Nagata M, Yotsuyanagi T, Ikeda K
Faculty of Pharmaceutical Sciences, Nagoya City University, Japan.
J Pharm Pharmacol. 1988 Feb;40(2):85-8. doi: 10.1111/j.2042-7158.1988.tb05186.x.
The solubilization of vitamin K1 by bile salts (sodium deoxycholate, sodium cholate and their corresponding glycine conjugates) and phosphatidylcholine (egg)-bile salt mixed micelles has been investigated. The solubilization curves were not always linear with increasing bile salts, but the vitamin was appreciably solubilized in the region below their CMCs. In the bile salt solutions (20 mM, phosphate buffered saline, pH 7.5, ions strength 0.2), the solubilized vitamin ranged from 0.3 to 0.9 mM. With increasing phosphatidylcholine, the amount of vitamin solubilized was dramatically increased; at the molar ratio of 1:1 (both 20 mM), the amount of vitamin solubilized was about 25-30 times more than by the corresponding bile salts alone. There is a possibility that exogenous phospholipid given orally as liposomal forms assists the solubilization of vitamin K1, in the intestine. This characteristic is suggested as being responsible, in part, for the enhanced recovery of blood coagulation after oral administration of liposomal vitamin K1 to warfarin-treated rabbits.
研究了胆盐(脱氧胆酸钠、胆酸钠及其相应的甘氨酸共轭物)和磷脂酰胆碱(鸡蛋)-胆盐混合胶束对维生素K1的增溶作用。增溶曲线并不总是随胆盐增加呈线性,但维生素在其临界胶束浓度以下区域能被显著增溶。在胆盐溶液(20 mM,磷酸盐缓冲盐水,pH 7.5,离子强度0.2)中,增溶的维生素浓度范围为0.3至0.9 mM。随着磷脂酰胆碱含量增加,维生素的增溶量显著增加;在摩尔比为1:1(均为20 mM)时,维生素的增溶量比单独使用相应胆盐时高出约25 - 30倍。口服脂质体形式的外源性磷脂有可能在肠道中协助维生素K1的增溶。这一特性被认为部分是口服脂质体维生素K1给华法林治疗的兔子后凝血恢复增强的原因。