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吡罗昔康经皮离子导入及含吡罗昔康:羟丙基-β-环糊精复合物的凝胶中吡罗昔康的皮肤滞留情况

Transdermal lontophoresis and skin retention of piroxicam from gels containing piroxicam: hydroxypropyl-beta-cyclodextrin complexes.

作者信息

Doliwa A, Santoyo S, Ygartua P

机构信息

Centro Galénico, Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Navarra, Pamplona, Spain.

出版信息

Drug Dev Ind Pharm. 2001 Sep;27(8):751-8. doi: 10.1081/ddc-100107238.

Abstract

Iontophoretic transport of piroxicam (Px) across porcine ear skin in vitro was investigated. Cathodal iontophoresis of negatively charged Px was carried out from gel formulations containing Px as an inclusion complex with hydroxypropl-beta-cyclodextrin (HP-beta-CD). From the gels, following a 7h application period at 0.4 mA/cm2, iontophoresis delivered 3.4 times more drug than passive diffusion. The formation of Px:-HP-beta-CD complexes did not increase the iontophoretic Px flux through the skin. However, Px complexation with HP-beta-CD allowed us to increase the drug concentration in the gel; because of that, the amount of Px transported across the skin increased considerably. After iontophoretic experiments, the amount of Px retained in skin seemed to be related to the flux values obtained in each case. Skin pretreatment with 20% HP-beta-CD, tested passively and iontophoretically for 3h, followed by the application of gel containing Px: HP-beta-CD complexes, showed no enhancing capacity in any case. The amount of Px retained in the skin after pretreatment experiments was found to be very similar to that obtained without skin pretreatment and was observed to be related to the Px flux through the skin.

摘要

研究了吡罗昔康(Px)在体外经猪耳皮肤的离子导入转运。以吡罗昔康与羟丙基-β-环糊精(HP-β-CD)形成的包合物形式,从含吡罗昔康的凝胶制剂中进行带负电荷的吡罗昔康的阴极离子导入。在0.4 mA/cm²的电流下作用7小时后,离子导入从凝胶中递送的药物比被动扩散多3.4倍。吡罗昔康与HP-β-CD形成的复合物并未增加其经皮离子导入通量。然而,吡罗昔康与HP-β-CD的络合使我们能够提高凝胶中的药物浓度;因此,经皮转运的吡罗昔康量显著增加。离子导入实验后,皮肤中保留的吡罗昔康量似乎与每种情况下获得的通量值有关。用20%的HP-β-CD对皮肤进行预处理,分别进行3小时的被动和离子导入测试,然后施用含吡罗昔康-HP-β-CD复合物的凝胶,在任何情况下均未显示出增强作用。发现预处理实验后皮肤中保留的吡罗昔康量与未进行皮肤预处理时获得的量非常相似,且观察到其与吡罗昔康经皮通量有关。

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