SHAH, Navnit, H.,PHUAPRADIT, Wantanee,DESAI, Dipen,VAGHASHIYA, Jaydeep,MEGHPARA, Kanji
申请号：
USUS2019/039573
公开号：
WO2020/006278A1
申请日:
2019.06.27
申请国别(地区):
US
年份:
2020
代理人:
摘要：
Self-regulating, osmotic, floating gastroretentive compositions that provide extended release, delayed release, and/or delayed extended release of active pharmaceutical agents, as well as, optionally, immediate release of the same or a different active pharmaceutical agent, are provided here. The gastroretentive compositions of the disclosure comprise a swellable, extended release, multilayer core comprising a push layer and a pull layer； a water-insoluble permeable elastic membrane surrounding the multilayer core； and an orifice (e.g., a laser- drilled orifice, a manually drilled orifice) on the pull-layer side of the dosage form. The gastric retention of the composition is controlled by rapid floating of the composition and expansion of the membrane. The rapid swelling of the composition to a size greater than the size of the pyloric sphincter is due to the presence of an osmogen, adequate membrane permeability that provides for fast generation of C02 from a gas-generating agent(s), and adequate membrane elasticity that provides for rapid expansion of the membrane. The hydrated core, especially the polyethylene oxide in the push layer, and the permeable elastic membrane with an orifice (1) provide extended release of the active pharmaceutical agent, and (2) maintain the dosage form at a size suitable for gastric retention. The self-regulating composition collapses, or breaks into pieces, after releasing at least about 80% of the drug from the composition.L'invention concerne des compositions osmotiques autorégulées à rétention gastrique par flottaison qui permettent une libération prolongée, une libération retardée et/ou une libération prolongée retardée d'agents pharmaceutiques actifs, ainsi que, de façon optionnelle, une libération immédiate de ces derniers ou d'un autre agent pharmaceutique actif. Les compositions à rétention gastrique de l'invention comprennent un noyau multicouche gonflable à libération prolongée, comprenant une couche de poussée et une couch
