透皮促进剂对消旋延胡索乙素体外经皮渗透的影响

 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NFDB3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NFDB3酮、丙二醇单独使用均对延胡索乙素有促透作用,月桂氮NFDB3酮促透效果较强,8%月桂氮NFDB3酮促透效果最好,平均渗透速率达到12.397 μg·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3.142 μg·cm^-2·h^-1。两者合用促透效果始终小于月桂氮NFDB3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NFDB3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NFDB3酮和丙二醇合用并未体现协同作用。

Influence of Penetration Enhancers on in Vitro Transdermal Permeation of D,L-Tethrahydropalmatine

OBJECTIVE To study the effect of penetration enhancers on the transdermal permeation in vitro of D,L-Tethrahydropalmatine (D,L-THP) through rat skin.METHODS Azone and propylene glycol (PG) as chemical penetration enhancers were applied alone or jointly to investigate the skin permeation rates of D,L-THP. The skin permeation profiles were evaluated by Valian-Chien permeation cells with isolated rat skin. HPLC-UV method was established to determine the concentration of D,L-THP in samples. RESULTS 8% Azone alone was observed to be the optimal penetration enhancer with the maximal penetration rate of 12.397 μg·cm^-2·h^-1. The highest penetration rate of PG alone was achieved at 15% with the rate of 3.142 μg·cm^-2·h^-1. The penetration potency of azone combined with PG was less effective than that of Azone alone. CONCLUSION 8% Azone was effective on transdermal permeation of D,L-THP in vitro. There is no synergistic effect to be found when Azone combined with various concentrations of PG.