挥发油3种加入方式对止痛凝胶贴膏剂基质及体外释放度的影响

Effect of Three Kinds of Additive Methods of Volatile Oil on Matrix and in Vitro Release of Zhitong Cataplasms

目的:通过比较挥发油不同加入方式(直接加入法、微乳法和β-环糊精包合物法)对止痛凝胶贴膏剂的影响,确定该制剂中挥发油的最佳加入形式。方法:以初黏力、持黏力、剥离强度、赋形性为指标,比较凝胶贴膏剂基质的物理性质;以阿魏酸和藁本内酯为指标成分,比较挥发油3种加入方式对止痛凝胶贴膏剂中指标成分体外释放度的影响;以挥发油含量为考察指标,比较该制剂的稳定性。结果:与空白基质比较,挥发油的加入降低了基质的黏附力,但对赋形性无影响;挥发油以直接加入法、微乳法和β-环糊精包合物法方式加入时,制备的止痛凝胶贴膏剂中阿魏酸的24 h累计透过量分别为563.45,419.50,454.40μg·cm^(-2),藁本内酯依次为871.40,550.07,792.60μg·cm^(-2);与β-环糊精包合物法、直接加入法相比,微乳法制备的止痛凝胶贴膏剂稳定性最佳。结论:挥发油的加入对止痛凝胶贴膏剂基质的物理性质、体外释放量及稳定性均有一定影响,其中微乳法对基质的黏附性影响较小、稳定性较佳,但该方式有效成分的体外累计透过量不及直接加入法和β-环糊精包合物法制备的止痛凝胶贴膏剂。

Objective：To determine the optimal additive form of volatile oil in Zhitong cataplasms by comparing the effect of additive forms of volatile oil on this preparation,such as direct addition method,β-cyclodextrin inclusion method and microemulsion method.Method：The physical properties of the matrix were compared,such as the initial adhesive force,the sticking force,the peel strength and formability.Effect of three different ways of adding volatile oil on the in vitro release were compared by taking ferulic acid and ligustilide as indexes.The volatile oil content was taken as the index,and its stability was compared.Result：The addition of volatile oil affected the physical properties of the matrix,but Zhitong cataplasms prepared in the form of microemulsion had little effect.In 24 hours,the cumulative releases of ferulic acid in Zhitong cataplasms prepared by direct adding method,β-cyclodextrin inclusion method and microemulsion method were 563.45,454.4,419.5 μg·cm-2,and the cumulative releases of ligustilide were 871.40,792.60,550.07 μg·cm-2,respectively.Compared with direct addition method and β-cyclodextrin inclusion method,the stability of Zhitong cataplasms prepared by microemulsion method was the best.Conclusion：The addition of essential oil affects the physical properties,in vitro release and stability of the matrix in Zhitong cataplasms,the microemulsion method has little effect on the adhesion of the matrix and stability of Zhitong cataplasms,but the cumulative releases of active ingredients are less than direct adding method and β-cyclodextrin inclusion method.