Faculty of Pharmaceutical Sciences, Hokkaido University Kita-12-jo, Nishi-6-chome, Kita-ku, Sapporo 060-0812, Japan.
MORESCO Corp. 5-5-3, Minatojimaminamimachi, Chuo-ku, Kobe 650-0047, Japan.
Eur J Pharm Sci. 2020 Jan 15;142:105144. doi: 10.1016/j.ejps.2019.105144. Epub 2019 Nov 13.
Emulsions have often been prepared to improve absorption of lipophilic compounds that have poor solubility. Coenzyme Q10 (CoQ10) is a lipophilic compound that has been used as an anti-aging supplement. We focused on oleyl polyethyleneoxy acetic acid, an oxa acid derivative, to prepare emulsions of CoQ10 with the expectation of application to oral pharmaceutics. Oxa acids were purified and classified into four groups based on the average length of the ethylene oxide chain. The emulsion that were prepared using the four oxa acid groups were administered to rats and the plasma concentration profiles of CoQ10 were analyzed. The absorption of CoQ10 was improved in all emulsion groups compared with that in the powder group. The emulsion using oxa acid (n = 9.0) greatly increased the plasma concentration of CoQ10. Absorption was also improved by using emulsions containing larger percentage of oxa acids (6%, 15% and 23%) to compared with the same oxa acid (n = 9.0). The effects of oxa acids on cell viability were almost the same as those of conventional surfactants such as polyoxyethylene (20) sorbitan monooleate (Tween 80). The results showed that oxa acids are useful to prepare emulsions for oral administration and that the absorption of CoQ10 using oxa acids is significantly improved by using our formulations.
乳液常被用来提高脂溶性化合物的吸收，这些化合物的溶解度较差。辅酶 Q10（CoQ10）是一种脂溶性化合物，已被用作抗衰老补充剂。我们专注于油酰聚氧乙烯乙酸，一种氧杂酸衍生物，来制备 CoQ10 的乳液，期望将其应用于口服药剂学。氧杂酸被纯化并根据乙氧化链的平均长度分为四组。使用这四种氧杂酸组制备的乳液被施用于大鼠，并分析 CoQ10 的血浆浓度曲线。与粉末组相比，所有乳液组中 CoQ10 的吸收都得到了改善。使用氧杂酸（n=9.0）的乳液大大增加了 CoQ10 的血浆浓度。与相同的氧杂酸（n=9.0）相比，使用含有较大百分比氧杂酸（6%、15%和 23%）的乳液也能提高吸收。氧杂酸对细胞活力的影响几乎与传统表面活性剂（如聚氧乙烯（20）山梨聚糖单油酸酯（吐温 80））相同。结果表明，氧杂酸可用于制备口服乳液，并且使用我们的制剂可显著提高 CoQ10 的吸收。
