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    • 30. 发明授权
    • Liquid ophthalmic sustained release delivery system
    • 液体眼科持续释放递送系统
    • US5422116A
    • 1995-06-06
    • US198924
    • 1994-02-18
    • Shau-Fong YenKenneth W. Reed
    • Shau-Fong YenKenneth W. Reed
    • A61K9/08A61K9/00A61K47/36A61K47/00
    • A61K9/0048A61K47/36Y10S514/912Y10S514/913Y10S514/914Y10S514/915Y10S514/95Y10S514/954Y10S514/955Y10S514/964
    • Disclosed is a sustained release liquid aqueous ophthalmic delivery system and a method of providing a slow and sustained release of ophthalmic treating agents to the eye of a mammal which comprises administering to the eye of a said mammal an effective amount of a homogeneous liquid aqueous ophthalmic pharmaceutical composition, of pH between about 3.0 and about 6.2, which is adminstrable in drop form and which comprises an ophthalmically effective concentration of a said ophthalmic treating agent and about 0.05% to about 10% by weight of the polymer chitosan; said polymer consisting essentially of(A) monomeric .beta.(1.fwdarw.4)-D-glucosamine linked units and of(B) monomeric .beta.(1.fwdarw.4)-D-glucosamine linked units which are scatteredrandomly in the molecule of the polymer, the numerical proportions of A and B being from about 60 to about 99% of A and about 1 to about 40% of B, the viscosity rating being from about 3 to about 3000 cps; in which method, upon contact with the higher pH of the ocular fluid, said liquid formulation is converted to a stiff gel from which the ophthalmic treating agent is slowly released over a prolonged period of time.
    • 本发明公开了一种持续释放液体水性眼科递送系统和向眼睛的哺乳动物提供缓慢且持续释放眼用治疗剂的方法,其包括向所述哺乳动物的眼睛施用有效量的均匀液体眼用水性药物 pH为约3.0至约6.2的组合物,其以滴剂形式施用,并且其包含眼睛上有效浓度的所述眼科治疗剂和约0.05重量%至约10重量%的聚合物壳聚糖; 所述聚合物基本上由(A)单体β(1-> 4)-D-葡糖胺连接单元和(B)单体β(1-> 4)-D-葡糖胺连接单元组成,其在 聚合物,A和B的数值比例为约60至约99%的A和约1至约40%的B,粘度等级为约3至约3000cps; 在该方法中,当与眼液的较高pH接触时,所述液体制剂被转化成刚性凝胶,眼药处理剂在较长时间内缓慢释放。