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LIQUID TO GEL, OPHTHALMIC SUSTAINED RELEASE DELIVERY SYSTEM

机译:液体,凝胶,眼科持续释放系统

摘要

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 (1-4)-D-glucosamine linked units and of (B) monomeric beta (1-4)-D-glucosamine linked units which are scattered randomly 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.
机译:公开了一种缓释液体眼用水性药物递送系统和一种向哺乳动物的眼中缓慢和持续释放眼科治疗剂的方法,该方法包括向所述哺乳动物的眼中施用有效量的均质液体眼用水性药物。 pH为约3.0至约6.2的组合物,其可以滴剂形式给药,并且包含眼科有效浓度的所述眼科治疗剂和按重量计约0.05%至约10%的聚合物壳聚糖;所述聚合物基本上由(A)单体β(1-> 4)-D-葡糖胺连接的单元和(B)单体β(1-> 4)-D-葡糖胺连接的单元组成,所述单元随机地分散在分子中。聚合物,A和B的数值比例为A的约60至约99%和B的约1至约40%,粘度等级为约3至约3000cps;在该方法中,在与较高pH的眼液接触后,所述液体制剂被转化为硬凝胶,眼科治疗剂在长时间内从中缓慢释放。

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