Holm R, Müllertz A, Pedersen G P, Kristensen H G
Department of Pharmaceutics, Royal Danish School of Pharmacy, Copenhagen.
Pharm Res. 2001 Sep;18(9):1299-304. doi: 10.1023/a:1013037927882.
To compare the influence of the degree of fatty acid unsaturation (oleic [C18:], linoleic [C18:2], or linolenic acid [C18:3]), with the intestinal lymphatic transport of halofantrine free base from disperse systems in anesthetized rats.
The mesenteric lymph duct was cannulated in anesthetized rats. Lipid vehicle containing halofantrine was administered by intraduodenal infusion. The concentration of halofantrine in blood and lymph samples was analyzed.
The rank order of the lymphatic transport of halofantrine was C18:2 > C18:1 > C18:3. Comparison of the area under the curve (AUC) from the three fatty acids showed no statistically significant differences between the AUCs from the lymph cannulated rats. In terms of rank order effects, the plasma concentrations of halofantrine were highest for the rats dosed C18:2 followed by C18:3 and C18:1.
Using C18:2 as a vehicle increased the lymphatic transport of halofantrine 16.6-fold over that observed for the system containing C18:3. The extent of lymphatic transport for the C18:1 system did not differ from the other two formulations, but the combined lymph and plasma data indicated that the C18:2 was the most suitable lipid vehicle for the oral delivery of halofantrine.
比较脂肪酸不饱和度程度（油酸[C18:1]、亚油酸[C18:2]或亚麻酸[C18:3]）对麻醉大鼠分散系统中卤泛群游离碱肠道淋巴转运的影响。
在麻醉大鼠中插入肠系膜淋巴管。通过十二指肠内输注给予含卤泛群的脂质载体。分析血液和淋巴样本中卤泛群的浓度。
卤泛群淋巴转运的顺序为C18:2 > C18:1 > C18:3。三种脂肪酸曲线下面积（AUC）的比较显示，插管大鼠淋巴的AUC之间无统计学显著差异。就排序效应而言，给予C18:2的大鼠血浆中卤泛群浓度最高，其次是C18:3和C18:1。
以C18:2作为载体时，卤泛群的淋巴转运比含C18:3的系统高16.6倍。C18:1系统的淋巴转运程度与其他两种制剂无差异，但淋巴和血浆综合数据表明，C18:2是口服卤泛群最合适的脂质载体。
