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SYSTEM FOR SUSTAINED RELEASE OF HYDROPHOBIC PROTEINS BASED ON A HYALURONIC ACID AMIDE

机译:基于透明质酸酰胺的疏水蛋白持续释放系统

摘要

The present invention relates to a system for sustained release of biologically active proteins, comprising a) a protein with a hydrophobic nature and b) a hyaluronic acid (HA) amide, wherein the HA used for the preparation of the amide has a weight-average molecular weight ranging between 500 and 730 kDa, wherein said protein with a hydrophobic nature has a GRAVY index not less than -0.5 and the HA amide is selected from HA hexadecylamide: HA amide with hexadecylamine, having a molar amidation percentage ranging between 7 and 14%; HA octylamide: HA amide with octylamine, having a molar amidation percentage ranging between 10 and 15%; HA dodecylamide: HA amide with dodecylamine, having a molar amidation percentage ranging between 10 and 15%; HA tert-butylamide: HA amide with tert-butylamine, having a molar amidation percentage ranging between 7 and 12%; HA benzylamide: HA amide with benzylamine, having a molar amidation percentage ranging between 7 and 15%; and wherein the ratio hyaluronic acid (HA) amide/protein is not less than 10:1. The invention provides sustained, slow release over time which increases the efficacy of the medicament and the patient's compliance.
机译:本发明涉及用于生物活性蛋白质的持续释放的系统,该系统包括:a)具有疏水性的蛋白质和b)透明质酸(HA)酰胺,其中用于制备酰胺的HA具有重均分子量在500至730 kDa之间,其中所述具有疏水性质的蛋白质的GRAVY指数不小于-0.5,且HA酰胺选自HA十六烷基酰胺:HA酰胺与十六烷基胺,摩尔酰胺化百分率在7至14之间%; HA辛酰胺:HA酰胺与辛胺的酰胺化百分比范围为10-15%。 HA十二烷基酰胺:具有十二烷基胺的HA酰胺,其酰胺化百分比范围为10至15%; HA叔丁酰胺:具有叔丁胺的HA酰胺,其酰胺化百分比范围为7至12%; HA苄基酰胺:HA酰胺与苄基胺,酰胺化百分率在7-15%之间;透明质酸(HA)酰胺/蛋白质的比例为10∶1以上。本发明提供了随着时间的持续缓慢释放,这增加了药物的效力和患者的依从性。

著录项

  • 公开/公告号EA031390B1

    专利类型

  • 公开/公告日2018-12-28

    原文格式PDF

  • 申请/专利权人 FIDIA FARMACEUTICI S.P.A.;

    申请/专利号EA20140091991

  • 发明设计人 MONICA;CRISTIAN;DAVIDE;

    申请日2013-05-30

  • 分类号A61K38;A61K47/36;A61K9;

  • 国家 EA

  • 入库时间 2022-08-21 12:02:35

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