离子导入对卡托普利透皮吸收的促进作用(英文)

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。

Improvement of transdermal permeation of captopril by iontophoresis

AIM: The feasibility of iontophoresis on the transdermal delivery of captopril was studied. METHODS: Iontophoresis was employed for enhancing transdermal transport of captopril through rat skin in vitro and in vivo. RESULTS: It was demonstrated that the iontophoresis-induced flux of captopril was affected by various factors such as pH, ionic concentration, and the concentration of captopril in donor compartments as well as the applied electric current intensity. Electric current could induce several-fold increase in captopril flux with hydrogel. Skin permeation study in vivo in rats demonstrated that iontophoresis could effectively promote the transdermal transport of captopril without significant skin irritation. Captopril concentration in plasma reached plateau (approximately 0.9 microgram/mL) at 1 h after current application and was maintained at the same level during the experiment. On the contrary, captopril could not be detected in plasma when the current was not applied. No obvious skin irritation was observed after 9-h continuous iontophoresis. CONCLUSION: Transdermal delivery of captopril can be effectively improved by iontopophoresis.