萘普生前药及其经皮渗透特征

Study on prodrugs of naproxen and their dermal permeability

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.