透皮促进剂对胰岛素离子导入大鼠体内血糖水平的影响

TRANSDERMAL IONTOPORESIS OF INSULIN:EFFECT OF PENETRATION ENHANCERS ON BLOOD GLUCOSE LEVEL IN DIABETIC RATSJS

研究了几种常用透皮促进剂如月桂氮 酮（ａｚｏｎｅ，ＡＺ），油酸（ｏｌｅｉｃａｃｉｄ，ＯＡ），泊洛沙姆（ｐｏｌｏｘａｍｅｒ１８８，ＰＯＬ１８８）和丙二醇（ｐｒｏｐｙｌｅｎｅｇｌｙｃｏｌ，ＰＧ）等对胰岛素离子导入大鼠体内血糖水平的影响。结果显示：离子导入３ｈ后，１００％ＡＺ和５％ＡＺ／ＰＧ处理组，处理后对处理前的大鼠血糖变化百分率（Ｄ％）分别为３８．５８％和２５．２８％，而对照组的为４５．４８％。１００％ＯＡ，１０％ＯＡ／ＰＧ，１０％ＰＯＬ１８８％和１００％ＰＧ处理组的Ｄ％分别为６６．２８％，６０．４７％，７６．７５％和５７．９３％。表明月桂氮 酮与离子导入有协同作用，丙二醇能够增强这种作用，３者并用有特别显著的促渗作用。而油酸、泊洛沙姆、丙二醇不增强离子导入的作用。离子导入和某些透皮促进剂并用，为多肽类药物的体内给药提供了新的思路和可能性。

The effects of many usual penetration enhancers such as azone(AZ) ,oleic acid(OA),poloxamer 188(POL 188)and propylene glycol(PG)on the blood glucose level in diabeticrats after transdermal iontophoresis of insulin were studied. The change of blood glucose level(D%),defined as the percent ratio of the concentration of blood glucose in rats after the iontophoreticapplication of insulin to that before administration of insulin, was used to present the data. The resultsshowed that following iontophoretic application of insulin for 3 h, the D%in diabetic rats treated with100%AZ and 5%AZ/PG was 38.58%and 25.28%respectively, and the D%in diabetic ratsuntreated with enhancers was 45.48%.The D%in diabetic rats treated with 100%OA,10%OA/PG,10%POL 188/PG and 10O%PG was 66.28%, 60.47%, 76.75%and 57.93%respectively.So,AZ showed a synergistic effect on the ability of iontophoresis to promote skinpermeation of insulin, and PG further increased this effect.The combination of AZ, PG andiontophoresis increased the permeation of insulin significantly.OA,POL 188 and PG did not displaysynergistic effect on iontophoresis enhancement.The combination of iontophoresis and some enhancersprovided a novel idea and possibility for the administration of polypeptide drugs.