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目的:研究离子导入技术对卡托普利透皮吸收的促进作用。方法:应用离子导入技术研究了卡托普利体外透过大鼠离体皮肤的影响因素,并进行了卡托普利水凝胶贴片大鼠在体的试验,测定了血药浓度的变化。结果:离子导入技术可以有效地促进卡托普利的透皮吸收,透皮速率增加约7倍。药物贮库中的各种因素如pH,离子强度,药物浓度和电流强度均影响药物的透皮速率。随着pH的增加,离子强度的减小,药物浓度的增加及电流强度的增加,透皮速率也增加。大鼠在体试验也表明用药1h后血药浓度即可达到坪值(约0.9μg/mL),并在整个试验阶段维持稳定。结论:离子导入可以有效地促进卡托普利的透皮吸收。
Objective: To study the promotion of transcatheter captopril by iontophoresis. Methods: The iontophoresis technique was used to study the influencing factors of captopril in isolated rat skin in vitro and the in vivo experiments of captopril hydrogel patch were performed to determine the change of plasma concentration. Results: Iontophoresis could effectively promote the transdermal absorption of captopril, and the transdermal rate increased about 7 times. Various factors in the drug depot, such as pH, ionic strength, drug concentration, and current intensity, affect the drug’s transdermal rate. With the increase of pH, the decrease of ionic strength, the increase of drug concentration and the increase of current intensity, the transdermal rate also increased. Rat in vivo tests also showed that plasma concentration reached the plateau value (about 0.9μg / mL) after 1h, and remained stable throughout the experimental period. Conclusion: Iontophoresis can effectively promote the transdermal absorption of captopril.