VAGHASHIYA, JAYDEEP,SHAH, NAVNIT H.,PHUAPRADIT, WANTANEE,DESAI, DIPEN,MEGHPARA, KANJI
申请号：
CA3065695
公开号：
CA3065695A1
申请日:
2019.06.27
申请国别(地区):
CA
年份:
2019
代理人:
摘要：
Self-regulating, osmotic, floating gastroretentive compositions that provideextendedrelease, delayed release, and/or delayed extended release of activepharmaceutical agents, aswell as, optionally, immediate release of the same or a different activepharmaceutical agent,are provided here. The gastroretentive compositions of the disclosure comprisea swellable,extended release, multilayer core comprising a push layer and a pull layer； awater-insolublepermeable elastic membrane surrounding the multilayer core； and an orifice(e.g., alaser-drilled orifice, a manually drilled orifice) on the pull-layer side ofthe dosage form. Thegastric retention of the composition is controlled by rapid floating of thecomposition andexpansion of the membrane. The rapid swelling of the composition to a sizegreater than thesize of the pyloric sphincter is due to the presence of an osmogen, adequatemembranepermeability that provides for fast generation of CO2 from a gas-generatingagent(s), andadequate membrane elasticity that provides for rapid expansion of themembrane. Thehydrated core, especially the polyethylene oxide in the push layer, and thepermeable elasticmembrane with an orifice (1) provide extended release of the activepharmaceutical agent,and (2) maintain the dosage form at a size suitable for gastric retention. Theself-regulatingcomposition collapses, or breaks into pieces, after releasing at least about80% of the drugfrom the composition.
