The pharmacokinetic profile of crocetin in healthy adult human volunteers after a single oral administration

• Published in: Phytomedicine (Stuttgart) 2011-05, Vol.18 (7), p.575-578
• Main Authors: Umigai, N., Murakami, K., Ulit, M.V., Antonio, L.S., Shirotori, M., Morikawa, H., Nakano, T.
• Format: Article
• Language: English
• Subjects: Administration, Oral; Adult; Antioxidants - administration & dosage; Antioxidants - chemistry; Antioxidants - pharmacokinetics; beta Carotene - blood; beta Carotene - pharmacokinetics; Carboxylic acids; Carotenoid; Carotenoids; Carotenoids - administration & dosage; Carotenoids - blood; Carotenoids - chemistry; Carotenoids - pharmacokinetics; Chromatography, High Pressure Liquid; Crocetin; Dose-Response Relationship, Drug; Female; Gardenia; Gardenia - chemistry; Health aspects; Humans; Lutein - blood; Lutein - pharmacokinetics; Lycopene; Male; Medicine, Traditional; Middle Aged; Pharmacokinetics; Physiological aspects; Plant Extracts - chemistry; Plants, Medicinal - chemistry; Time Factors
• ISSN: 0944-7113; 1618-095X
• DOI: 10.1016/j.phymed.2010.10.019

Crocetin, a unique carotenoid with a short carbon chain length, is an active compound of saffron and Gardenia jasminoides Ellis used as traditional herbal medicine. The present study was undertaken to investigate the pharmacokinetic profiles of crocetin in healthy adult subjects. The study was conducted as an open-label, single dose escalation with 10 Filipino volunteers (5 men and 5 women). The subjects received a single dose of crocetin at three doses (7.5, 15 and 22.5mg) in one week interval. Blood samples were collected from the brachial vein before and at 1, 2, 4, 6, 8, 10 and 24h after administration. Plasma concentrations of crocetin were determined by high-performance liquid chromatography (HPLC). Crocetin was rapidly absorbed and detected within an hour of administration with a mean time to reach maximum concentration (Tmax) of crocetin ranging from 4.0 to 4.8h. The mean values of Cmax and AUC0–24h ranged from 100.9 to 279.7ng/ml and 556.5 to 1720.8ng.h/ml respectively. Cmax and AUC values increased with dose proportional manner. Crocetin was eliminated from human plasma with a mean elimination half life (T1/2) of 6.1 to 7.5h. In summary, there were no serious adverse events up to 22.5mg dose of crocetin while crocetin was found to be absorbed more quickly than the other carotenoids such as β-carotene, lutein and lycopene.