萘普生前药及其经皮渗透特征  

Study on prodrugs of naproxen and their dermal permeability

作　　者：成志毅[1] 朱辉[1] 

机构地区：[1]中山大学药学院,广东广州510080

出　　处：《中国现代应用药学》2004年第5期379-382,共4页Chinese Journal of Modern Applied Pharmacy

摘　　要：目的　研究萘普生前药的经皮渗透性。方法　合成萘普生酯作为萘普生的前药 ,考察这些前药的经皮渗透速率和在经皮渗透过程中被皮肤代谢的情况。结果　合成了 7个萘普生酯 ,其中萘普生薄荷酯的经皮渗透速率超过了萘普生的渗透速率 ,萘普生前药在经皮渗透过程中均能一定程度地被皮肤代谢。结论　萘普生酯的酯基为 8～ 10个碳链 ,有利于前药经皮渗透 。OBJECTIVE To investigate the dermal permeability of naproxen's prodrugs.METHOD Synthesizing esters of naproxen as its prodrugs and testing their dermal permeability.RESULTS Seven esters of naproxen were synthesized, the dermal penetration rate of menthyl naproxen exceeded the rate of its matrix, naproxen's prodrugs were metabolized in a certain extent during penetration through skin.CONCLUSION The prodrug of naproxen with 8～10 carbon-chain ester group is propitious to dermal penetration and the lipophilic prodrug tends to be metabolized in skin.

关 键 词：萘普生 前药 合成 经皮渗透 

分 类 号：R971[医药卫生—药品] R943.43[医药卫生—药学]