吡罗昔康凝胶离子导入经皮给药研究

Study on transdermal iontophoresis of piroxicam gel

目的 考察吡罗昔康凝胶的体外经皮离子导入。方法 以高分子材料制备吡罗昔康凝胶 ,大鼠皮为模型皮肤 ,采用改良Franz扩散池分别进行药物凝胶的经皮直流电导入和超音频导入 (频率为 5 0kHz ,占空比为 1∶1) ,并测定了吡罗昔康从凝胶中的释放速率。结果 与被动扩散相比 ,电流密度分别为 0 .1mA·cm-2 和 0 .2mA·cm-2 的直流电对吡罗昔康凝胶通过大鼠皮的促渗倍数分别为 2 .0 1和 3.81,对离子型药物的促渗作用较为明显 ,吡罗昔康从凝胶中呈零级释放 ,在 0 .1mA·cm-2 的超音频电流作用下 ,吡罗昔康凝胶的透皮速率和 4h累积渗透量分别为 (14.2± 4.93) μg/cm-2 ·h-1和 (32 5± 2 7.0 ) μg。 结论 电流对吡罗昔康凝胶的经皮渗透有显著的促进作用 。

OBJECTIVE To investigate the transdermal iontophoresis of piroxicam gel in vitro .METHOD Different high molecule materials were employed to prepare piroxicam gel.Rat abdomen skin and modified Franz diffusion cells were used in the study of transdermal direct current iontophoresis and ultra audio iontophoresis(frequency=50kHz;on∶off=1∶1).The release rate of piroxicam from the gel was also investigated.RESULTS The enhanced rates of direct current iontophoresis of piroxicam gel at 0.1 mA·cm -2 and 0.2 mA·cm -2 were 2.01 and 3.81,respectively.Piroxicam released from drug gel was coincide with zero order.With ultra audio iontophoresis at 0.1 mA·cm -2 ,the flux and 4h cumulative permeation amount of piroxicam were (14.2±4.93) μg·cm -2 ·h -1 and (325±27.0) μg,respectively.CONCLUSION The results suggested that the enhancement to ionized drug was greater than that of uncharged drug.Iontophoresis could significantly increase the transdermal permeation of piroxicam gel.There were no statistically difference between the flux and the cumulative permeation amount of piroxicam gel with direct current iontophoresis and ultra audio iontophoresis.