Gastric residence systems for sustained release of therapeutic agents and methods of use thereof
Inventors
KANASTY, Rosemary • Bellinger, Andrew • Gardner, Colin • Grant, Tyler • MOORTHY, Saumya
Assignees
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Publication Number
US-11576859-B2
Publication Date
2023-02-14
Expiration Date
Abstract
Gastric residence systems comprising therapeutic agent formulations for sustained gastric release of therapeutic agents are disclosed, as well as methods for using such systems. The systems are characterized by use of a dispersant in the formulations, which improves the burst release characteristics and long-term release rate characteristics of the systems. Milling of therapeutic agent can also be performed to prepare agent particles of desired size.
Core Innovation
The invention relates to a gastric residence system for administration to a patient that includes a plurality of carrier polymer-agent components. The carrier polymer comprises vinylpyrrolidone-vinyl acetate copolymer (VA64) and polycaprolactone, and a therapeutic agent, or pharmaceutically-acceptable salt thereof, is blended into the carrier polymer. The carrier polymer-agent components are linked together by one or more coupling polymer components, wherein at least one coupling polymer component is an elastomer.
The gastric residence system further includes a dispersant comprising silica (SiO2) and an excipient that comprises a release enhancer comprising poloxamer P407 and a stabilizer. The system has a compacted form in a container suitable for administration orally or through a feeding tube, and an uncompacted form when released from the container. The system is retained in the stomach for a residence period between at least about 24 hours and about one month.
The system releases a therapeutically effective amount of the therapeutic agent over an effective release period while releasing less than about 20% of the therapeutic agent, or pharmaceutically-acceptable salt thereof, within about a six-hour period. Therapeutic agents are selected from doxycycline, donepezil, ivermectin, risperidone, cetirizine, and rosuvastatin, or pharmaceutically-acceptable salts thereof.
Claims Coverage
The document provides two independent claims. Across these claims, the inventive architecture is a gastric residence system with linked elastomer-coupled carrier polymer-agent components including VA64 and polycaprolactone, a silica dispersant, and an excipient with poloxamer P407 and a stabilizer, configured for compacted oral or feeding-tube administration and stomach retention with controlled early release.
Linked elastomer-coupled carrier polymer-agent components
A plurality of carrier polymer-agent components linked together by one or more coupling polymer components, wherein at least one of the one or more coupling polymer components is an elastomer.
VA64 and polycaprolactone blended carrier
The carrier polymer comprises vinylpyrrolidone-vinyl acetate copolymer (VA64) and polycaprolactone, and a therapeutic agent or a pharmaceutically-acceptable salt thereof is blended into the carrier polymer.
Silica dispersant and poloxamer P407 release enhancer with stabilizer
The system includes a dispersant comprising silica (SiO2) and an excipient comprising a release enhancer comprising poloxamer P407 and a stabilizer.
Compacted container form and uncompacted stomach release
The gastric residence system has a compacted form in a container, suitable for administration orally or through a feeding tube, and an uncompacted form when released from the container.
Stomach retention for 24 hours to one month
The gastric residence system is retained in the stomach for a residence period of between at least about 24 hours and about one month.
Limited early release less than about 20% in six hours
The system releases a therapeutically effective amount of the therapeutic agent over an effective release period and releases less than about 20% of the therapeutic agent, or pharmaceutically-acceptable salt thereof, within about a six-hour period.
Therapeutic-agent selection set
The therapeutic agent, or pharmaceutically-acceptable salt thereof, is selected from doxycycline, donepezil, ivermectin, risperidone, cetirizine, and rosuvastatin.
Across the independent claims, the coverage centers on a gastric residence system with linked elastomer coupling, VA64 and polycaprolactone carrier-agent components, silica dispersant, and an excipient containing poloxamer P407 release enhancer plus stabilizer, arranged in a compacted container form for oral or feeding-tube administration that becomes uncompacted in the stomach and provides therapeutically effective release with less than about 20% released within about six hours over a residence period of at least about 24 hours up to about one month.
Stated Advantages
Releases a therapeutically effective amount of the therapeutic agent over an effective release period.
Limits release such that less than about 20% of the therapeutic agent is released within about a six-hour period.
Provides stomach retention for a residence period of between at least about 24 hours and about one month.
Configured for administration in a compacted form orally or through a feeding tube and an uncompacted form when released from the container.
Documented Applications
Administration to a patient via an oral route or through a feeding tube using a gastric residence system retained in the stomach for at least about 24 hours up to about one month.
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