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目的考察不同透皮促进剂对消旋延胡索乙素体外经皮渗透的影响。方法采用Valia-Chien双室渗透扩散池,以大鼠离体皮肤为渗透屏障,用高效液相色谱法对延胡索乙素进行含量测定,考察月桂氮酮、丙二醇及两者按不同比例混合对消旋延胡索乙素的促透效果。结果月桂氮酮、丙二醇单独使用均对延胡索乙素有促透作用,月桂氮酮促透效果较强,8%月桂氮酮促透效果最好,平均渗透速率达到12.397μg.cm-2.h-1。单用丙二醇时,15%丙二醇促透效果较好,平均渗透速率为3.142μg.cm-2.h-1。两者合用促透效果始终小于月桂氮酮单独使用时效果,且与单用8%Azone有极显著性差异(P<0.01)。结论月桂氮酮浓度为8%时消旋延胡索乙素饱和溶液体外渗透具有最大促透效果,月桂氮酮和丙二醇合用并未体现协同作用。
Objective To investigate the effects of different transdermal enhancers on transdermal permeation of racemic tetrahydropalmatine in vitro. Methods Valia-Chien dual-chamber osmotic diffusion cells were used to separate the skin of rats as permeation barrier. The content of tetrahydropalmatine was determined by HPLC. The effects of different concentrations of azinon, Hydrochloric acid tetrahydropalmatine prophylactic effect. Results Both azinonone and propanediol could enhance the permeation of tetrahydropalmatine, the permeation efficiency of azinon was stronger, the permeation rate of 8% laurocapram was the best, and the average penetration rate reached 12.397μg.cm- 2.h-1. Propylene glycol alone, 15% propylene glycol penetration better, with an average penetration rate of 3.142μg.cm-2.h-1. The combination effect of the two is always less than the effect of azathione alone, and extremely significant difference with 8% Azone (P <0.01). CONCLUSION: In vitro permeation of racemic tetrahydropalmatine (OVX) with azinon ketone concentration of 8% has the most obvious permeation enhancing effect. The combination of azaseride and propylene glycol did not show synergistic effect.