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    • 2. 发明申请
    • Stabilized Antibody-Containing Liquid Formulations
    • 含稳定抗体的液体制剂
    • US20130022625A1
    • 2013-01-24
    • US13522848
    • 2011-01-20
    • Tomoyuki IgawaChifumi Moriyama
    • Tomoyuki IgawaChifumi Moriyama
    • C07K16/00A61K39/395C07K16/28C07K1/00
    • A61K9/0019A61K9/19A61K39/395A61K39/39591A61K47/12A61K47/18A61K47/183A61K47/26
    • An objective of the present invention is to provide stable antibody-containing formulations which are suitable for subcutaneous administration and in which aggregation formation is suppressed during long-term storage.The present inventors discovered that a significant stabilization effect was achieved by using an acidic amino acid, aspartic acid or glutamic acid as a counter ion species in histidine buffer or tris(hydroxymethyl)aminomethane, specifically by using histidine-aspartate buffer or histidine-glutamate buffer, or tris(hydroxymethyl)aminomethane-aspartate or tris(hydroxymethyl)aminomethane-glutamate as a buffer. The present inventors also discovered that a significant stabilization effect was achieved by using an acidic amino acid, aspartic acid or glutamic acid, as a counter ion species to a basic amino acid such as arginine, specifically by using arginine-aspartate or arginine-glutamate.
    • 本发明的目的是提供适用于皮下给药的稳定的含抗体制剂,并且在长期保存期间抑制聚集形成。 本发明人发现通过使用酸性氨基酸,天冬氨酸或谷氨酸作为组氨酸缓冲液或三(羟甲基)氨基甲烷中的抗衡离子物质,特别是通过使用组氨酸 - 天冬氨酸缓冲液或组氨酸 - 谷氨酸盐缓冲液 ,或三(羟甲基)氨基甲烷 - 天冬氨酸盐或三(羟甲基)氨基甲烷 - 谷氨酸盐缓冲液。 本发明人还发现,通过使用酸性氨基酸,天冬氨酸或谷氨酸,作为对离子种类与碱性氨基酸如精氨酸,特别是使用精氨酸 - 天冬氨酸或精氨酸 - 谷氨酸,实现了显着的稳定化效果。