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    • 6. 发明申请
    • COLONIC DELIVERY OF ACTIVE AGENTS
    • 有效代理的殖民地交付
    • WO2006085075A2
    • 2006-08-17
    • PCT/GB2006/000448
    • 2006-02-09
    • DA VOLTERRACENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUESTEVENS, Ian, EdwardFATTAL, EliasANDREMONT, AntoineCOUVREUR, PatrickBOURGEOIS, Sandrine
    • FATTAL, EliasANDREMONT, AntoineCOUVREUR, PatrickBOURGEOIS, Sandrine
    • A61K9/1652A61K9/1682A61K31/155A61K38/465A61K38/47C12Y305/02006G01N2800/065
    • Drug delivery devices that are orally administered, and that release active ingredients in the colon, are disclosed. In one embodiment, the active ingredients are those that inactivate antibiotics, such as macrolides, quinolones and beta-lactam containing antibiotics. One example of a suitable active agent is an enzyme such as beta-lactamases. In another embodiment, the active agents are those that specifically treat colonic disorders, such as Chrohn's Disease, irritable bowel syndrome, ulcerative colitis, colorectal cancer or constipation. The drug delivery devices are in the form of beads of pectin, crosslinked with calcium and reticulated with polyethyleneimine. The high crosslink density of the polyethyleneimine is believed to stabilize the pectin beads for a sufficient amount of time such that a substantial amount of the active ingredients can be administered directly to the colon. Advantageously, the amount of polyethyleneimine is sufficient to allow a substantial portion of the pectin beads to pass through the gastrointestinal tract to the colon without releasing the active agent, and is also sufficient such that the pectin beads are sufficiently degraded in the colon to release an effective amount of the active agent.
    • 公开了口服给药并且释放结肠中活性成分的药物输送装置。 在一个实施方案中,活性成分是使抗生素失活的成分,例如大环内酯类,喹诺酮类和含β-内酰胺类的抗生素。 合适的活性剂的一个实例是酶如β-内酰胺酶。 在另一个实施方案中,活性剂是特异性治疗结肠疾病如克罗恩病,肠易激综合征,溃疡性结肠炎,结肠直肠癌或便秘的那些。 药物递送装置是果胶珠的形式,与钙交联并用聚乙烯亚胺网化。 据信聚乙烯亚胺的高交联密度使果胶珠稳定足够的时间,使得大量的活性成分可以直接施用于结肠。 有利地,聚乙烯亚胺的量足以使大部分果胶珠通过胃肠道进入结肠而不释放活性剂,并且也足够使得果胶珠在结肠中充分降解以释放 有效量的活性剂。