摘要
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.
出处
《药学学报》
CAS
CSCD
北大核心
1995年第10期776-780,共5页
Acta Pharmaceutica Sinica
基金
国家自然科学基金