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    • 7. 发明申请
    • Reduced-mass, long-acting dosage forms
    • 减质量,长效剂型
    • US20080305115A1
    • 2008-12-11
    • US12157368
    • 2008-06-09
    • Thomas R. TicePeter MarklandJay K. Staas
    • Thomas R. TicePeter MarklandJay K. Staas
    • A61K39/395A61K31/7088
    • C07K16/00A61K9/0048A61K9/0051A61K9/1647A61K31/7088A61K2039/505
    • Methods and compositions are disclosed whereby free antibody or nucleic acid co-administered with a long-acting formulation, such as a microparticle or implant, containing the antibody or nucleic acid to achieve a long duration of antibody or nucleic acid release. One result is that less of the long-acting formulation excipient or polymer is needed allowing for small-volume administrations as required, for example, for ocular, intra-dermal, orthopedic, brain and spinal delivery. In one aspect, the free antibody or nucleic acid alone has efficacy for an extended period, during which time, very little or no long-acting formulation antibody or nucleic acid is released. In one aspect, after the free antibody or nucleic acid has diminished activity, is gone, or no longer has activity, the long-acting formulation antibody or nucleic acid begins to release for a desired preprogrammed duration to provide long-acting durations. Less formulation mass is needed because the entire antibody or nucleic acid is not encapsulated or implanted with encapsulation or implant excipient or polymer. In addition, more antibody or nucleic acid can be administered to afford longer-acting formulations.
    • 公开了方法和组合物,其中游离抗体或核酸与包含抗体或核酸的长效制剂如微粒或植入物共同施用以实现长时间的抗体或核酸释放。 一个结果是需要较少的长效制剂赋形剂或聚合物,允许根据需要进行小批量给药,例如用于眼部,皮内,矫形,脑和脊柱递送。 在一个方面,单独的游离抗体或核酸具有长时间的功效,在此期间很少或没有长效的制剂抗体或核酸被释放。 一方面,在游离抗体或核酸活性降低,消失或不再具有活性之后,长效制剂抗体或核酸开始释放所需的预编程持续时间以提供长效持续时间。 需要较少的制剂质量,因为整个抗体或核酸不被包封或植入赋形剂或聚合物包封或植入。 此外,可以施用更多的抗体或核酸以提供长效制剂。