Promotion of Nasal Absorption of Insulin by Glycyrrhetinic Acid Derivatives. I

概要

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Nasal absorption of insulin in rats was enhanced by addition of sodium glycyrrhetinate (GA Na), dipotassium glycyrrhizinate (GZ K_2), and carbenoxolone (glycyrrhetinic acid hydrogen succinate) disodium salt (GAHS Na_2). The latter agent was the most effective. On addition of 1% GAHS Na_2,plasma immunoreactive insulin levels in rats showed a maximum level of 0.75 mU/ml at 15 min and plasma glucose levels were decreased to about 25 mg/dl after nasal administration of 10 U/kg insulin. In a comparison of the absorption rates of insulin by nasal and intravenous (i.v.) routes in rats, nasal absorptions of 10 U/kg insulin in the presence of 1% GAHS Na_2,0.5% GA Na and 1% GZ K_2 were 26.5%, 13.2% and 14.5% of that in the case of a 5 U/kg i.v. dose, respectively. Hemolytic activies of GAHS Na_2,GA Na and GZ K_2 were milder than those of Na caprate and Na laurate, and nasal leucine aminopeptidase activity was more strongly inhibited by GAHS Na_2 than by medium chain fatty acid salts, sodium glycocholate, GA Na or GZ K_2. Therefore, it is suggested that GAHS Na_2 is a very useful promoter which dose not irritate the nasal mucosal membrane or degrade insulin.
公益社団法人日本薬学会の論文
1989-09-01