摘要
目的：考察N-三甲基壳聚糖（N—trimethylchitosan，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。
Objective： To study the penetration effect of N-trimethyl chitosan （TMC） on Diclofenac sodium. Method： TMC60 was synthesized by a two-slep 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 penetration 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 Diclofenae sodium.
出处
《中国药师》
CAS
2007年第12期1186-1188,共3页
China Pharmacist
