不同吸收促进剂及酶抑制剂对胰岛素体内及体外口腔黏膜渗透性的影响  

Comparison of the effects of various absorption enhancers and enzyme inhibitors on buccal insulin delivery in vitro and in vivo

作　　者：杨天智[1] 陈大兵[1] 张强[1] 

机构地区：[1]北京大学药学院药剂学系,北京100083

出　　处：《北京大学学报（医学版）》2001年第3期238-242,共5页Journal of Peking University:Health Sciences

摘　　要：目的 :研究不同的吸收促进剂及酶抑制剂对胰岛素透过口腔黏膜的影响。方法 :体外实验中 ,在不同吸收促进剂及酶抑制剂作用下 ,测定胰岛素透过仓鼠和家兔口腔黏膜的渗透系数 ;体内实验中 ,在胰岛素口腔喷雾剂中加入不同的吸收促进剂及酶抑制剂 ,考察大鼠经口腔喷入胰岛素后的血糖降低情况。结果 :SDCh ,Brij78,SLS以及lecithin可以显著增加胰岛素透过口腔黏膜的渗透系数 ,而aprotinin ,bacitracin ,1 menthol以及 poloxamer的作用相对较小。胰岛素溶液中加入SDCh ,Brij78,SLS以及lecithin后 ,正常大鼠口腔喷雾给药 ,药理生物利用度都有显著的提高 ,而aprotinin ,bacitracin ,1 menthol以及 poloxamer对血糖的影响较小。结论 :对于考察吸收促进剂及酶抑制剂对胰岛素的促进吸收作用来说 ,体外实验与体内实验结果是一致的 ,可以通过体外实验来粗略地筛选吸收促进剂及酶抑制剂 。To study the effects of various absorption enhancers and enzyme inhibitors on insulin permeation in vitro and in vivo . Methods: The penetration of insulin through hamster and rabbit buccal membrane was investigated by measuring in vitro transbuccal flux. Buccal insulin absorption was estimated in vivo from the cumulative response of serum glucose concentrations and comparison was made with the results of subcutaneous experiments. Results: There was a statistically significant permeability increase of insulin over controls after co administration with the SDCh, Brij78, SLS or lecithin, aprotinin, bacitracin, whereas 1 menthol or poloxamer were less effective. Buccal insulin efficacy in the absence of co administration adjuvants was very low relative to subcutaneous administration of insulin. When co administered buccally with SDCh, SLS, lecithin or Brij78, Fr (relative pharmacological bioavailability) values were all increased significantly. Conclusion: The present studies showed that with the most effective absorption adjuvants, buccal insulin was one fifth to one fourth as effective as subcutaneous insulin. Results of in vitro experiments were in agreement with the in vivo results with respect to the enhancement of these adjuvants.

关 键 词：胰岛素 代谢 口腔黏膜 吸收促进剂 酶抑制剂 药理学 渗透性 

分 类 号：R977.15[医药卫生—药品]