Gastric residence systems with release rate-modulating films
Inventors
KANASTY, Rosemary • BHISE, Nupura • ZALE, Stephen • Carter, Bennett • Yang, Jung Hoon • Bellinger, Andrew • Low, Susan • Wright, James • Altreuter, David • Gardner, Colin
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-12023406-B2
Publication Date
2024-07-02
Expiration Date
Abstract
The invention provides gastric residence systems, or components of gastric residence system such as segments or elongate members of gastric residence systems, with release rate-modulating films and methods for making and using such systems. The release rate-modulating films provide good control over release of agents (such as therapeutic, diagnostic, or nutritional agents) present in the gastric residence system. The films also permit higher drug loading in the gastric residence systems and components of gastric residence systems while maintaining good control over release of agents. Some embodiments of the films can provide resistance against burst release of agent upon exposure to alcohol.
Core Innovation
The invention provides a gastric residence system for delivering a therapeutically effective amount of an agent or a pharmaceutically acceptable salt. The system includes a compacted configuration and an uncompacted configuration and comprises a plurality of elongate members affixed to a central elastomer. At least one elongate member includes a carrier polymer and the agent or salt, with the elongate member surface coated by a release-rate modulating polymer film.
The release-rate modulating polymer film is configured to limit differential release in 40% ethanol/60% simulated gastric fluid over one hour relative to release in 100% simulated gastric fluid over one hour. In particular, the release in 40% ethanol/60% simulated gastric fluid over one hour is no more than about 40% higher than the release from an equivalent system in 100% simulated gastric fluid over one hour. The system is configured to release the agent or salt over a specified gastric residence period.
The polymer film comprises one or more polyester materials with a repeating unit of the form —R1—O—C(≈O)—, where R1 is selected from C1–C12 alkylene groups, ethers containing between two and twelve carbon atoms, and polyethers containing between three and twelve carbon atoms. The elongate members and the central elastomer support compacted and uncompacted, including star/stellate or ring configurations, for gastric residence and subsequent passage through the pylorus after the specified period.
Claims Coverage
The independent claims recite a gastric residence system architecture plus constraints on release behavior and the polyester film repeating unit chemistry. Four inventive features are identified.
Compact/uncompacted gastric residence system with elongate members and central elastomer
A gastric residence system having a compacted configuration and an uncompacted configuration, comprising a plurality of elongate members affixed to a central elastomer.
Carrier polymer with agent and release-rate modulating polymer film on elongate member surface
At least one elongate member comprises a carrier polymer, the agent or the pharmaceutically acceptable salt thereof, and a release-rate modulating polymer film coated on the surface of the at least one elongate member.
Ethanol-challenge release constraint using 40% ethanol/60% simulated gastric fluid versus 100% simulated gastric fluid
The release-rate modulating polymer film is configured such that release of agent or salt from the system in 40% ethanol/60% simulated gastric fluid over one hour is no more than about 40% higher compared to release of agent or salt from an equivalent system in 100% simulated gastric fluid over one hour.
Polyester release-rate modulating film with repeating unit —R1—O—C(≈O)— and defined R1 selection
The release-rate modulating polymer film comprises one or more polyester materials with a repeating unit of the form —R1—O—C(≈O)—, wherein R1 is selected from C1–C12 alkylene groups, ethers containing between two and twelve carbon atoms, and polyethers containing between three and twelve carbon atoms.
Overall, the claim coverage centers on a compacted/uncompacted gastric residence system formed from elongate members affixed to a central elastomer, where a polyester release-rate modulating polymer film on carrier polymer-containing elongate members provides controlled release under an ethanol challenge constraint while supporting release over a specified gastric residence period.
Stated Advantages
Limits differential release under ethanol challenge, with release in 40% ethanol/60% simulated gastric fluid over one hour no more than about 40% higher than release in 100% simulated gastric fluid over one hour.
Provides release-rate modulation via polyester release-rate modulating polymer films having a defined repeating unit chemistry.
Enables release of an agent or salt over a specified gastric residence period.
Documented Applications
Use as a gastric residence system to release a therapeutically effective amount of an agent or a pharmaceutically acceptable salt in the stomach over a specified gastric residence period.
Release profiling and evaluation of coated versus uncoated segments/elongate members in simulated gastric fluids and 40% ethanol/60% simulated gastric fluid challenge conditions.
Interested in licensing this patent?