月桂氮卓酮复合促吸收剂促胰岛素经舌下黏膜吸收的研究

目的研究促胰岛素经舌下黏膜吸收的月桂氮卓酮 (Azone)复合促吸收剂。方法应用正常大鼠的降血糖实验对Azone复合促吸收剂的组成进行正交筛选 ,研究胰岛素在不同组成的促吸收剂作用下对猪舌下黏膜的体外渗透扩散系数及促渗比。结果由正交实验确定了最佳组成中Azone复合促吸收剂的比例为 2 .5 %Azone、5 %丙二醇、2 .5 %吐温 80。胰岛素分别在 5 %丙二醇、5 %丙二醇 +2 .5 %吐温 80、5 %丙二醇 +2 .5 %吐温 80 +2 .5 %A zone促吸收剂作用下的促渗比分别为 1.9(P >0 .0 5 )、2 .6 (P >0 .0 5 )和 7.8(P <0 .0 5 )。结论Azone复合促吸收剂中Azone是使黏膜通透性发生变化的主要因素。

Study on absorption promoting Azone composite for enhancing the sublingual absorption of insulin

PurposeTo study absorption promoting Azone composite for enhancing the sublingual absorption of insulin.MethodsInsulin emulsion was prepared by mixing insulin phosphonate buffer (pH 7.4) with Azone composite , and the ideal formulation of insulin emulsion (IFIE) was screened out by orthogonal test according to the hypoglycemic effects on rats. The permeation coefficient (P) and enhancement ratio of insulin co-administration with different absorption promoting composite through pig sublingual membrane was investigated.ResultsIFIE was composed of 5% propylene glycol(PG), 2.5% Azone, 2.5% Tween-80 and 18.7 u/ml insulin in phosphonate buffer. Enhancement ratio of 5% PG is 1.9 (P>0.05), 5% PG 2.5% Tween-80 2.6 (P>0.05) and 5% PG 2.5% Tween 80 2.5% Azone 7.8 (P<0.05).ConclusionIn the absorption promoting Azone composite, Azone plays a key role in affecting the sublingual membrane.