Pronova Biopharma Norge AS, part of BASF, P.O. Box 420, NO-1327, Lysaker, Norway.
BASF Corporation, 100 Park Ave, Florham Park, NJ, 07932, USA.
Lipids Health Dis. 2017 Oct 16;16(1):204. doi: 10.1186/s12944-017-0589-0.
Absorption of EPA and DHA from Omega-3-acid ethyl ester (EE) concentrate supplements occurs most efficiently when taken in context of a fatty meal; adequate fat intake is required to release bile salts that emulsify and pancreatic enzymes that digest omega-3-containing lipids in the intestine. Current guidelines recommend reduction in fat intake and therefore there is a need to optimize the absorption of Omega-3 in those consuming low-fat or no-fat meals. To this end, BASF has developed an Absorption Acceleration Technology, a novel self-micro-emulsifying delivery system (SMEDS) formulation of highly concentrated Omega-3-acid EE which enables rapid emulsification and microdroplet formation upon entering the aqueous environment of the gut therefore enhances the absorption.
Two separate single dose, crossover studies were conducted to determine the relative bioavailability of omega-3-acid EE concentrate, either as a novel SMEDS formulation (PRF-021) or as control, in healthy fasted male and female adults at two dose levels (Study 1 "low dose": 630 mg EPA + DHA in PRF-021 vs. 840 mg EPA + DHA in control; Study 2 "high dose": 1680 mg EPA + DHA in PRF-021 vs. 3360 mg EPA + DHA in control). Blood samples were collected immediately before supplementation and at defined time intervals for 48 h. Plasma concentration of total EPA and DHA were determined for pharmacokinetic analysis, area under the curve (AUC) and maximum observed concentration (C) was determined.
Total EPA plus DHA absorption from SMEDS formulation PRF-021 were 6.4 and 11.5 times higher compared to control in low- and high-dose studies respectively, determined as the ratio of baseline corrected, dose normalized AUC of PRF-021 over that of control. EPA and DHA individually showed differing levels of enhancement: the AUC ratio for EPA was 23.8 and 25.7 in low and high dose studies, respectively, and the AUC ratio for DHA was 3.6 and 5.6 in low and high dose studies, respectively. C was also increased for both EPA and DHA 2.7- to 9.2-fold.
PRF-021 is a novel SMEDS formulation of Omega-3-acid EE demonstrating a marked improvement in absorption of a single dose of EPA and DHA EE under fasted conditions. This allows adequate absorption of Omega-3 from the supplement without the requirement of a high-fat meal.
当与高脂肪餐一起服用时，从欧米伽 3 酸乙酯（EE）浓缩物补充剂中吸收 EPA 和 DHA 的效率最高；需要足够的脂肪摄入来释放胆汁盐，胆汁盐乳化并消化肠道中含有的 omega-3 脂肪的胰腺酶。目前的指南建议减少脂肪摄入，因此需要优化那些食用低脂肪或无脂肪膳食的人的 Omega-3 吸收。为此，巴斯夫开发了一种吸收加速技术，这是一种新型的自微乳化药物传递系统（SMEDS）配方，可高度浓缩的欧米伽 3 酸 EE，在进入肠道的水性环境后可迅速乳化和形成微滴，从而增强吸收。
在两个单独的单剂量交叉研究中，确定了新型 SMEDS 配方（PRF-021）或对照品中欧米伽 3 酸 EE 浓缩物的相对生物利用度，在健康的禁食男性和女性成年人中，以两种剂量水平（研究 1“低剂量”：PRF-021 中的 630mg EPA+DHA 与对照品中的 840mg EPA+DHA；研究 2“高剂量”：PRF-021 中的 1680mg EPA+DHA 与对照品中的 3360mg EPA+DHA）。在补充前和 48 小时内的特定时间间隔采集血样。进行药代动力学分析，以确定总 EPA 和 DHA 的血浆浓度，确定曲线下面积（AUC）和最大观察浓度（C）。
与对照品相比，低剂量和高剂量研究中 SMEDS 配方 PRF-021 中的总 EPA+DHA 吸收分别高 6.4 倍和 11.5 倍，这是通过基线校正，PRF-021 归一化 AUC 与对照品的 AUC 之比确定的。EPA 和 DHA 分别表现出不同程度的增强：低剂量和高剂量研究中 EPA 的 AUC 比分别为 23.8 和 25.7，DHA 的 AUC 比分别为 3.6 和 5.6。C 也分别增加了 2.7-9.2 倍。
PRF-021 是一种新型的 SMEDS 配方的欧米伽 3 酸 EE，在空腹条件下，单一剂量的 EPA 和 DHA EE 的吸收得到了显著改善。这使得从补充剂中吸收足够的 Omega-3 成为可能，而无需高脂肪餐。
