Food effects on the absorption and pharmacokinetics of cocoa flavanols

Derek D. Schramm, Malina Karim, Heather R. Schrader, Roberta R. Holt, Nadine J. Kirkpatrick, John A. Polagruto, Jodi L. Ensunsa, Harold H. Schmitz, Carl L Keen

Research output: Contribution to journalArticle

121 Citations (Scopus)

Abstract

Macronutrients in food and gastric acid are known to have a pronounced effect on the metabolism of many xenobiotics, an effect that impacts their efficacy as bioactive agents. In this investigation we assessed the impact of select food treatments and the histamine H2-receptor antagonist Famotidine (Pepcid-AC) on flavanol absorption and metabolism. Four crossover intervention studies were conducted with 6 subjects each. Volunteers consumed sugar-free, flavanol-rich cocoa (0.125 g/kg body wt) alone, with macronutrient-rich foods (8.75 or 17.5 kJ/kg subject body wt) or Famotidine (Pepcid-AC). Blood samples were drawn at 5 time points including baseline. Plasma samples were analyzed for epicatechin and catechin flavanols by HPLC. Pharmacokinetic parameters were assessed using non-compartmental methodology. When provided at 17.5 kJ/kg subject body weight (∼4 kcal/kg), sugar and bread test meals increased flavanol area under the curve (AUC) values to 140% of control values (P < 0.05). A corresponding tendency for plasma antioxidant capacity to increase was observed for the cocoa treatment at 1.5 and 2.5 h (P < 0.17, P < 0.06, respectively). The ability of treatment meals to affect AUC values was positively correlated with treatment carbohydrate content (r = 0.83; P< 0.02). In contrast to carbohydrate rich meals, lipid and protein rich meals and Famotidine treatment had minimal effects on flavanol absorption. Based on Cmax and AUC values, this data suggests that the uptake of flavanols can be increased significantly by concurrent carbohydrate consumption.

Original languageEnglish (US)
Pages (from-to)857-869
Number of pages13
JournalLife Sciences
Volume73
Issue number7
DOIs
StatePublished - Jul 4 2003

Fingerprint

Cocoa
Famotidine
Pharmacokinetics
Meals
Food
Area Under Curve
Catechin
Carbohydrates
Metabolism
Sugars
Histamine H2 Antagonists
Plasmas
Therapeutics
Bread
Gastric Acid
Xenobiotics
Cross-Over Studies
Volunteers
Blood
Antioxidants

Keywords

  • Absorption
  • Carbohydrate
  • Chocolate
  • Cocoa
  • Epicatechin
  • Flavanol
  • Flavonoid

ASJC Scopus subject areas

  • Pharmacology

Cite this

Schramm, D. D., Karim, M., Schrader, H. R., Holt, R. R., Kirkpatrick, N. J., Polagruto, J. A., ... Keen, C. L. (2003). Food effects on the absorption and pharmacokinetics of cocoa flavanols. Life Sciences, 73(7), 857-869. https://doi.org/10.1016/S0024-3205(03)00373-4

Food effects on the absorption and pharmacokinetics of cocoa flavanols. / Schramm, Derek D.; Karim, Malina; Schrader, Heather R.; Holt, Roberta R.; Kirkpatrick, Nadine J.; Polagruto, John A.; Ensunsa, Jodi L.; Schmitz, Harold H.; Keen, Carl L.

In: Life Sciences, Vol. 73, No. 7, 04.07.2003, p. 857-869.

Research output: Contribution to journalArticle

Schramm, DD, Karim, M, Schrader, HR, Holt, RR, Kirkpatrick, NJ, Polagruto, JA, Ensunsa, JL, Schmitz, HH & Keen, CL 2003, 'Food effects on the absorption and pharmacokinetics of cocoa flavanols', Life Sciences, vol. 73, no. 7, pp. 857-869. https://doi.org/10.1016/S0024-3205(03)00373-4
Schramm DD, Karim M, Schrader HR, Holt RR, Kirkpatrick NJ, Polagruto JA et al. Food effects on the absorption and pharmacokinetics of cocoa flavanols. Life Sciences. 2003 Jul 4;73(7):857-869. https://doi.org/10.1016/S0024-3205(03)00373-4
Schramm, Derek D. ; Karim, Malina ; Schrader, Heather R. ; Holt, Roberta R. ; Kirkpatrick, Nadine J. ; Polagruto, John A. ; Ensunsa, Jodi L. ; Schmitz, Harold H. ; Keen, Carl L. / Food effects on the absorption and pharmacokinetics of cocoa flavanols. In: Life Sciences. 2003 ; Vol. 73, No. 7. pp. 857-869.
@article{00e8ccec00e047d09280950d586fa91c,
title = "Food effects on the absorption and pharmacokinetics of cocoa flavanols",
abstract = "Macronutrients in food and gastric acid are known to have a pronounced effect on the metabolism of many xenobiotics, an effect that impacts their efficacy as bioactive agents. In this investigation we assessed the impact of select food treatments and the histamine H2-receptor antagonist Famotidine (Pepcid-AC) on flavanol absorption and metabolism. Four crossover intervention studies were conducted with 6 subjects each. Volunteers consumed sugar-free, flavanol-rich cocoa (0.125 g/kg body wt) alone, with macronutrient-rich foods (8.75 or 17.5 kJ/kg subject body wt) or Famotidine (Pepcid-AC). Blood samples were drawn at 5 time points including baseline. Plasma samples were analyzed for epicatechin and catechin flavanols by HPLC. Pharmacokinetic parameters were assessed using non-compartmental methodology. When provided at 17.5 kJ/kg subject body weight (∼4 kcal/kg), sugar and bread test meals increased flavanol area under the curve (AUC) values to 140{\%} of control values (P < 0.05). A corresponding tendency for plasma antioxidant capacity to increase was observed for the cocoa treatment at 1.5 and 2.5 h (P < 0.17, P < 0.06, respectively). The ability of treatment meals to affect AUC values was positively correlated with treatment carbohydrate content (r = 0.83; P< 0.02). In contrast to carbohydrate rich meals, lipid and protein rich meals and Famotidine treatment had minimal effects on flavanol absorption. Based on Cmax and AUC values, this data suggests that the uptake of flavanols can be increased significantly by concurrent carbohydrate consumption.",
keywords = "Absorption, Carbohydrate, Chocolate, Cocoa, Epicatechin, Flavanol, Flavonoid",
author = "Schramm, {Derek D.} and Malina Karim and Schrader, {Heather R.} and Holt, {Roberta R.} and Kirkpatrick, {Nadine J.} and Polagruto, {John A.} and Ensunsa, {Jodi L.} and Schmitz, {Harold H.} and Keen, {Carl L}",
year = "2003",
month = "7",
day = "4",
doi = "10.1016/S0024-3205(03)00373-4",
language = "English (US)",
volume = "73",
pages = "857--869",
journal = "Life Sciences",
issn = "0024-3205",
publisher = "Elsevier Inc.",
number = "7",

