会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 8. 发明申请
    • WATER-DISPERSIBLE ORAL, PARENTERAL, AND TOPICAL FORMULATIONS FOR POORLY WATER SOLUBLE DRUGS USING SMART POLYMERIC NANOPARTICLES
    • 使用智能聚合物纳米颗粒的水溶性难溶性药物的水分散性口服,肠胃外和局部用制剂
    • WO2008073558A2
    • 2008-06-19
    • PCT/US2007080536
    • 2007-10-05
    • UNIV JOHNS HOPKINSMAITRA ANIRBANFELDMANN GEORGBISHT SAVITA
    • MAITRA ANIRBANFELDMANN GEORGBISHT SAVITA
    • A61K47/48A61K9/19A61K47/32
    • A61K9/146A61K9/19A61K9/5138A61K47/6933A61K47/6935B01J13/14B01J13/18B82Y5/00
    • Polymeric nanoparticles with a hydrophobic core and a hydrophilic shell are formed from: 1) N-isopropyl acrylamide (NIPAAM), at a molar ratio of about 50% to about 90%, and preferably 60% for specific delivery routes such as oral or parenteral; either water-soluble vinyl derivatives like vinylpyrolidone (VP) or vinyl acetate (VA), or water insoluble vinyl derivatives like methyl methacrylate (MMA) or styrene (ST), at a molar ratio of about 10% to about 30%;, and acrylic acid (AA), at a molar ratio of about 10% to about 30%. The formed nanoparticles may be optionally surface functional using reactive groups present in AA, including PEGylation, or conjugation of moieties such as chemotherapeutics, contrasting agents, antibodies, radionucleides, ligands, and sugars, for diagnostic, therapeutic, and imaging purposes. The polymeric nanoparticles are preferably dispersed in aqueous solutions. The polymeric nanoparticles incorporate one or more types of medicines or bioactive agents in the hydrophobic core; on occasion, the medicine or bioactive agent may be conjugated to the nanoparticle surface via reactive functional groups. The polymeric nanoparticles are capable of delivering the said medicines or bioactive agents through oral, parenteral, or topical routes. The polymeric nanoparticles allow poorly water soluble medicines or bioactive agents, or those with poor oral bioavailability, to be formulated in an aqueous solution, and enable their convenient delivery into the systemic circulation.
    • 具有疏水性芯和亲水性壳的聚合物纳米颗粒由1)N-异丙基丙烯酰胺(NIPAAM)以约50%至约90%,优选60%的摩尔比用于特定递送途径如口服或肠胃外 ; 或水溶性乙烯基衍生物如乙烯基吡咯烷酮(VP)或乙酸乙烯酯(VA)或水不溶性乙烯基衍生物如甲基丙烯酸甲酯(MMA)或苯乙烯(ST),摩尔比为约10%至约30%;和 丙烯酸(AA)以约10%至约30%的摩尔比混合。 为了诊断,治疗和成像目的,所形成的纳米颗粒可以使用存在于AA中的反应基团(包括聚乙二醇化)或部分(例如化学治疗剂,造影剂,抗体,放射性核素,配体和糖)的缀合来任选表面功能。 聚合物纳米粒子优选分散在水溶液中。 聚合物纳米粒子在疏水性核心中掺入一种或多种类型的药物或生物活性剂; 有时,药物或生物活性剂可以通过反应性官能团与纳米颗粒表面缀合。 聚合物纳米颗粒能够通过口服,肠胃外或局部途径递送所述药物或生物活性剂。 聚合物纳米颗粒允许水溶性差的药物或生物活性剂或口服生物利用度差的那些配制在水溶液中,并使其能够方便地输送到体循环中。