[氮酮辅助胰岛素鼻腔吸收的功能与病理学研究]

[Functional and pathological study of intranasal absorption of insulin aided by azone].

作者信息

Hou Tiening, Xin Weihong, Dong Zhen

机构信息

Department of Otorhinolaryngology Head and Neck Surgery, Affiliated SIR RUN RUN SHAW Hospital, Zhejiang University, Hangzhou 310016, China.

出版信息

Zhonghua Er Bi Yan Hou Ke Za Zhi. 2002 Aug;37(4):271-3.

PMID:12772412

Abstract

OBJECTIVE

To distinguish the different permeation function between sodium glycocholic acid (SGC) and Azone, and study the pathological changes induced by Azone on nasal mucosa.

METHODS

Insulin was given intravenouslly at the dose of 4.0 U. The blood samples were determined by radioimmunity method. SGC or Azone was administered respectively via nasal route with Insulin 270 U/ml. Insulin nasal drops 10 microL were given to each of rabbits via nasal route. The Azone 50 microL was administered via nasal route, t.i.d., lasted for 1 week and 3 months.

RESULTS

The level of blood Insulin was as follows: (3,954.47 +/- 644.47) mU/L, AUC = (1,264.87 +/- 148.00) mU.L-1.min-1 x 10(-3) in i.v. group; (740.44 +/- 94.16) mU/L, AUC = (298.02 +/- 63) mU.L-1.min-1 x 10(-3) in SGC group; (908.18 +/- 201.19) mU/L, AUC = (596.92 +/- 84.00) mU.L-1.min-1 x 10(-3) in Azone group. The bioavailability was 23.56% and 47.19% respectively. The pathological changes included cilia detachment from epithelium, glandular hypertrophy and connective tissue proliferation.

CONCLUSION

It was found that Azone was an excellent permeation enhance which promoted more Insulin to be absorbed into blood stream through nasal mucosa. However, Azone also damaged the nasal mucosa in the view of pathology.

摘要

目的

区分甘氨胆酸钠（SGC）和氮酮的不同渗透功能，并研究氮酮对鼻黏膜引起的病理变化。

方法

静脉注射胰岛素，剂量为4.0 U。采用放射免疫法测定血样。分别将SGC或氮酮与270 U/ml胰岛素经鼻给药。给每只兔经鼻滴入10 μl胰岛素滴鼻剂。经鼻给予50 μl氮酮，每日3次，持续1周和3个月。

结果

静脉注射组血胰岛素水平为：（3954.47±644.47）mU/L，AUC =（1264.87±148.00）mU·L⁻¹·min⁻¹×10⁻³；SGC组为（740.44±94.16）mU/L，AUC =（298.02±63）mU·L⁻¹·min⁻¹×10⁻³；氮酮组为（908.18±201.19）mU/L，AUC =（596.92±84.00）mU·L⁻¹·min⁻¹×10⁻³。生物利用度分别为23.56%和47.19%。病理变化包括纤毛从上皮脱落、腺体肥大和结缔组织增生。