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

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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 investigate the effect of quaternization (DQ) of N-trimethyl chitosan (TMC) on the transdermal absorption of diclofenac sodium (DS). Methods: Chitosan and Iodine were used as main raw materials to synthesize TMCs with TQ of 20%, 40% and 60% respectively, namely TMC20, TMC40 and TMC60. A 2% Azone was used as a positive control. The skin of mice was used as a barrier to investigate the transdermal effects of various concentrations of TMC on DS gel. Results: The DQ of TMC20, TMC40 and TMC60 were 20.2%, 40.1% and 64.4% respectively. The cumulative transdermal flux and the steady-state transdermal rate of DSMC in vitro were in order of TMC60 group> azone group> TMC40 group> TMC20 group> blank group, with the promotion of TMC60 being greater than that of Azone at the same concentration (P <0.05) And TMC20 were weaker than Azone (P <0.05). Conclusion: DQ of TMC has a great influence on its transdermal absorption.
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