双氯芬酸钠气雾剂的透皮吸收作用

Diclofenac sodium percutaneous penetration in its aerosol

目的 :考察双氯芬酸钠气雾剂中双氯芬酸钠的透皮吸收情况。方法 :采用双室扩散池法进行体外透皮吸收试验 ,用高效液相色谱法测定家兔经皮给药的血清药物浓度 ,并测定经皮给药的LD50 。结果 :双氯芬酸钠在促进剂的作用下 ,可显著地透过离体皮肤 ;家兔血清药物浓度测定发现 ,经皮给药后 ,双氯芬酸钠气雾剂的吸收速率常数较快 (0 .71h-1) ,达峰时间需2 .2 6h ,峰浓度较高 ,在体内的驻留时间较长 (6 .5 8h) ;按Bliss法计算LD50 为 2 0 5 .0 5mg·kg-1。结论 :气雾剂中的双氯芬酸钠可透过皮肤吸收。

OBJECTIVE:To study diclofenac sodium percutaneous penetration in its aerosol.METHODS:Diclofenac sodium permeation tests in vitro through naked rat skin in two compartment diffusion device were performed;serum diclofenac sodium concentrations were determined with HPLC in rabbits;and LD50 was calculated.RESULTS:Under the effect of transdermal enhancers,diclofenac sodium could penetrate through naked rat skin markedly in vitro;after determining serum diclofenac sodium concentrations,it was found that diclofenac sodium had a faster absoption rate constant( 0.71 h -1 ),a longer arrived peak time( 2.26 h),a higher peak concentration and a longer MRT;LD 50 was 205.05 mg·kg -1 by Bliss methods.CONCLUSIONS:Diclofenac sodium in diclofenac sodium aerosol could percutaneous penetration.