Ichihashi T, Kinoshita H, Takagishi Y, Yamada H
Shionogi Research Laboratories, Shionogi & Co. Ltd, Osaka, Japan.
J Pharm Pharmacol. 1992 Jul;44(7):560-4. doi: 10.1111/j.2042-7158.1992.tb05464.x.
[14C]Mepitiostane in various vehicles was administered to the small intestine of anaesthetized rats with cannulated thoracic ducts, and the effect of lipids on lymphatic absorption was examined. The extent of lymphatic absorption was greatest when administered in triolein and sesame oil, which are triglycerides of long-chain fatty acids. Absorption in the presence of other vehicles was in the order of 10% Tween 80 aqueous solution greater than monolein greater than oleic acid approximately oleic acid/monolein (2:1 mol/mol) greater than aqueous suspension. Differences between the extents of lymphatic absorption of mepitiostane in the various formulations were not due to variation in the lymph flow but to the increased secretion of chylomicron and very low density lipoproteins. During absorption of mepitiostane from the small intestine, oil affected not only the penetration into epithelium cells and the metabolism in them, but also the partition between blood and lymph.
将[14C]美替奥斯坦以不同载体形式给予胸导管插管的麻醉大鼠小肠，研究脂质对淋巴吸收的影响。当以三油酸甘油酯和芝麻油（长链脂肪酸的甘油三酯）为载体给药时，淋巴吸收程度最大。在其他载体存在下的吸收顺序为：10%吐温80水溶液大于单油酸甘油酯大于油酸约等于油酸/单油酸甘油酯（2:1摩尔/摩尔）大于水混悬液。不同制剂中美替奥斯坦淋巴吸收程度的差异并非由于淋巴流量的变化，而是由于乳糜微粒和极低密度脂蛋白分泌增加。在美替奥斯坦从小肠吸收过程中，油不仅影响其进入上皮细胞和在细胞内的代谢，还影响其在血液和淋巴之间的分配。
