高分子药物的研究Ⅰ．炔诺酮－α，β－聚（羟烷基）－DL－天冬酰胺高分子药物体外释放的研究

STUDIES ON THE POLYMERIC DRUGSⅠ.IN-VITRO RELEASE OF NORETHINDRONE-α,β-POLY(HYDROXYAIKYL)-DL-ASPARAMIDE CONJUGATES

本文对炔诺酮－α，β－聚（羟烷基）－ＤＬ－天冬酰胺进行了体外释放的研究，其中包括炔诺酮－α，β－聚（３－羟丙基）－ＤＬ天冬酰胺（ＮＥＴ－ＰＨＰＡ）和炔诺酮－α，β－聚（４－羟丁基）－ＤＬ－天冬酰胺（ＮＥＴ－ＰＨＢＡ）。实验结果表明，在药物接入量接近的情况下，悬臂的长短对药物释放有一定的影响，从释放１２０ｄ的情况来看，接入量为２４．０％的ＮＥＴ－ＰＨＰＡ的释放速率为０．２４μｇ－ＮＥＴ／ｍｇＰｏｌｙ·ｄａｙ：接入量为２０．１％的ＮＥＴ－ＰＨＢＡ的释放速率为０．３７μｇ－ＮＥＴ／ｍｇ－Ｐｏｌｙ·ｄａｙ．

The in-vitro release of norethindrone-α,β-poly (hydroxyalkyl)DL-asparamide conjugates were studied in this paper.The polymeric drugs involved norethindrone-α.-poly(3-hydroxypropyl)-DL-asparamide( NET-PHPA )and norethindrone α.β-poly (4-hydroxybutyl)DL-asparamide(NET-PHBA ).The results th showed that the length of the spacer affectedthe in-vitro release.UP till now,the in-vitro release had been carried out in 120 days.The release rate of 24. 0% for NET-HPA was 0. 24 μg-NET/mg-poly·day and 20. 1 % for NETPHBA was 0.37 μg-NET/mg-poly ·day.