不同季铵化程度的N-三甲基壳聚糖对双氯芬酸钠体外经皮吸收的影响研究  

Effect of Quaternization Degree of N-trimethyl Chitosan on Transdermal Penetration of Diclofenac Sodium in vitro

作　　者：于书海[1] 王军[2] 何文[2] 

机构地区：[1]河南省人民医院药学部,郑州450003 [2]武汉大学人民医院药学部

出　　处：《中国药师》2013年第3期337-338,341,共3页China Pharmacist

摘　　要：目的:考察N-三甲基壳聚糖(TMC)的季铵化程度(DQ)对双氯芬酸钠(DS)透皮吸收促进作用的影响。方法:以壳聚糖及碘甲炕为主要原料,合成DQ分别为20%,40%及60%的TMC,即TMC20,TMC40及TMC60。以2%氮酮为阳性对照,以离体小鼠皮肤为屏障,考察同浓度的各种TMC对DS凝胶的透皮促进作用。结果:TMC20,TMC40及TMC60的DQ分别为20.2%,40.1%及64.4%。体外DS的累积透过量及稳态透皮速率大小顺序为TMC60组>氮酮组>TMC40组>TMC20组>空白组,其中TMC60的促进作用大于同浓度的氮酮(P<0.05),而TMC40及TMC20的促进作用弱于氮酮(P<0.05)。结论:TMC的DQ对其发挥透皮吸收促进作用有较大的影响。Objective：To study the effect of quaternization degree（DQ） of N-trimethyl chitosan（TMC） on the transdermal penetration of diclofenac sodium（DS） in vitro.Method：TMC with DQ of 20%,40%and 60%,namely TMC20,TMC40 and TMC60, was respectively synthesized by a two-step method using ehitosan and methyl iodide.2%Azone as the positive control,the transdermal penetration enhancement of TMC20,TMC40 and TMC60 to DS gels was studied using the excised mice skin as the barrier.Result：DQ of TMC20,TMC40 and TMC60 was 20.2%,40.1%and 64.4%,respectively.The order of cumulative penetration（Q） and the steady penetration rate（J） was TMC60 group Azone group TMC40 group TMC20 group the blank control.The results showed the significant transdermal penetration enhancement of TMC,and TMC60 was stronger than Azone（P 0.05） while TMC20 and TMC40 were weaker than that of Azone（P 0.05）.Conclusion：DQ exhibits notable effect on the transdermal penetration enhancement of TMC.

关 键 词：N-三甲基壳聚糖 透皮吸收促进作用 季铵化程度 

分 类 号：R945[医药卫生—微生物与生化药学]