MOON, SUN JIN,文瑄眞,文瑄眞,SHIN, CHEONG BYEOL,申晴星,申晴星,HONG, SUNG HEE,洪性熙,洪性熙,KIM, DAE JIN,金大振,金大振,KWON, SE CHANG,权世昌,權世昌
申请号：
TW105123400
公开号：
TW201718022A
申请日:
2016.07.22
申请国别(地区):
TW
年份:
2017
代理人:
摘要：
Provided is a method of preparing a physiologically active polypeptide conjugate, in which a physiologically active polypeptide and a non-peptidyl polymer are linked to each other via a covalent bond. The method is to improve an overall yield of the physiologically active polypeptide conjugate by improving a reaction of the non-peptidyl polymer and the physiologically active polypeptide, and particularly, the method is to prepare a physiologically active polypeptide conjugate in a high yield by performing a two-step reaction through selective precipitation.The preparation method of the present invention is used to produce a non-peptidyl polymer-physiologically active polypeptide conjugate and a physiologically active polypeptide-physiologically active carrier conjugate in a high yield, and therefore, the method may be used in the development of long-acting formulations of various peptide drugs which maintain in vivo activity at a relatively high level and have remarkably increased blood half-life.本發明係提供一種製備生理活性多肽接合物的方法,其中,生理活性多肽及非肽基聚合物係經由共價鍵彼此連接。該方法係藉由增進該非肽基聚合物及該生理活性多肽之反應而增進該生理活性多肽接合物之總產率,具體而言,該方法係藉由透過選擇性沉澱施行二步驟反應而以高產率製備生理活性多肽接合物。本發明之製備方法係用於以高產率製造非肽基聚合物-生理活性多肽接合物以及生理活性多肽-生理活性載體接合物,因此,該方法可用於開發以相對高水平維持活體內活性且具有明顯增加的血中半衰期之各種胜肽藥物之長效調配物。由於本案的圖僅為實驗數據,並非本案的代表圖。故本案無指定代表圖。
