公开(公告)号：US06818669B2

公开(公告)日：2004-11-16

申请号：US09955485

申请日：2001-09-19

申请人： Michael A. Moskowitz ,  James K. Liao ,  Eyal S. Ron ,  Mary Nallin Omstead

发明人： Michael A. Moskowitz ,  James K. Liao ,  Eyal S. Ron ,  Mary Nallin Omstead

IPC分类号： A61K31351

CPC分类号： A61K31/7048 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2846 ,  A61K31/198 ,  A61K31/505 ,  A61K31/519 ,  A61K31/525 ,  A61K31/7076 ,  A61K31/195 ,  A61K2300/00

摘要： A method and compositions are provided for increased cerebral bioavailability of blood-born compositions by administering the composition of interest while increasing brain NO levels. This increase in NO levels may be accomplished by stimulating increased production of NO by eNOS, especially by administering L-arginine, by administering agents that increase NO levels independent of ecNOS, or by any combination of these methods. As NO is increased, cerebral blood flow is consequently increased, and drugs in the blood stream are carried along with the increased flow into brain tissue. By increased flow, the site of action will be exposed to more drug molecules. By stimulating increased NO production, administration of drugs that are not easily introduced to the brain may be facilitated and/or the serum concentration necessary to achieve desired physiologic effects may be reduced.

摘要翻译： 提供了通过在增加脑NO水平的同时施用感兴趣的组合物来提高血液出生组合物的脑生物利用度的方法和组合物。 NO水平的这种增加可以通过刺激通过eNOS增加NO的产生，特别是通过施用L-精氨酸，通过施用增加NO水平而不依赖于ecNOS的药剂或通过这些方法的任何组合来实现。 随着NO增加，脑血流量增加，血液中的药物随着流入脑组织的增加而被携带。 通过增加流动，作用部位将暴露于更多的药物分子。 通过刺激增加的NO产生，可以促进不容易引入脑的药物的给药和/或可以降低达到所需生理学效果所需的血清浓度。