发明名称 |
NEW PROCESSES FOR THE PRODUCTION OF CHEMICALLY-MODIFIED HEPARINS |
摘要 |
The present invention relates to a process for the production of heparin derivatives having an average molecular weight of from about 4.6 to about 6.9 kDa and an anti-factor Xa activity of less than about 10 IU/mg, comprising the steps of oxidation of unfractionated heparin, depolymerisation and reduction of resulting terminal groups. |
申请公布号 |
US2016137754(A1) |
申请公布日期 |
2016.05.19 |
申请号 |
US201414898862 |
申请日期 |
2014.06.19 |
申请人 |
DILAFOR AB |
发明人 |
ERIKSSON Per-Olov;HOLMER Erik Yngve |
分类号 |
C08B37/00;A61K31/727 |
主分类号 |
C08B37/00 |
代理机构 |
|
代理人 |
|
主权项 |
1. A process for the preparation of a heparin derivative having an average molecular weight of from about 4.6 to about 6.9 kDa and an anti-factor Xa activity of less than about 10 IU/mg, comprising the consecutive steps of:
oxidising an acidic aqueous solution of unfractionated heparin by addition of an oxidising agent; (ii) depolymerising the oxidised heparin by subjecting the product of step (i) to alkali to form an alkaline solution; (iii) maintaining said solution from step (ii) at an alkaline pH for a period of time required to provide depolymerised heparin with a molecular weight within the aforesaid range; and (iv) reducing terminal aldehyde groups of said depolymerised heparin by addition of a hydride reducing agent to the solution obtained from step (iii), wherein the period of time between the completion of step (i) and the start of step (iv) is controlled in order to minimise the effect of residual oxidising agents; and wherein said period of time in step (iii) is determined by analysis of said solution, or by reference to a previously-performed substantially identical step (iii). |
地址 |
Solna SE |