}

TY - JOUR

T1 - Food effects on the absorption and pharmacokinetics of cocoa flavanols

AU - Schramm, Derek D.

AU - Karim, Malina

AU - Schrader, Heather R.

AU - Holt, Roberta R.

AU - Kirkpatrick, Nadine J.

AU - Polagruto, John A.

AU - Ensunsa, Jodi L.

AU - Schmitz, Harold H.

AU - Keen, Carl L

PY - 2003/7/4

Y1 - 2003/7/4

N2 - Macronutrients in food and gastric acid are known to have a pronounced effect on the metabolism of many xenobiotics, an effect that impacts their efficacy as bioactive agents. In this investigation we assessed the impact of select food treatments and the histamine H2-receptor antagonist Famotidine (Pepcid-AC) on flavanol absorption and metabolism. Four crossover intervention studies were conducted with 6 subjects each. Volunteers consumed sugar-free, flavanol-rich cocoa (0.125 g/kg body wt) alone, with macronutrient-rich foods (8.75 or 17.5 kJ/kg subject body wt) or Famotidine (Pepcid-AC). Blood samples were drawn at 5 time points including baseline. Plasma samples were analyzed for epicatechin and catechin flavanols by HPLC. Pharmacokinetic parameters were assessed using non-compartmental methodology. When provided at 17.5 kJ/kg subject body weight (∼4 kcal/kg), sugar and bread test meals increased flavanol area under the curve (AUC) values to 140% of control values (P < 0.05). A corresponding tendency for plasma antioxidant capacity to increase was observed for the cocoa treatment at 1.5 and 2.5 h (P < 0.17, P < 0.06, respectively). The ability of treatment meals to affect AUC values was positively correlated with treatment carbohydrate content (r = 0.83; P< 0.02). In contrast to carbohydrate rich meals, lipid and protein rich meals and Famotidine treatment had minimal effects on flavanol absorption. Based on Cmax and AUC values, this data suggests that the uptake of flavanols can be increased significantly by concurrent carbohydrate consumption.

AB - Macronutrients in food and gastric acid are known to have a pronounced effect on the metabolism of many xenobiotics, an effect that impacts their efficacy as bioactive agents. In this investigation we assessed the impact of select food treatments and the histamine H2-receptor antagonist Famotidine (Pepcid-AC) on flavanol absorption and metabolism. Four crossover intervention studies were conducted with 6 subjects each. Volunteers consumed sugar-free, flavanol-rich cocoa (0.125 g/kg body wt) alone, with macronutrient-rich foods (8.75 or 17.5 kJ/kg subject body wt) or Famotidine (Pepcid-AC). Blood samples were drawn at 5 time points including baseline. Plasma samples were analyzed for epicatechin and catechin flavanols by HPLC. Pharmacokinetic parameters were assessed using non-compartmental methodology. When provided at 17.5 kJ/kg subject body weight (∼4 kcal/kg), sugar and bread test meals increased flavanol area under the curve (AUC) values to 140% of control values (P < 0.05). A corresponding tendency for plasma antioxidant capacity to increase was observed for the cocoa treatment at 1.5 and 2.5 h (P < 0.17, P < 0.06, respectively). The ability of treatment meals to affect AUC values was positively correlated with treatment carbohydrate content (r = 0.83; P< 0.02). In contrast to carbohydrate rich meals, lipid and protein rich meals and Famotidine treatment had minimal effects on flavanol absorption. Based on Cmax and AUC values, this data suggests that the uptake of flavanols can be increased significantly by concurrent carbohydrate consumption.

KW - Absorption

KW - Carbohydrate

KW - Chocolate

KW - Cocoa

KW - Epicatechin

KW - Flavanol

KW - Flavonoid

UR - http://www.scopus.com/inward/record.url?scp=0037836031&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0037836031&partnerID=8YFLogxK

U2 - 10.1016/S0024-3205(03)00373-4

DO - 10.1016/S0024-3205(03)00373-4

M3 - Article

VL - 73

SP - 857

EP - 869

JO - Life Sciences

JF - Life Sciences

SN - 0024-3205

IS - 7

ER -