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    • 8. 发明授权
    • Drug delivery systems utilizing liquid crystal structures
    • 使用液晶结构的药物输送系统
    • US5891845A
    • 1999-04-06
    • US975827
    • 1997-11-21
    • Garry Myers
    • Garry Myers
    • A61K47/34A61K9/00A61K9/127A61K9/14A61K9/20A61K9/48A61K31/355A61K31/455A61K31/554A61K38/00A61K38/13A61K31/44A61K31/55
    • A61K9/146A61K31/355A61K38/13A61K9/1274A61K9/0092A61K9/2013A61K9/2072A61K9/4858
    • Vitamin E TPGS/drug compositions and methods are provided which obviate the need for surfactants or non-evaporated co-solvents because the active drug component is dissolved directly into Vitamin E TPGS to form a true molecular solution--not an emulsion or a micro-emulsion. The invention provides a slowly dissolving TPGS/Drug matrix that absorbs gastrointestinal fluid into the matrix at the dosage form/fluid interface, where a gel-like liquid crystal is formed. This gel front forms a liquid crystal boundary where drug dissolution is highest. At this liquid crystal/GI fluid boundary, a synchronization takes place in which the rate of formation of liquid crystals equals the dissolution rate of liquid crystals at the water interface, thereby giving controlled order release of the drug into the GI tract. The rate of dissolution is also controlled by the geometry of the dosage form. The solid Vitamin E TPGS/drug matrices of the invention can be solidified and compressed into tablets or filled into capsules, with other excipients, binders and/or fillers. The solid TPGS/drug solution of the invention also can be made into an immediate release liquid formulation upon addition of water, or into a controlled release system solid tablet by the use of impermeable or semi-permeable barriers or coatings surrounding portions of the tablet.
    • 提供维生素E TPGS /药物组合物和方法,其消除了对表面活性剂或非蒸发共溶剂的需要,因为活性药物组分直接溶解于维生素E TPGS中以形成真正的分子溶液 - 而不是乳液或微乳液 。 本发明提供了缓慢溶解的TPGS /药物基质,其在形成凝胶状液晶的剂型/流体界面处将胃肠液吸收到基质中。 该凝胶前体形成药物溶出度最高的液晶边界。 在该液晶/ GI液体边界处,发生液晶的形成速率等于水界面处的液晶的溶解速率的同步,从而将药物控制释放到GI道中。 溶解速率也可以通过剂型的几何形状来控制。 本发明的固体维生素E TPGS /药物基质可以固化并压制成片剂或者与其它赋形剂,粘合剂和/或填充剂一起填充到胶囊中。 本发明的固体TPGS /药物溶液还可以通过加入水制成立即释放的液体制剂,或通过使用围绕片剂部分的不渗透的或半渗透的屏障或涂层,进入控释系统的固体片剂。