Saffran M, Franco-Saenz R, Kong A, Papahadjopoulos D, Szoka F
Can J Biochem. 1979 Jun;57(6):548-53. doi: 10.1139/o79-069.
The intragastric administration of lysine vasopressin (LVP) to rats is used as a model to study the biological activity of orally administered peptide hormones. Using a modification of the antidiuretic assay of Sawyer, LVP given by stomach tube caused a significant antidiuresis that was dose dependent in doses of 300 to 2000 mU. The simultaneous administration of the protease inhibitor, Trasylol, increased the antidiuretic effect of LVP. The synthetic peptide (1-deamino, 4 valine)-8-D-arginine-vasopressin also caused a dose-dependent prolonged and significant antidiuresis. No pressor effect was observed after intragastric administration of LVP in doses up to 40 U/rat. We are now using this model to test other procedures for enhancing the activity of lysine vasopressin administered in the gastrointestinal tract such as encapsulation into liposomes. The information gained with vasopressin will then be applied to insulin with the ultimate goal of making oral administration practical.
给大鼠胃内注射赖氨酸加压素（LVP）作为研究口服肽类激素生物活性的模型。采用索耶抗利尿试验的改良方法，经胃管给予LVP可引起显著的抗利尿作用，在300至2000 mU剂量范围内呈剂量依赖性。同时给予蛋白酶抑制剂抑肽酶可增强LVP的抗利尿作用。合成肽（1-脱氨基，4-缬氨酸）-8-D-精氨酸加压素也引起剂量依赖性的持久且显著的抗利尿作用。胃内给予高达40 U/大鼠剂量的LVP后未观察到升压作用。我们现在正使用该模型测试其他增强胃肠道给予赖氨酸加压素活性的方法，如包封于脂质体中。然后将从加压素获得的信息应用于胰岛素，最终目标是使口服给药切实可行。
