Hao J S, Zheng J M, Yang W Z
Department of Pharmaceutics, Shenyang Pharmaceutical University.
Yao Xue Xue Bao. 1995;30(10):776-80.
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 diabetic rats 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 iontophoretic application of insulin to that before administration of insulin, was used to present the data. The results showed that following iontophoretic application of insulin for 3 h, the D% in diabetic rats treated with 100% AZ and 5% AZ/PG was 38.58% and 25.28% respectively, and the D% in diabetic rats untreated with enhancers was 45.48%. The D% in diabetic rats treated with 100% OA, 10%-OA/PG, 10% POL 188/PG and 100% 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 skin permeation of insulin, and PG further increased this effect. The combination of AZ, PG and iontophoresis increased the permeation of insulin significantly. OA, POL 188 and PG did not display synergistic effect on iontophoresis enhancement. The combination of iontophoresis and some enhancers provided a novel idea and possibility for the administration of polypeptide drugs.
研究了许多常用渗透促进剂，如氮酮（AZ）、油酸（OA）、泊洛沙姆188（POL 188）和丙二醇（PG）对糖尿病大鼠经皮离子导入胰岛素后血糖水平的影响。血糖水平变化率（D%）定义为离子导入胰岛素后大鼠血糖浓度与胰岛素给药前血糖浓度的百分比，以此来呈现数据。结果显示，经皮离子导入胰岛素3小时后，用100% AZ和5% AZ/PG处理的糖尿病大鼠的D%分别为38.58%和25.28%，未用促进剂处理的糖尿病大鼠的D%为45.48%。用100% OA、10% OA/PG、10% POL 188/PG和100% PG处理的糖尿病大鼠的D%分别为66.28%、60.47%、76.75%和57.93%。因此，AZ对离子导入促进胰岛素经皮渗透的能力具有协同作用，而PG进一步增强了这种作用。AZ、PG与离子导入相结合显著增加了胰岛素的渗透。OA、POL 188和PG对离子导入增强作用未显示协同效应。离子导入与某些促进剂的结合为多肽药物的给药提供了新的思路和可能性。
