不同化学促渗剂对核应急碘化钾经皮渗透作用的影响

Effect of different chemical enhancers on percutaneous permeation of potassium iodide in nuclear emergency

目的通过探讨不同化学促渗剂对碘化钾体外经皮渗透的影响,筛选出最佳促渗方案。方法选用乙醇、丙二醇、氮酮、薄荷醇为碘化钾促渗剂,采用改良的Franz扩散池法,以离体大鼠背部皮肤为透皮屏障,以碘化钾的累积透过量(Q)、稳态透皮速率(Js)、增渗比(ER)等作为主要指标,评价不同促渗剂单用或联用对碘化钾的促渗效果。结果4种促渗剂对碘化钾均有不同程度的经皮促渗作用,其中乙醇的促渗作用明显优于丙二醇,氮酮的促渗作用明显优于薄荷醇。当乙醇浓度为10%~75%时,碘化钾累积透过量及稳态透皮速率随着乙醇浓度升高而增加。当丙二醇浓度为5%~50%时,各组碘化钾累积透过量由高到低排序为:10%>5%>0%>25%>50%。当氮酮和薄荷醇浓度为1%~10%时,碘化钾累积透过量和稳态透皮速率随着促渗剂浓度升高而增加,二者联用具有协同作用。当促渗剂为10%氮酮时,增加碘化钾浓度使碘化钾累积透过量接近成倍增加。结论本研究筛选出终浓度为50%乙醇、10%氮酮和2%碘化钾为碘化钾经皮渗透最佳处方,5%氮酮联合5%薄荷醇使用也可取得良好的碘化钾经皮渗透效果。

Objective To i nvestigate t he e ffect o f d ifferent c hemical p ermeation e nhancers o n t ransdermal penetration of potassium iodide in vitro,and to screen out the best penetration-enhancement scheme.Methods Ethanol,propylene glycol,azone,and menthol were selected as permeation enhancers of potassium iodide.Improved Franz diffusion cell method was adopted and the isolated back skin of rats were used as the transdermal barrier.The cumulative penetration amount(Q)of potassium iodide,the steady-state penetration rate(Js),and the enhancement ratio(ER)were used as main indicators to evaluate the effect of single or combined application of different permeation enhancers on transdermal penetration of potassium iodide.Results The four kinds of permeation enhancers could promote the transdermal penetration of potassium iodide to varying degrees.The penetrationenhancement effect of ethanol was better than that of propylene glycol,and that of azone was better than menthol.When the concentration of ethanol was 10%~75%,the Q and Js of potassium iodide increased with the increase of ethanol concentration.When the concentration of propylene glycol was 5%~50%,the Q of potassium iodide in each group ranked from high to low as follows:10%>5%>0%>25%>50%.When the concentration of azone and menthol was 1%~10%,the Q and Js of potassium iodide increased with the increase of azone and menthol concentration.The combination of azone and menthol had a synergic effect.When the concentration of potassium iodide was increased,the Q of potassium iodide increased nearly the same fold.Conclusion The final concentration of 50%ethanol,10%azone and 2%potassium iodide was selected as best prescription for transdermal penetration of potassium iodide.The combination of 5%azone and 5%menthol can also obtain a good potassium iodide penetration effect.