基质pH及促渗剂对阿昔洛韦水凝胶贴剂体外透皮性能的影响

分别制备了基质pH为5.0、6.0、7.5的不含促渗剂的阿昔洛韦水凝胶贴剂,在基质pH 6.0的处方中加入不同浓度的月桂氮革酮、Ⅳ.甲基吡咯烷酮(NMP)、薄荷醇、吐温-80、聚乙二醇(PEG)400作为促渗荆,以考察基质pH及促渗剂对阿昔洛韦透过离体小鼠皮肤的影响.结果表明,基质pH升高,阿昔洛韦的透皮速率增大.与不含促渗剂的基质pH6.0处方组对照,NMP、PEG 400单用不能提高阿昔洛韦的渗透速率,4%的吐温-80、薄荷醇和月桂氮革酮均可提高阿昔洛韦的经皮渗透.

Influence of Matrix pH and Percutaneous Enhancers on in vitro Permeation of Acyclovir Hydrogel Patch

Acyclovir hydrogel patches with out percutaneous enhancer in matrix pH of 5.0, 6.0 and 7.5 were prepared, respectively. And several percutaneous enhancers such as azone, N-methylpyrrolidone (NMP), menthol, Tween-80 and PEG 400 with different concentrations were added to the patches in matrix pH of 6.0, respectively. The influences of matrix pH values and percutaneous enhancers on permeation of acyclovir through excised mouse skin were investigated. The results showed that the permeation rate of acyclovir increased with the increasing of matrix pH value. Compared with the pH 6.0 patch without percutaneous enhancer, NMP and PEG 400 alone had little enhancement effect on the permeability, while 4% Tween-80, menthol and azone showed significant enhancing effect.