Di Renzo Laura, Smeriglio Antonella, Ingegneri Mariarosaria, Gualtieri Paola, Trombetta Domenico
Section of Clinical Nutrition and Nutrigenomic, Department of Biomedicine and Prevention, University of Tor Vergata, Via Montpellier 1, 00133 Rome, Italy.
Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Ferdinando Stagno d'Alcontres 31, 98166 Messina, Italy.
Pharmaceutics. 2023 Feb 23;15(3):743. doi: 10.3390/pharmaceutics15030743.
Current evidence supports the use of extra virgin olive oil (EVOO) and its minor components such as hydroxytyrosol or 3,4-dihydroxyphenyl ethanol (DOPET), to improve cardiovascular and metabolic health. Nevertheless, more intervention studies in humans are needed because some gaps remain in its bioavailability and metabolism. The aim of this study was to investigate the DOPET pharmacokinetics on 20 healthy volunteers by administering a hard enteric-coated capsule containing 7.5 mg of bioactive compound conveyed in EVOO. The treatment was preceded by a washout period with a polyphenol and an alcohol-free diet. Blood and urine samples were collected at baseline and different time points, and free DOPET and metabolites, as well as sulfo- and glucuro-conjugates, were quantified by LC-DAD-ESI-MS/MS analysis. The plasma concentration versus time profiles of free DOPET was analyzed by a non-compartmental approach, and several pharmacokinetic parameters (C, T, T, AUC, AUC, AUC AUC, C and K) were calculated. Results showed that DOPET C (5.5 ng/mL) was reached after 123 min (T), with a T of 150.53 min. Comparing the data obtained with the literature, the bioavailability of this bioactive compound is about 2.5 times higher, confirming the hypothesis that the pharmaceutical formulation plays a pivotal role in the bioavailability and pharmacokinetics of hydroxytyrosol.
目前的证据支持使用特级初榨橄榄油（EVOO）及其微量成分，如羟基酪醇或3,4-二羟基苯乙醇（DOPET），以改善心血管和代谢健康。然而，由于其生物利用度和代谢方面仍存在一些差距，因此需要在人体中进行更多的干预研究。本研究的目的是通过给20名健康志愿者服用一粒硬肠溶胶囊，其中含有7.5毫克以EVOO输送 的生物活性化合物，来研究DOPET的药代动力学。在治疗前有一个采用不含多酚和酒精饮食的洗脱期。在基线和不同时间点采集血液和尿液样本，并通过LC-DAD-ESI-MS/MS分析对游离DOPET及其代谢物以及磺基和葡糖醛酸共轭物进行定量。通过非房室方法分析游离DOPET的血浆浓度-时间曲线，并计算几个药代动力学参数（Cmax、Tmax、T1/2、AUC(0-t)、AUC(0-inf)、AUC(0-t)/AUC(0-inf)、CL和Ke）。结果显示，123分钟（Tmax）后达到DOPET Cmax（5.5纳克/毫升），T1/2为150.53分钟。将获得的数据与文献数据进行比较，这种生物活性化合物的生物利用度高出约2.5倍，证实了药物制剂在羟基酪醇的生物利用度和药代动力学中起关键作用这一假设。
