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Single-Dose Pharmacokinetic Study of Lycopene Delivered in a Well-Defined Food-Based Lycopene Delivery System (Tomato Paste-Oil Mixture) in Healthy Adult Male Subjects

¹ Division of Hematology-Oncology, Department of Medicine, University of Chicago, Chicago, Illinois; ² Department of Pharmacy Practice, College of Pharmacy, ³ Department of Human Nutrition, ⁴ Departments of Ophthalmology and Visual Sciences, and ⁵ Division of Hematology-Oncology, Department of Medicine, University of Illinois at Chicago, Chicago, Illinois; ⁶ Division of Hematology-Oncology, Department of Medicine, Vanderbilt University, Nashville, Tennessee; and ⁷ Division of Cancer Prevention, National Cancer Institute, Rockville, Maryland

Requests for reprints: Keith A. Rodvold, m/c 886, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Room #164, Chicago, IL 60612. Phone: (312) 996-3341; Fax: (312) 413-1797. E-mail: kar{at}uic.edu

This report details the findings of a single-dose Phase I pharmacokinetic and toxicity study of a food-based formulation of lycopene in healthy adult male subjects. Five dosing groups (n = 5 per group) were sequentially treated with increasing doses of lycopene ranging from 10 to 120 mg. Blood samples were collected for a total of 28 days (672 h) after administration of single doses of lycopene. The mean time (t_max) to reach maximum total lycopene concentration (C_max) ranged from 15.6 to 32.6 h. The C_max for total lycopene ranged between 4.03 and 11.27 µg/dl (0.075–0.210 µM). Mean AUC_0–96 and elimination half-life for total lycopene ranged from 214 to 655 µg h/dl (3.986–12.201 µmol h/l) and 28.1 and 61.6 h, respectively. The changes observed in lycopene exposure parameters (e.g., C_max and AUC_0–96) were not proportional to increments in dose, with larger increases observed at the lowest end of the dosing range (10–30 mg). Chylomicron lycopene was measured during the first 12 h with the differences observed among the dosing groups not reaching statistical significance. These findings may reflect a process of absorption that is saturable at very low dosing levels or may be explained by the large interindividual variability in attained lycopene concentrations that were observed within each dosing group. Pharmacokinetic parameters for trans- and cis-lycopene isomers were calculated and are reported here. The formulation was well tolerated with minimal side effects, which were mainly of gastrointestinal nature and of very low grade.

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