由于相当多药物的透皮吸收不理想,达不到治疗的要求,所以很多研究者致力于发现透皮吸收促进剂。80年代初报道了Azone的透皮吸收促进作用优于二甲亚砜(DMSO),虽然它的作用机理还不清楚。为了更进一步比较透皮吸收促进剂的构效关系,本文作者研究了带有一个烷基或烯基(萜烯)侧链(10,15或20个碳原子)的9种氮杂环烷酮(5,6或7元环)衍生物的透皮吸收促进作用。体外皮肤穿透实验是用雄性豚鼠(250g)的皮肤,在37℃恒温水浴中进行。实验中用的药物是6-巯基嘌呤([~(14)C]6-MP,65mCi/mmol),用LSC-903型闪烁计数仪测定 Due to the unsatisfactory transdermal absorption of a large number of drugs and the lack of therapeutic requirements, many researchers are devoted to discovering transdermal absorption enhancers. In the early 1980s Azone was reported to be superior to dimethylsulfoxide (DMSO) in promoting transdermal absorption, though its mechanism of action is unclear. To further compare the structure-activity relationship of transdermal absorption enhancers, the authors investigated nine azacycloalkanones with one alkyl or alkenyl (terpene) side chain (10, 15, or 20 carbon atoms) (5,6 or 7-membered ring) derivatives to promote transdermal absorption. In vitro skin penetration experiments were performed on the skin of male guinea pigs (250 g) in a constant temperature water bath at 37 ° C. The drug used in the experiment was 6-mercaptopurine ([~ (14) C] 6-MP, 65 mCi / mmol) and was measured by LSC-903 scintillation counter