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    • 4. 发明授权
    • Controlled release oral drug delivery system
    • 控制释放口服药物输送系统
    • US06692766B1
    • 2004-02-17
    • US08750674
    • 1997-02-28
    • Abraham RubinsteinRaphael RadaiMichael FriedmanBoaz TiroshMuhammad BaluomTaher Nassar
    • Abraham RubinsteinRaphael RadaiMichael FriedmanBoaz TiroshMuhammad BaluomTaher Nassar
    • A61K910
    • A61K9/2027A61K9/2013Y10S514/944Y10S514/946
    • The present invention relates to a controlled release drug delivery system comprising a drug which is susceptible to enzymatic degradation by enzymes present in the intestinal tract; and a polymeric matrix which undergoes erosion in the gastrointestinal tract comprising a hydrogel-forming polymer selected from the group consisting of (a) polymers which are themselves capable of enhancing absorption of said drug across the intestinal mucosal tissues and of inbihiting degradation of said drug by intestinal enzymes; and (b) polymers which are not themselves capable of enhancing absorption of said drug across the intestinal mucosal tissues and of inhibiting degradation of said drug by intestinal enzymes; wherein when the matrix comprises a polymer belonging to group (b) the delivery system further comprises an agent which enhances absorption of said drug across the intestinal mucosal tissues and/or an agent which inhibits degradation of said drug by intestinal enzymes and when the matrix comprises a polymer belonging to group (a) the delivery system optionally further comprises an agent which enhances absorption of said drug across the intestinal mucosal tissues and/or an agent which inhibits degradation of said drug by intestinal enzymes.
    • 本发明涉及一种控释药物递送系统,其包含易于通过存在于肠道中的酶进行酶降解的药物; 以及在胃肠道中遭受侵蚀的聚合物基质,其包含选自以下的水凝胶形成性聚合物:(a)本身能够增强所述药物穿过肠粘膜组织的吸收的聚合物和所述药物的不利因素降解 肠酶; 和(b)本身不能增强所述药物穿过肠粘膜组织的吸收并且通过肠酶抑制所述药物降解的聚合物; 其中当所述基质包含属于组(b)的聚合物时,所述递送系统还包含增强所述药物穿过肠粘膜组织的吸收的试剂和/或通过肠酶抑制所述药物降解的药剂,并且当所述基质包含 属于(a)组的聚合物任选地还包含增强所述药物穿过肠粘膜组织的吸收的试剂和/或通过肠酶抑制所述药物降解的试剂。
    • 8. 发明申请
    • Method for Selecting Cationic or Anionic Liposomes for Treatment of a Mucosa Membrane, and Kit Comprising the Same
    • 用于选择阳离子或阴离子脂质体用于治疗粘膜膜的方法,以及包含它的试剂盒
    • US20070212403A1
    • 2007-09-13
    • US10578090
    • 2004-11-03
    • Yechezkel BarenholzAbraham RubinsteinTareq Jubeh
    • Yechezkel BarenholzAbraham RubinsteinTareq Jubeh
    • A61K9/127
    • A61K9/1272A61K9/127
    • The present invention is based on the use of electrical surface charge as a docking tool to bring charged lipid assemblies in the vicinity of a diseased, e.g. inflamed epithelium of the mucosa, or alternatively, to a normal epithelium, for executing a desired medical procedure. Thus, the present invention provides a method for selecting a medicament for a medical procedure has now been designed. The medical procedure is selected from treatment, for the healing of a disease or disorder of a mucosa, prophylaxis of a disease or disorder or a mucosa, or a combination of same. The method steps are based on the observation that there are differences in the attachment properties of charged lipid assemblies, such as liposomes, when examined in healthy or inflamed mucosal tissues. The invention also provides a kit making use of the method of the invention. Yet, the invention concerns a method and a medicament for the treatment or prevention of a disease or disorder of the gastrointestinal mucosa, as well as the use of charged lipid assemblies for obtaining said medicament, based on the principles of the differential adhesion of positively vs. negatively charged lipid assemblies to healthy and diseased mucosa, respectively.
    • 本发明基于使用电表面电荷作为对接工具,以使带电的脂质组件在患病的附近,例如, 粘膜的发炎的上皮,或者替代地,用于正常的上皮,用于执行所需的医疗程序。 因此,本发明提供了一种用于选择用于医疗程序的药物的方法。 医疗程序选自治疗,治疗粘膜疾病或病症,预防疾病或病症或粘膜,或其组合。 方法步骤基于观察,当在健康或发炎的粘膜组织中检查时,带电脂质组件(例如脂质体)的附着性质存在差异。 本发明还提供了使用本发明方法的试剂盒。 然而,本发明涉及用于治疗或预防胃肠粘膜疾病或病症的方法和药物,以及用于获得所述药物的带电脂质组合物的用途,基于差异粘附的原则 带负电荷的脂质组件分别为健康和患病的粘膜。