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不同的赋形剂、添加剂会影响皮肤屏障,从而对药物穿透皮肤产生影响。本研究的目的是为了测定油酸对17β-雌二醇、曲安缩松及三氟胸苷透皮的影响,并且了解在二元油酸赋形剂体系中丙二醇能否被极性较小的2-乙基-1,3-已二醇(EHD)替代而不降低该体系的助渗效果。研究结果表明,17β-雌二醇的渗透系数(P)在含有2.5%油酸的丙二醇赋形剂中与不含油酸的同样赋形剂相比增加了6倍。当油酸浓度提高到10%时,渗透效果只增加2倍,这可能是由于随着浓度增加,药物在赋形剂中溶解度增加而引起的。在二元赋形剂体系中,当丙二醇被EHD 替代后,油酸的助渗效果很低。在丙二醇赋形剂体系中,当月桂氮(?)酮(azone)替代油酸时,渗透效果也显著降低。
Different excipients, additives can affect the skin barrier, thus affecting the drug through the skin. The purpose of this study was to determine the effect of oleic acid on the transdermal delivery of 17β-estradiol, triamcinolone and trifluorothymidine and to understand whether propylene glycol can be less polar in the binary oleic excipient system Of 2-ethyl-1,3-hexanediol (EHD) without reducing the osmotic effect of the system. The results show that the permeability coefficient (P) of 17 [beta] -estradiol is increased six-fold in the propylene glycol vehicle containing 2.5% oleic acid compared to the same vehicle without oleic acid. The osmotic effect increased by only 2-fold when the oleic acid concentration was increased to 10%, probably due to the increased solubility of the drug in the vehicle as the concentration increased. In binary vehicle systems, oleic acid has a low osmotic effect when propylene glycol is replaced by EHD. In the propylene glycol vehicle system, osmotic effect is also significantly reduced when azone is substituted for oleic acid.