Mishima M, Wakita Y, Nakano M
Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
J Pharmacobiodyn. 1987 Nov;10(11):624-31. doi: 10.1248/bpb1978.10.624.
We investigated the promoting effect of medium chain fatty acid salts such as sodium caprylate, sodium caprate (Na C10) and sodium laurate on rat nasal absorption of insulin. Further, we studied the possible mechanism of the absorption promoting effect by fatty acid salts in terms of hemolytic activity, osmotic pressure, chelating effect and inhibition of leucine aminopeptidase activity. Na C10 exhibited the strongest absorption promoting effect on insulin among these fatty acid salts. The promoting effect of Na C10 was very rapid reaching the maximum immunoreactive insulin level within 5 min and its optimum concentration was about 1%. The amount of insulin absorbed after a nasal administration with Na C10 was about 98% of one half subcutaneous dose. The absorption promoting effect of fatty acid salts on insulin was at least in part associated with the chelating ability for calcium ions and the inhibitory action on leucine aminopeptidase activity.
我们研究了中链脂肪酸盐（如辛酸钠、癸酸钠（Na C10）和月桂酸钠）对大鼠鼻腔吸收胰岛素的促进作用。此外，我们从溶血活性、渗透压、螯合作用和亮氨酸氨肽酶活性抑制方面研究了脂肪酸盐吸收促进作用的可能机制。在这些脂肪酸盐中，Na C10对胰岛素表现出最强的吸收促进作用。Na C10的促进作用非常迅速，在5分钟内达到最大免疫反应性胰岛素水平，其最佳浓度约为1%。用Na C10鼻腔给药后吸收的胰岛素量约为皮下半剂量的98%。脂肪酸盐对胰岛素的吸收促进作用至少部分与对钙离子的螯合能力和对亮氨酸氨肽酶活性的抑制作用有关。
