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    • 8. 发明申请
    • STABILIZED REVERSE MICELLE COMPOSITIONS AND USES THEREOF
    • 稳定的反胶束组合物及其用途
    • WO03047493A3
    • 2003-10-16
    • PCT/US0238473
    • 2002-12-03
    • DOR BIOPHARMA INCCONSTANTINIDES PANOS PLIANG LIKANJANG EUN-HYUN
    • CONSTANTINIDES PANOS PLIANG LIKANJANG EUN-HYUN
    • A61K8/14A61K9/107A61K9/48A61K31/727A61K47/10A61K47/14A61K47/32A61K47/34A61K47/48A61Q19/00A61K9/127A61F13/00A61K9/20
    • A61K31/727A61K8/0291A61K9/107A61K9/1075A61K9/4891A61K38/09A61K38/23A61K38/27A61K38/28A61K38/29A61Q19/00
    • The invention relates to compositions and methods for drug delivery suitable for promoting the transmucosal absorption of drugs, especially drugs with poor intrinsic bioavailability, such as peptides, proteins, vaccines, and nucleic acids. The delivery system of this invention preferably comprises fatty acid esters and their hydrophilic derivatives that associate with water and other polar solvents to form reverse micelles tha are physiclally stabilized in the presence of gastrointestinal fluid, water, and other hydrophilic solvents. Such stable reverse micelles are formed by suitable mixtures of polymeric or non-polymeric compounds with amphiphiles. Micelles made using these methods undergo phase transformation more slowly resulting in delayed drug release profiles and sustained absorption. When administered as a pharmaceutical to mucosal surfaces following oral ingestion or intranasal administration, therapeutic molecules principally solubilized in the aqueous phase are protected from digestion by mucosal enzymes and other mucosal degradative processes and are taken up by absorptive cell mechanisms and reach appropriate body compartments. The reverse micelle compositions may comprise mono-, di-glycerides and/or their transesterifed products containing C6-C12 fatty acids chains, wherein the transester groups consist of hydrohilic moieties.
    • 本发明涉及用于药物递送的组合物和方法,所述组合物和方法适于促进药物,特别是具有差的内在生物利用度的药物如肽,蛋白质,疫苗和核酸的透粘膜吸收。 本发明的递送系统优选包含脂肪酸酯及其亲水性衍生物,其与水和其它极性溶剂缔合以形成在胃肠液,水和其它亲水性溶剂存在下物理稳定的反胶束。 这种稳定的反胶束由聚合物或非聚合物与两亲物的适宜混合物形成。 使用这些方法制备的胶束经历相变更慢,导致药物释放曲线延迟和持续吸收。 当作为药物在口服或鼻内给药后粘膜表面施用时,主要溶解在水相中的治疗分子被粘膜酶和其他粘膜降解过程保护免于消化,并被吸收细胞机制吸收并到达适当的身体隔室。 反胶束组合物可包含含有C 6 -C 12脂肪酸链的甘油单酯,甘油二酯和/或其酯交换产物,其中酯基由亲水部分组成。
    • 9. 发明申请
    • REVERSE MICELLE COMPOSITIONS AND USES THEREOF
    • 反相MICELLE组合物及其用途
    • WO03047494A2
    • 2003-06-12
    • PCT/US0238474
    • 2002-12-03
    • DOR BIOPHARMA INCCONSTANTINIDES PANOS PLIANG LIKANJANG EUN-HYUN
    • CONSTANTINIDES PANOS PLIANG LIKANJANG EUN-HYUN
    • A61K8/14A61K9/107A61K47/48A61K49/00A61Q19/00A61J
    • A61K8/0291A61K9/1075A61K49/0004A61Q19/00
    • The invention relates to reverse micelle compositions and method s for drug delivery suitable for promoting the transmucosal absorption of biologically active molecules, especially drugs with poor intrinsic bioavailability, such as peptides, proteins, vaccines, and nucleic acids. The delivery system of this invention preferably comprises fatty acid esters and their hydrophilic derivatives that associate with water and othe polar solvents to form stable reverse micelles. When administered as pharmaceutical to mucosal surfaces following oral or intrasanal administration, biologically active molecules principally solubilized in the hydrophilic phase are protected from digestion by mucosal enzymes and other mucosal degradative processes and are taken up by absorptive cell mechanisms and reach appropriate body compartments. The reverse micelle compositions described in this invention may comprise monoglycerides and/or their transesterified products containing C6-C12 fatty acids chains, wherein the transester groups consist of hydrophilic moieties.
    • 本发明涉及用于药物递送的反胶束组合物和方法,其适用于促进生物活性分子的经粘膜吸收,特别是具有差的内在生物利用度的药物,例如肽,蛋白质,疫苗和核酸。 本发明的递送系统优选包含与水和极性溶剂缔合的脂肪酸酯及其亲水性衍生物以形成稳定的反胶束。 当口服或体内给药后作为药物施用于粘膜表面时,主要溶解在亲水相中的生物活性分子被保护不被粘膜酶和其它粘膜降解过程消化,并被吸收细胞机制吸收并达到适当的身体隔室。 本发明中描述的反胶束组合物可以包含含有C 6 -C 12脂肪酸链的单酸甘油酯和/或其酯交换产物,其中酯基组由亲水部分组成。