DAVID MONTEITH,JOHN O'MULLANE,JOSEPH P. REO,ROBERT T. NOWAK,JIANSHENG WAN,MOHAMMED A. KABIR,MALAZ A. ABUTARIF,GLENN E. FRITZ
申请号:
BRPI0712532
公开号:
BRPI0712532A2
申请日:
2007.06.01
申请国别(地区):
BR
年份:
2013
代理人:
摘要:
PHENILEFRINE FORMULATIONS AND PHARMACEUTICAL COMPOSITIONS FOR COLONICAL ABSORPTION. The present invention relates to a pharmaceutical composition comprising phenylephrine or a pharmaceutically acceptable salt thereof and a wearable layer which is for oral administration, wherein the composition releases phenylephrine or a pharmaceutically acceptable salt thereof by absorption into the colon. The pharmaceutical composition comprises a core comprising phenylephrine or a pharmaceutically acceptable salt thereof and a wearable layer which is in a time-dependent, pH-dependent, or colon-specific enzyme-wearable layer that degrades to expose the core to release phenylephrine in the colon. In a preferred embodiment, the wearable layer packs the core. The composition optionally also comprises phenylephrine in the wearable layer or other additional layer (s). The pharmaceutical composition may also comprise one or more additional therapeutically active agents selected from one or more of the group consisting of antihistamines, analgesics, antipyretics, and non-steroidal antiinflammatory agents. The invention also describes methods of administering phenylephrine through the colon, thereby increasing the bioavailable amount of therapeutically active unconjugated phenylephrine with respect to total plasma phenylephrine.FORMULAÇÕES E COMPOSIÇÕES FARMACÊUTICAS DE FENILEFRINA PARA ABSORÇçO COLâNICA. A presente invenção refere-se a composição farmacêutica compreendendo fenilefrina ou um sal farmaceuticamente aceitável desta e uma camada desgastável que é para administração oral, em que a composição libera fenilefrina ou um sal farmaceuticamente aceitável desta por meio da absorção no cólon. A composição farmacêutica compreende um núcleo compreendendo fenilefrina ou um sal farmaceuticamente aceitável desta e uma camada desgastável que está em uma camada desgastável dependente do tempo, dependente do pH, ou dependente da enzima específica do cólon que degrada-se para expor o núcleo pa