醇类基质的极性对酮洛芬透皮释药行为的影响

 目的 探讨酮洛芬在一系列醇类基质中的体外透皮释药规律。方法 建立以联苯酚为内标的HPLC，测定接收液中酮洛芬的含量；以甲醇到正壬醇一系列溶剂配制相同浓度的酮洛芬供给液（100 mg·mL^-1），用水平扩散池研究体外透皮释药行为；冷冻切片考察各种溶剂对皮肤结构的影响。结果 从冷冻切片发现，甲醇、乙醇和正丙醇对皮肤的损伤较大，这可能是酮洛芬在三者中的透皮释放量较大的原因；除甲醇、乙醇、正丙醇外，从正丁醇到正辛醇随着溶剂极性减小，酮洛芬的累计透过量和释药速率增加；正壬醇的累计透过量略小于正辛醇，但两者无显著性差异；测定方法可靠。结论 随着醇类基质的极性减小，酮洛芬透皮释放增大。

Study on the permeation of ketoprofen excised rat skin in various alcohois

OBJECTIVE To investigate the influence of polarity of various alcohols on the permeation of ketoprofen(KTP) through excised rat skin.METHODS HPLC method with xenol as the internal standard was established to determine the content of KTP in receiver diffusion cell.The permeation behavior of KTP through excised rat skin in a series of alcohols (100 mg·mL^-1) was studied with Valia-Chien in vitro releasing device.The freezing microtomy was used to find the influence of various alcohols on skin.RESULTS Based on the freezing microtomy,it was found that methanol,ethanol and n-propanol injured skin considerablly,which related to the high permeation of KTP in them. The cumulative penetrating amount and steady state flux of KTP increased when the polarity of solvents decreased from n-butyl alcohol to n-octyl alcohol.There was no significant difference on the permeation of KTP in n-octyl alcohol and n-nonyl alcohol.CONCLUSION The permeation of KTP through excised rat skin increased when the polarity of the preparation decreased.