Pillion D J, Atchison J A, Wang R X, Meezan E
Department of Pharmacology, University of Alabama at Birmingham.
J Pharmacol Exp Ther. 1994 Dec;271(3):1274-80.
A series of alkylglycosides with various alkyl chain lengths and carbohydrate residues were tested for their ability to enhance systemic absorption of insulin after topical ocular delivery in anesthetized rats. Several reagents, including tetradecyl-, tridecyl- and dodecylmaltoside and dodecylsucrose, were potent stimulators of insulin absorption when used at concentrations as low as 0.125%. Other alkylglycosides such as decylsucrose, decylmaltoside, nonylglucoside, octylmaltoside, heptylglucoside and hexylglucoside were less potent or ineffective as absorption-enhancing reagents. By comparison, the bile salt sodium glycocholate was effective only when used at concentrations of 0.5% or greater. All of the reagents were effective only when used at concentrations above their critical micelle concentration and the most hydrophobic alkylglycoside reagents were the most efficacious at promoting systemic insulin absorption. The possible utilization of eyedrops containing insulin plus an absorption-enhancing alkylglycoside reagent in humans is discussed.
测试了一系列具有不同烷基链长度和碳水化合物残基的烷基糖苷在麻醉大鼠局部眼部给药后增强胰岛素全身吸收的能力。几种试剂，包括十四烷基、十三烷基和十二烷基麦芽糖苷以及十二烷基蔗糖，在低至0.125%的浓度下使用时是胰岛素吸收的有效刺激剂。其他烷基糖苷，如癸基蔗糖、癸基麦芽糖苷、壬基葡糖苷、辛基麦芽糖苷、庚基葡糖苷和己基葡糖苷，作为吸收增强试剂的效力较低或无效。相比之下，胆盐甘氨胆酸钠仅在浓度为0.5%或更高时才有效。所有试剂仅在高于其临界胶束浓度的浓度下才有效，并且最疏水的烷基糖苷试剂在促进胰岛素全身吸收方面最有效。讨论了含有胰岛素加吸收增强烷基糖苷试剂的眼药水在人类中的可能应用。
