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_杨天智.pdf

( ) ·238 · JOURNAL OF PEKING UNIVERSITY(HEALTH SCIENCES)　Vol.33　No.3　June 2001 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 ■ 杨天智, 陈大兵,张　强 (, 　100083) [] /;;;/; [　] 目的:。方法:, , ;, , 。结果:SDCh, Brij78, SLS lecithin , aprotinin, bacitracin, 1-menthol poloxamer 。SDCh, Brij78, SLS lecithin , , , aprotinin, bacitracin, 1-menthol poloxamer 。结论: , , , 。 [] R977.15-332　　[] A　　[] 1671-167 (2001)03-0238-05 Comparison of the effects of various absorption enhancers and enzyme inhibitors on buccal insulin delivery in vitro and in vivo YANG Tian-Zhi, CHEN Da-Bing, ZHANG Qiang (Department of Pharmaceutics, Peking University School of Pharmaceutical Sciences, Beijing　100083, China) KEY WORDS　Insulin/metab;Mouth mucosa;Absorption enhancers;Enzyme inhibitors/pharmacol; Permeability SUMM RY　Objective: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 ab- sorption was estimated in vivo from the cumulative response of serum glucose concentrations and com- parison was made with the results of subcutaneous experiments.Results:There was a statistically sig- nificant 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 in- sulin efficacy in the absence of co-administration adjuvants was very low relative to subcutaneous ad- ministration of insulin.When co-administered buccally with SDCh, SLS, lecithin