Comparison of the effects of various absorption enhancers and enzyme inhibitors on buccal insulin delivery in vitro and in vivo
- VernacularTitle: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
- Author:
Tianzhi YANG
- Publication Type:Journal Article
- From:
Journal of Peking University(Health Sciences)
2001;33(3):238-242
- CountryChina
- Language:Chinese
-
Abstract:
Objective: To study the effects of variou s absorption enhancers and enzyme inhibitors on in sulin permeation in vitro and in vivo . Methods: The pene tration of insulin throu gh hamster and rabbit buccal membrane was investigated by measuring in vitro transbuccal flux. Buccal insulin absorption was estimated in vivo from th e cumula tive response of serum glucose concentrations and comparison was made with the results of subcutaneous experiments. Results: There was a statistically significant permeabil ity increas e of insulin over controls after co-administration with the SDCh, Brij78, SLS or lecithin, aprotinin, bacitracin, whereas 1-menthol or poloxamer were less e ffective. Buccal insulin efficacy in the absence of co-administration adjuvants was very low relative t o subcutaneous administration of insulin. When co-administered buccally with SD Ch, SLS, l ecithin or Brij78, Fr (relative pharmacological bioavailability) values were al l 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 re sults with respect to the enhancement of these adjuvants.
