Nasal Insulin Delivery in Rabbits Using Soybean-Derived Sterylglucoside and Sterol Mixtures as Novel Enhancers in Suspension Dosage Forms

概要

論文の詳細を見る
The effect of a soybean-derived sterol mixture (SS) and a steryl glucoside mixture (SG) as enhancers of the nasal absorption of insulin in rabbits was investigated. SS consists of β-sitosterol (Sit), campesterol (Camp), stigmasterol (Stig) and brassicaterol (Bras), and SG is a mixture of their monoglucosides. For each component of SS tested for efficacy in promoting the systemic absorption of nasally administered insulin, the following order was observed : Sit≩Camp>Stig. This finding was in agreement with the order of the enhancers' lipophilicity. In the case of SG, the effect of β-sitosterol β-D-glucoside (Sit-G) was significantly greater than that of SG. The pharmacological bioavailability was 6.7% for SG and 11.3% for Sit-G in the suspension dosage forms SG showed a greater degree of enhacment of insulin permeation through the nasal mucosa than SS. To elucidate the contribution of SG to the enhanced absorption, inslin permeation through an artificial membrane and the nasal mucosa was investigated in vitro, and the results were compared with those for SS. The findings suggest that SG and SS have some effect on nasal mucosa lipids.
公益社団法人日本薬学会の論文
1998-08-15