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Enhancement of intestinal absorption of coenzyme Q10 using emulsions containing oleyl polyethylene acetic acids.
European Journal of Pharmaceutical Sciences ( IF 4.3 ) Pub Date : 2019-11-13 , DOI: 10.1016/j.ejps.2019.105144 Yuki Sato 1 , Sayaka Yokoyama 1 , Yoshiaki Yamaki 1 , Yuta Nishimura 1 , Mami Miyashita 1 , Shingo Maruyama 2 , Yoh Takekuma 1 , Mitsuru Sugawara 1
European Journal of Pharmaceutical Sciences ( IF 4.3 ) Pub Date : 2019-11-13 , DOI: 10.1016/j.ejps.2019.105144 Yuki Sato 1 , Sayaka Yokoyama 1 , Yoshiaki Yamaki 1 , Yuta Nishimura 1 , Mami Miyashita 1 , Shingo Maruyama 2 , Yoh Takekuma 1 , Mitsuru Sugawara 1
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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.
中文翻译：
使用含油基聚乙烯乙酸的乳液增强辅酶Q10的肠道吸收。
通常制备乳剂以改善溶解性差的亲脂性化合物的吸收。辅酶Q10（CoQ10）是一种亲脂性化合物，已被用作抗衰老补充剂。我们专注于草酸衍生物油基聚氧乙烯乙酸，以制备CoQ10乳液，并有望应用于口服药物。纯化草酸，并根据环氧乙烷链的平均长度将其分为四类。将使用四个草酸基团制备的乳液给药于大鼠，并分析了CoQ10的血浆浓度分布。与粉末组相比，所有乳液组的CoQ10吸收均得到改善。使用草酸（n = 9.0）的乳液大大提高了辅酶Q10的血浆浓度。与相同的草酸（n = 9.0）相比，通过使用含有更多草酸（6％，15％和23％）的乳剂，吸收也得到了改善。草酸对细胞活力的影响与常规表面活性剂如聚氧乙烯（20）脱水山梨醇单油酸酯（Tween 80）几乎相同。结果表明，草酸可用于制备口服乳剂，使用草酸配方可显着改善草酸对辅酶Q10的吸收。
更新日期：2019-11-13
中文翻译：
使用含油基聚乙烯乙酸的乳液增强辅酶Q10的肠道吸收。
通常制备乳剂以改善溶解性差的亲脂性化合物的吸收。辅酶Q10（CoQ10）是一种亲脂性化合物，已被用作抗衰老补充剂。我们专注于草酸衍生物油基聚氧乙烯乙酸，以制备CoQ10乳液，并有望应用于口服药物。纯化草酸，并根据环氧乙烷链的平均长度将其分为四类。将使用四个草酸基团制备的乳液给药于大鼠，并分析了CoQ10的血浆浓度分布。与粉末组相比，所有乳液组的CoQ10吸收均得到改善。使用草酸（n = 9.0）的乳液大大提高了辅酶Q10的血浆浓度。与相同的草酸（n = 9.0）相比，通过使用含有更多草酸（6％，15％和23％）的乳剂，吸收也得到了改善。草酸对细胞活力的影响与常规表面活性剂如聚氧乙烯（20）脱水山梨醇单油酸酯（Tween 80）几乎相同。结果表明，草酸可用于制备口服乳剂，使用草酸配方可显着改善草酸对辅酶Q10的吸收。
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