comprising Larazotide acetate, and an outside delayed-release coating comprising a co-polymer of acrylate or methacrylate that is stable in simulated gastric fluid and releases at least 70% upon exposure to simulated intestinal fluid having a pH greater than 5.
Across both independent claims, the coverage is directed to oral formulations of Larazotide acetate using two types of delayed-release particles differentiated by anatomical release target (duodenum versus jejunum). The main inventive aspects are the particle structure and the specified stability and release thresholds in simulated gastric fluid versus simulated intestinal fluid (pH greater than 5).
Stated Advantages
Enables Larazotide acetate release in a patient in the duodenum using first delayed-release particles and release in the jejunum using second delayed-release particles.
Provides delayed-release coatings that are stable in simulated gastric fluid while releasing at least 70% under simulated intestinal fluid conditions.
Documented Applications
Oral administration of Larazotide acetate (AT1001) to deliver release in the duodenum and jejunum of a patient using first and second delayed-release particles.
Simulated dissolution/stability characterization in simulated gastric fluid and simulated intestinal fluid to support the release behavior of duodenum- versus jejunum-capable delayed-release particles.
Interested in licensing this patent?