N-三甲基壳聚糖对双氯芬酸钠经皮渗透作用的研究

目的:考察N-三甲基壳聚糖(N-trimethyl chitosan,TMC)作为透皮吸收促进剂的作用。方法:用壳聚糖及碘甲烷为主要原料,合成季铵化程度为60%的TMC,即TMC60,通过1H-NMR确定其季铵化程度。以2%氮酮为阳性对照,以双氯芬酸钠为模型药物,以离体小鼠皮肤为屏障,采用预处理法考察2%TMC60对双氯芬酸钠透过离体皮肤的促渗作用。结果:经~1H- NMR确定合成得到的TMC60季铵化程度为67.2%。体外透皮实验中,累积透过量及稳态透皮速率大小顺序均为:TMC60组>氮酮组>空白组,TMC60的促进作用强度大于同浓度的氮酮(P<0.05)。结论:TMC对双氯芬酸钠具有较好的经皮促渗透作用。

Study on Penetration Effect of N-trimethyl Chitosan on Diclofenac Sodium

Objective:To study the penetration effect of N-trimethyl chitosan(TMC)on Diclofenac sodium.Method:TMC60 was synthesized by a two-step method,chitosan and methyl-iodide were used.The degree of quaternization of TMC was determined by ~1H-NMR.The excised mice skin treated by 2% TMC60 or 2% Azone was employed to study the 12h cumulative penetration,Diclofenac sodium was used as model drug.Result:The DQ of TMC60 was 67.2%.The order of cumulative penetration(Q)and the steady pene- tration rate(J)was TMC60 group>Azone group>blank control.The penetration enhancement of TMC60 was stronger than that of Azone(P<0.05).Conclusion:The TMC60 was a promising penetration enhancer for Diclofenac sodium.