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    • 1. 发明申请
    • GASTRORETENTIVE CONTROLLED RELEASE PHARMACEUTICAL DOSAGE FORMS
    • 气体控制释放药物剂型
    • WO0137812A2
    • 2001-05-31
    • PCT/IL0000774
    • 2000-11-20
    • YISSUM RES DEV COFRIEDMAN MICHAELKLAUSNER EYTANLAVY ERANHOFFMAN AMNON
    • FRIEDMAN MICHAELKLAUSNER EYTANLAVY ERANHOFFMAN AMNON
    • A61K47/30A61K9/08A61K9/107A61K9/14A61K9/20A61K9/22A61K9/26A61K9/40A61K9/52A61K31/525A61K47/10A61K47/14A61K47/24A61K47/32A61K47/36A61K47/38A61K47/42A61P1/04
    • A61K9/2086
    • Pharmaceutical gastroretentive drug delivery system for the controlled release of an active agent in the gastrointestinal tract, which comprises: (a) a single- or multi-layered matrix having a two- or three-dimensional geometric configuration comprising a polymer that does not retain in the stomach more than a conventional dosage form selected from (1) degradable polymers that may be hydrophilic polymers not instantly soluble in gastric fluids, enteric polymers substantially insoluble at pH less than 5.5 and/or hydrophobic polymers and mixtures thereof; (2) non-degradable polymers; and any mixtures of (1) and (2); (b) a continuous or non-continuous membrane, that does not retain in the stomach more than a conventional dosage form, affixed or attached to said matrix, the membrane comprising at least one polymer having a substantial mechanical strength; and (c) a drug; wherein the matrix when affixed or attached to said membrane prevents evacuation from the stomach of said delivery system for a period of time of from about 3 to about 24 hours. The system may further comprise a shielding layer. The delivery system is particularly suitable for the delivery of drugs having a narrow absorption window in the gastrointestinal tract, drugs intended for local treatment of the gastrointestinal tract and drugs degraded in the colon, and is intended for human and veterinary use.
    • 用于在胃肠道中控制释放活性剂的药物胃滞留药物递送系统,其包括:(a)具有二维或三维几何构型的单层或多层基质,其包含不保留在 胃超过常规剂型,选自(1)可降解的聚合物,其可以是不能立即溶于胃液的亲水性聚合物,在pH小于5.5时基本上不溶解的肠溶聚合物和/或疏水聚合物及其混合物; (2)不可降解聚合物; 和(1)和(2)的任何混合物; (b)连续或不连续的膜,其不比常规剂型保留在固定或附着到所述基质上,所述膜包含至少一种具有显着机械强度的聚合物; 和(c)药物; 其中当固定或连接到所述膜时所述基质防止从所述递送系统的胃排出约3至约24小时的时间。 该系统还可以包括屏蔽层。 递送系统特别适合于在胃肠道中递送具有窄吸收窗口的药物,用于局部治疗胃肠道的药物和在结肠中降解的药物,并且用于人和兽医用途。