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Pharmacokinetics of caffeine and its metabolites in plasma and urine after consuming a soluble green/roasted coffee blend by healthy subjects

Coffee is widely consumed worldwide; therefore, the methylxanthines contained in coffee, mainly caffeine (CF), are among the most abundant bioactive compounds in our diet. In the present work, the bioavailability and metabolism of methylxanthines in a commercial soluble green/roasted coffee blend wa...

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Published in:Food research international 2014-10, Vol.64, p.125-133
Main Authors: Martínez-López, Sara, Sarriá, Beatriz, Baeza, Gema, Mateos, Raquel, Bravo-Clemente, Laura
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description Coffee is widely consumed worldwide; therefore, the methylxanthines contained in coffee, mainly caffeine (CF), are among the most abundant bioactive compounds in our diet. In the present work, the bioavailability and metabolism of methylxanthines in a commercial soluble green/roasted coffee blend was studied. After a 3-day restriction of methylxanthine-containing foods, fasting healthy subjects (12 men and women) consumed the coffee product containing 70.69mg CF and 0.119mg theobromine (TB). Plasma samples were taken before (t=0h) and after coffee consumption at different time points (0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 9, 10 and 12h). Urine was collected at baseline (−2–0h) and at different intervals (0–2, 2–5, 5–8, 8–12 and 12–24h). Samples were analyzed by HPLC-DAD and LC–MS-QToF, and pharmacokinetic parameters were calculated. CF was the main methylxanthine found in plasma (Cmax=10.50μM, Tmax=1.2h). In addition, seven methylxanthines and methyluric acids were detected between 0.5 and 12h after coffee intake, paraxanthine (PX) being the major metabolite (Cmax=3.36μM), followed by 1-methyluric acid (1-MU; Cmax=1.44μM) and 1-methylxanthine (1-MX; Cmax=1.27μM), identified in plasma samples for the first time. In 24h urine, eleven methylxanthines and methyluric acids were detected, 1-MU being the major metabolite (Cmax=150.52μM, Tmax=12h) amounting to 67.7% of the total urinary metabolites. In conclusion, a rapid absorption, metabolization and excretion of caffeine and its derived methylxanthines and methyluric acids have been observed after consumption of a green/roasted coffee product. •Novel findings on caffeine metabolites in plasma and urine after coffee intake•8 metabolites were identified in plasma, including 1-methylxanthine and 1-methyluric.•11 urine metabolites (tri- di- & mono-methylxanthines & methyluric acids) detected•LC–MS-QToF and HPLC-DAD (single run) were used with minimum sample preparation.•Caffeine is rapidly absorbed and metabolized after coffee intake by healthy subjects.
doi_str_mv 10.1016/j.foodres.2014.05.043
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In the present work, the bioavailability and metabolism of methylxanthines in a commercial soluble green/roasted coffee blend was studied. After a 3-day restriction of methylxanthine-containing foods, fasting healthy subjects (12 men and women) consumed the coffee product containing 70.69mg CF and 0.119mg theobromine (TB). Plasma samples were taken before (t=0h) and after coffee consumption at different time points (0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 9, 10 and 12h). Urine was collected at baseline (−2–0h) and at different intervals (0–2, 2–5, 5–8, 8–12 and 12–24h). Samples were analyzed by HPLC-DAD and LC–MS-QToF, and pharmacokinetic parameters were calculated. CF was the main methylxanthine found in plasma (Cmax=10.50μM, Tmax=1.2h). In addition, seven methylxanthines and methyluric acids were detected between 0.5 and 12h after coffee intake, paraxanthine (PX) being the major metabolite (Cmax=3.36μM), followed by 1-methyluric acid (1-MU; Cmax=1.44μM) and 1-methylxanthine (1-MX; Cmax=1.27μM), identified in plasma samples for the first time. In 24h urine, eleven methylxanthines and methyluric acids were detected, 1-MU being the major metabolite (Cmax=150.52μM, Tmax=12h) amounting to 67.7% of the total urinary metabolites. 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In addition, seven methylxanthines and methyluric acids were detected between 0.5 and 12h after coffee intake, paraxanthine (PX) being the major metabolite (Cmax=3.36μM), followed by 1-methyluric acid (1-MU; Cmax=1.44μM) and 1-methylxanthine (1-MX; Cmax=1.27μM), identified in plasma samples for the first time. In 24h urine, eleven methylxanthines and methyluric acids were detected, 1-MU being the major metabolite (Cmax=150.52μM, Tmax=12h) amounting to 67.7% of the total urinary metabolites. 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In the present work, the bioavailability and metabolism of methylxanthines in a commercial soluble green/roasted coffee blend was studied. After a 3-day restriction of methylxanthine-containing foods, fasting healthy subjects (12 men and women) consumed the coffee product containing 70.69mg CF and 0.119mg theobromine (TB). Plasma samples were taken before (t=0h) and after coffee consumption at different time points (0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 9, 10 and 12h). Urine was collected at baseline (−2–0h) and at different intervals (0–2, 2–5, 5–8, 8–12 and 12–24h). Samples were analyzed by HPLC-DAD and LC–MS-QToF, and pharmacokinetic parameters were calculated. CF was the main methylxanthine found in plasma (Cmax=10.50μM, Tmax=1.2h). In addition, seven methylxanthines and methyluric acids were detected between 0.5 and 12h after coffee intake, paraxanthine (PX) being the major metabolite (Cmax=3.36μM), followed by 1-methyluric acid (1-MU; Cmax=1.44μM) and 1-methylxanthine (1-MX; Cmax=1.27μM), identified in plasma samples for the first time. In 24h urine, eleven methylxanthines and methyluric acids were detected, 1-MU being the major metabolite (Cmax=150.52μM, Tmax=12h) amounting to 67.7% of the total urinary metabolites. In conclusion, a rapid absorption, metabolization and excretion of caffeine and its derived methylxanthines and methyluric acids have been observed after consumption of a green/roasted coffee product. •Novel findings on caffeine metabolites in plasma and urine after coffee intake•8 metabolites were identified in plasma, including 1-methylxanthine and 1-methyluric.•11 urine metabolites (tri- di- &amp; mono-methylxanthines &amp; methyluric acids) detected•LC–MS-QToF and HPLC-DAD (single run) were used with minimum sample preparation.•Caffeine is rapidly absorbed and metabolized after coffee intake by healthy subjects.</abstract><cop>Kidlington</cop><pub>Elsevier Ltd</pub><pmid>30011631</pmid><doi>10.1016/j.foodres.2014.05.043</doi><tpages>9</tpages><orcidid>https://orcid.org/0000-0003-2585-5286</orcidid><orcidid>https://orcid.org/0000-0002-7312-8641</orcidid></addata></record>
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subjects Bioavailability
Biological and medical sciences
Blends
Caffeine
Coffee
Consumption
Food industries
Foods
Fundamental and applied biological sciences. Psychology
Green coffee
Human
Metabolism
Metabolites
Methylxanthines
Urine
title Pharmacokinetics of caffeine and its metabolites in plasma and urine after consuming a soluble green/roasted coffee blend by healthy subjects
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