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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。
Objective: To investigate the effect of N-trimethyl chitosan (TMC) as a transdermal absorption enhancer. Methods: Chitosan and methyl iodide were used as main raw materials to synthesize TMC with quaternization degree of 60%, namely TMC60. The degree of quaternization was determined by1H-NMR. Using 2% Azone as a positive control and diclofenac sodium as a model drug, the skin of the isolated mice was used as a barrier. The pretreatment method was used to investigate the effect of 2% TMC60 on penetration of diclofenac sodium through isolated skin. Results: The degree of quaternization of TMC60 synthesized by ~ 1H-NMR was 67.2%. In vitro transdermal experiments, the order of cumulative transmutation and steady transdermal rate were as follows: TMC60 group> azone group> blank group. The promoting effect of TMC60 was greater than that of azone at the same concentration (P <0.05). Conclusion: TMC has good transdermal and osmotic effect on diclofenac sodium.