包含至少一种pi在5.8与8.5之间的基础胰岛素和带有羧酸根电荷及疏水基的共聚氨基酸的ph 7为7的可注射溶液

文档序号:1026395 发布日期:2020-10-27 浏览:3次 >En<

阅读说明:本技术 包含至少一种pi在5.8与8.5之间的基础胰岛素和带有羧酸根电荷及疏水基的共聚氨基酸的ph 7为7的可注射溶液 (Injectable solution at pH 7 comprising at least one basal insulin with a PI between 5.8 and 8.5 and a polyamino acid with carboxylate charge and hydrophobic group ) 是由 陈友平 罗曼·诺埃尔 亚历山大·盖斯勒 沃尔特·罗格 里夏尔·沙尔韦 尼古拉斯·劳伦特 于 2018-12-07 设计创作,主要内容包括:在一个实施方案中,根据本发明的组合物的特征在于,带有羧酸根电荷及至少一个疏水基-Hy的共聚氨基酸选自根据下文式XXXb的共聚氨基酸:&lt;Image he="317" wi="700" file="DDA0002561495820000011.GIF" imgContent="drawing" imgFormat="GIF" orientation="portrait" inline="no"&gt;&lt;/Image&gt;其中,●D独立地表示基团-CH&lt;Sub&gt;2&lt;/Sub&gt;-(天冬氨酸)或基团-CH&lt;Sub&gt;2&lt;/Sub&gt;-CH&lt;Sub&gt;2&lt;/Sub&gt;-(谷氨酸),●X表示在包括碱阳离子的组中选择的阳离子实体,●R&lt;Sub&gt;b&lt;/Sub&gt;和R&lt;Sub&gt;b&lt;/Sub&gt;’相同或不同,为疏水基-Hy或在由H、C2至C10直链酰基、C3至C10支链酰基、苄基、末端“氨基酸”单元和焦谷氨酸根组成的组中选择的基团,Rb和R’b中的至少一者是疏水基-Hy,●Q和Hy如上所定义。●n+m表示共聚氨基酸的聚合度DP,即每个共聚氨基酸链的单体单元的平均数,且5≤n+m≤250。(In one embodiment, the composition according to the invention is characterized in that the copolymerized amino acids bearing a carboxylate charge and at least one hydrophobe-Hy are selected from the group consisting of the copolymerized amino acids according to formula XXXb below: wherein ● D independently represents a group-CH 2 - (aspartic acid) or radicals-CH 2 ‑CH 2 - (glutamic acid), ● X represents a cationic entity chosen in the group comprising the alkali cations, ● R b And R b &#39;same or different, is a hydrophobic group-Hy or a group selected in the group consisting of H, C2 to C10 straight acyl, C3 to C10 branched acyl, benzyl, a terminal &#34;amino acid&#34; unit, and pyroglutamate, at least one of Rb and R&#39; b being a hydrophobic group-Hy, ● Q and Hy being as defined above. ● n &#43; m represents the degree of polymerization DP of the copolymerized amino acid, i.e., the average number of monomer units per copolymerized amino acid chain, and 5. ltoreq. n &#43; m. ltoreq.250.)

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