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不同吸收促进剂和蛋白酶抑制剂对大鼠肺内给药胰岛素吸收的增强作用。

Absorption enhancement of intrapulmonary administered insulin by various absorption enhancers and protease inhibitors in rats.

作者信息

Yamamoto A, Umemori S, Muranishi S

机构信息

Department of Biopharmaceutics, Kyoto Pharmaceutical University, Japan.

出版信息

J Pharm Pharmacol. 1994 Jan;46(1):14-8. doi: 10.1111/j.2042-7158.1994.tb03712.x.

DOI:10.1111/j.2042-7158.1994.tb03712.x
PMID:7515417
Abstract

The effects of absorption enhancers and protease inhibitors on the pulmonary absorption of insulin were examined by means of an in-situ pulmonary absorption experiment. Absorption enhancers used in this study were sodium glycocholate, linoleic acid-surfactant mixed micelles and N-lauryl-beta-D-maltopyranoside whereas aprotinin, bacitracin and soybean trypsin inhibitor were used as protease inhibitors. The absorption of insulin from the lung was evaluated by its hypoglycaemic effect. In the absence of these additives, a slight hypoglycaemic effect was obtained following intrapulmonary administration of insulin. However, we found significant and continuous hypoglycaemic effects after the insulin administration with these additives. N-Lauryl-beta-D-maltopyranoside and bacitracin appeared to be more effective for enhancing the pulmonary absorption of insulin than the other adjuvants. These findings suggest that the use of these two adjuvants would be a useful approach for improving the pulmonary absorption of insulin.

摘要

通过原位肺部吸收实验研究了吸收促进剂和蛋白酶抑制剂对胰岛素肺部吸收的影响。本研究中使用的吸收促进剂为甘氨胆酸钠、亚油酸 - 表面活性剂混合胶束和N - 月桂酰 -β-D - 麦芽糖苷,而抑肽酶、杆菌肽和大豆胰蛋白酶抑制剂用作蛋白酶抑制剂。通过胰岛素的降血糖作用评估其从肺部的吸收。在没有这些添加剂的情况下,肺内给予胰岛素后获得轻微的降血糖作用。然而,我们发现用这些添加剂给予胰岛素后有显著且持续的降血糖作用。N - 月桂酰 -β-D - 麦芽糖苷和杆菌肽在增强胰岛素肺部吸收方面似乎比其他佐剂更有效。这些发现表明,使用这两种佐剂将是改善胰岛素肺部吸收的有用方法。

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