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胰岛素肺部给药: 各种吸收促进剂对胰岛素经肺吸收的促进作用

沈赞聪, 程驿, 张强*, 魏树礼, 王夔   

  1. 北京医科大学药学院, 北京 100083
  • 收稿日期:1999-03-18 修回日期:1999-06-02 出版日期:2000-03-15 发布日期:2000-03-15
  • 通讯作者: 张强*

Pulmonary Delivery of Insulin: Absorption Enhancement of Insulin by Various Absorption Promoters in Rats

Shen Zancong, Cheng Yi, Zhang Qiang*, Wei Shun, Wang Kui   

  1. School of Pharmaceutical Sciences, Beijing Medical University, Beijing 100083
  • Received:1999-03-18 Revised:1999-06-02 Online:2000-03-15 Published:2000-03-15
  • Contact: Zhang Qiang*

摘要:

通过肺部导入胰岛素溶液的方法研究各种吸收剂对胰岛素肺部吸收的影响, 以血糖的下降程度为吸收评价指标(PA%)。研究发现, 20 mmol·L-1胆酸钠(PA% = 69.1%), 1%辛酸钠PA% =40.4%), 1%苄泽35 (PA% = 46.6%),1%苄泽78(PA%=53.6%)以及稀土化合物氯化钆[PA%=32.2%,(0.04 mg·kg-1)PA% = 36.3%, 0.2 mg·kg-1)]等能显著增强胰岛素对大鼠血糖的下降作用, 1% EDTA (PA% = 19.1%), 5%油酸(PA% = 20.8%)和稀土化合物氯化镥(PA% = 25.1%, 0.2 mg·kg-1) 无明显的吸收促进作用。结果表明, 选用合适的吸收促进剂有利于胰岛素的肺部吸收。

关键词: 胰岛素, 肺部给药, 低血糖效应, 吸收促进剂, 大鼠

Abstract:

The effects of absorption promoters on the pulmonary absorption of insulin were examined by intratracheal administration of insulin solution in rats. The absorption of insulin from the lung was evaluated by its pharmacological bioavailability (PA%). Results revealed that the coadministration of insulin with 20 mmol·L-1 sodium cholate (PA% = 69.1%), 1% sodium caprilate (PA% = 40.4%), 1% Brij 35 (PA% = 46.6%). 1% Brij 78 (PA% = 53.6%) or GdCl3(PA% = 32.2% at 0.04 mg.kg-1 and 36.3% at 0.2 mg·kg-1) (lanthanide compound) induced a significantly greater decline in blood glucose levels, while coadministration of insulin with adjunvants such as 1% EDIA (PA% = 19.1%), 5% oleic acid (PA% = 20.8%) or LuCl3 (PA% = 25.1%,at 0.2 mg.kg-1) (lanthanide compound) appeared to have no enhancement effect. These observations indicated that the use of proper absorption promoters would be useful for improving the pulmonary absorption of insulin.

Key words: Insulin, Insulin, Intratracheal administration, Intratracheal administration, Hypoglycemic effect, Hypoglycemic effect, Absorption promoters, Absorption promoters, Rat, Rat

Supporting: *Tel: 010-62091717; fax: 010-62015584; e-mail: zqdodo@bjmu.edu.cn