Collectively, tocopherols and tocotrienols are known as tocochromanols, a lipid‐soluble group of chemicals that make up the vitamin E family of compounds. There are four primary tocopherols (α‐tocopherol, β‐tocopherol, γ‐tocopherol, and δ‐tocopherol) and four primary tocotrienols (α‐tocotrienol, β‐tocotrienol, γ‐tocotrienol, δ‐tocotrienol). To date, tocotrienols have received less attention for their effects on mammalian health compared to their counterparts, tocopherols. Yet, δ‐tocotrienols (DT3) have shown efficacy in pre‐clinical anti‐cancer research. The purpose of this study was to investigate the pharmacokinetics and bioavailability of a powdered, sublingual form of DT3, in healthy men and women. We hypothesized that there would a steady increase in plasma DT3 followed by a decrease after reaching peak concentrations over an 8‐hour period. Volunteers (m=4, f=1, 30 +/‐ 4 years, 175 +/‐ 4 cm, 83.4 +/‐ 7.4 kg) were administered 80mg of DT3 powder in a fasted state. Volunteers were asked to keep the powder under their tongues until it was fully dissolved in two separate doses of 40mg given consecutively. Blood samples were taken at 0, 60, 90, 120, 180, 240, 300, 360, 420, and 480 minutes. Volunteers were given a meal consisting of carbohydrates, proteins, and fats after four hours. Blood samples collected were placed in a centrifuge to separate blood from plasma. Plasma was collected and stored in a ‐80° freezer. DT3 concentrations were calculated from plasma using protein precipitation followed by liquid‐liquid extraction. Analytes were separated by HPLC with the extracts assayed against a calibration curve. DT3 bioavailability was assessed using the parameters peak plasma concentration (Cmax), time to reach peak plasma concentration (Tmax) and total area under the plasma concentration‐time curve (AUC). Plasma concentration of DT3 reached 110.2 ng/ml (Cmax) 420 minutes after administration (Tmax). DT3 concentration decreased between 420 and 480 minutes. The 0‐8 h AUC reached 27,165.8 ng/ml*min. DT3 appears to exhibit a progressive, near linear upward absorption profile over the course of 7 hours, after which there is a decrease in plasma DT3.
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