6种透皮吸收促进剂对盐酸普萘洛尔乳膏透皮吸收性能的影响

摘要

目的:考察氮酮、油酸、丙二醇、氮酮+油酸、氮酮+丙二醇、油酸+丙二醇6种透皮吸收促进剂对盐酸普萘洛尔乳膏透皮性能的影响.方法:分别制备含氮酮、油酸、丙二醇、氮酮+油酸、氮酮+丙二醇、油酸+丙二醇6种透皮吸收促进剂的盐酸普萘洛尔乳膏,透皮吸收促进剂的量均为2％.采用智能透皮试验仪进行大鼠体外透皮吸收试验,高效液相色谱法测定6种盐酸普萘洛尔乳膏接受液中盐酸普萘洛尔的含量,并计算12h内的单位面积累积透过量(Q)和经皮渗透速率(J),同时与无促进剂的盐酸普萘洛尔乳膏进行比较.结果:以Q为指标,促透作用依次为:油酸[(2 552.01±264.59) μg/cm2]＞氮酮[(2 389.39±346.45) μg/cm2]＞油酸+丙二醇[(2 082.04±214.30) μg/cm2]＞丙二醇[(1 852.92±256.00) μg/cm2]＞氮酮+油酸[(1 602.55±13.56) μg/cm2]＞氮酮+丙二醇[(1 432.35±149.02) μg/cm2]＞无促进剂[(1 030.68±98.00) μg/cm2].与以J为指标得出的结果相同.结论:6种透皮吸收促进剂均可增强盐酸普萘洛尔局部给药的透皮吸收作用,其中以油酸的促透作用最好.%OBJECTIVE:To investigate the effects of 6 penetration enhancers on percutaneous absorption of Propranolol hydrochloride cream,such as azone,oleic acid,propanediol,azone+oleic acid,azone+propanediol,oleic acid+propanediol.METHODS:Propranolol hydrochloride creams added with 6 penetration enhancers were prepared with penetration enhancers concentration of 2 ％.In vitro percutaneous absorption test of rats was performed with intelligent permeability instrument,and the contents of propranolol hydrochloride in 6 kinds of cream receptors were determined by HPLC.The accumulative transit dose (Q) and percutaneous permeability (J) within 12 h were calculated and compared with those of Propranolol hydrochloride cream without enhancer.RESULTS:With Q value as index,the action of 6 penetration enhancers in descending order was as follows:oleic acid [(2 552.01 ± 264.59) μg/cm2] ＞azone[(2 389.39 ± 346.45) μg/cm2] ＞oleic acid+propanediol[(2 082.04 ± 214.30) μg/cm2] ＞propanedio1[(1 852.92 ± 256.00) μg/cm2] ＞azone+oleic acid[(1 602.55 ± 13.56) μg/cm2] ＞azone+propanediol[(1 432.35 ± 149.02) μg/cm2] ＞no enhancer[(1 030.68 ± 98.00) μg/cm2],the same to the result with J value as index.CONCLUSIONS:6 kinds of penetration enhancers can enhance the percutaneous absorption of Propranolol hydrochloride cream with local administration,and oleic acid is the best.