Department of Pharmacokinetics, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto, 607-8412, Japan.
J Mater Sci Mater Med. 2010 Feb;21(2):835-41. doi: 10.1007/s10856-009-3923-x. Epub 2009 Nov 14.
Two kinds of insulin were loaded into self-dissolving micropile array tip (following tip). Fully-loaded tip (f-tip) and partially-loaded tip (p-tip) were prepared using chondroitin sulfate for the percutaneous administration of insulin. One hundred micropiles were constructed on a 1.0 x 1.0 cm tip. The mean length of the micropile in a tip were 483.4 +/- 4.7 mum for the f-tip and 492.6 +/- 2.4 mum for the p-tip. The insulin content of the p-tip was 28.5% of that of the f-tip. The pharmacological efficiency of insulin loaded tip was evaluated in rat experiments by measuring their hypoglycemic effects. The maximum hypoglycemic effect of insulin was observed at 1.7 +/- 0.2 h for the f-tip and 1.5 +/- 0.2 h for the p-tip. Good dose-dependency was observed for the plasma glucose level vs. time curves. These results suggest the usefulness of p-tip as a percutaneous DDS of insulin.
两种胰岛素被载入自溶解微针阵列尖端（以下简称尖端）。使用硫酸软骨素制备了完全载入尖端（f-tip）和部分载入尖端（p-tip），用于经皮给予胰岛素。在 1.0 x 1.0 cm 的尖端上构建了 100 个微针。f-tip 中每个尖端的微针平均长度为 483.4 +/- 4.7 mum，p-tip 为 492.6 +/- 2.4 mum。p-tip 中的胰岛素含量为 f-tip 的 28.5%。通过测量其降血糖作用，在大鼠实验中评估了载入胰岛素的尖端的药效学效率。f-tip 的最大降血糖作用在 1.7 +/- 0.2 h 时观察到，p-tip 在 1.5 +/- 0.2 h 时观察到。血糖水平与时间曲线表现出良好的剂量依赖性。这些结果表明 p-tip 作为胰岛素经皮给药系统的有用性。
