Ullmann U, Metzner J, Schulz C, Perkins J, Leuenberger B
R&D Human Nutrition & Health, DSM Nutritional Products Ltd., Kaiseraugst, Switzerland.
J Med Food. 2005 Fall;8(3):397-9. doi: 10.1089/jmf.2005.8.397.
Commercial Coenzyme Q10 (CoQ10, ubiquinone) formulations are often of poor intestinal absorption. We investigated the bioavailability of DSM Nutritional Products Ltd. (Kaiseraugst, Switzerland) CoQ10 10% TG/P (all-Q), a new tablet-grade formulation, with CoQ10 Q-Gel Softsules based on the Bio-Solv technology (Tishcon Corp., Salisbury, MD; marketed by Epic4Health, Smithtown, NY) and Q-SorB (Nature's Bounty, Bohemia, NY). Twelve healthy male subjects participated in a randomized, three-period crossover bioequivalence study. Plasma CoQ10 was determined from pre-dose until +36 hours. To compare bioavailability, corrected maximum concentration (Cmax) and area under the curve from 0 to +14 hours [AUC(0-14 h)] were assessed and tested for bioequivalence. The bioequivalence ranges of 0.8-1.25 hour x microg/mL for AUC(0-14 h) and 0.75-1.33 microg/mL for Cmax were applied. In summary, the kinetic profiles of all CoQ10 preparations revealed a one-peak plasma concentration-time course. Highest Cmax values were seen after Q-Gel application, whereas time to Cmax was nearly identical across all treatments. The AUC(0-14 h) values were highest for Q-Gel, narrowly followed by all-Q. The tests for bioequivalence showed a bioequivalence between Q-Gel and all-Q, and both preparations were found to have better bioavailability properties than Q-SorB. Although all-Q and Q-Gel have equivalent bioavailability properties, all-Q can be directly used in tablets, while this is not the case for Q-Gel or other similar forms.
市售的辅酶Q10制剂在肠道的吸收往往较差。我们研究了帝斯曼营养产品有限公司(瑞士凯瑟劳斯特)生产的新型片剂级辅酶Q10制剂CoQ10 10% TG/P(全Q)的生物利用度,并与基于Bio-Solv技术的辅酶Q10 Q-Gel软胶囊(美国马里兰州索尔兹伯里的Tishcon公司;由纽约史密斯敦的Epic4Health销售)以及Q-SorB(纽约波希米亚的自然之宝公司)进行了比较。12名健康男性受试者参与了一项随机、三周期交叉生物等效性研究。测定了给药前至给药后36小时的血浆辅酶Q10水平。为比较生物利用度,评估了校正后的最大浓度(Cmax)以及给药后0至14小时的曲线下面积[AUC(0 - 14 h)],并进行生物等效性测试。应用的生物等效性范围为:AUC(0 - 14 h)为0.8 - 1.25小时×微克/毫升,Cmax为0.75 - 1.33微克/毫升。总之,所有辅酶Q10制剂的动力学曲线均显示为单峰血浆浓度 - 时间过程。服用Q-Gel后Cmax值最高,而所有治疗的达峰时间几乎相同。Q-Gel的AUC(0 - 14 h)值最高,全Q紧随其后。生物等效性测试表明Q-Gel与全Q具有生物等效性,并且发现这两种制剂的生物利用度均优于Q-SorB。尽管全Q和Q-Gel具有等效的生物利用度,但全Q可直接用于片剂,而Q-Gel或其他类似剂型则不然。