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Pharmacokinetics of Sodium and Calcium Salts of (6S)-5-Methyltetrahydrofolic Acid Compared to Folic Acid and Indirect Comparison of the Two Salts

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Laboratory Medicine, Department of Clinical Chemistry, Saarland University Hospital, Building 57, D-66424 Homburg/Saar, Germany
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BioTeSys GmbH, Schelztorstr. 54-56, D-73728 Esslingen, Germany
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Department of Nutrition and Food Science, Rheinische Friedrich-Wilhelms University, Endenicher Allee 19B, D-53115 Bonn, Germany
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Department of Mathematics, Natural and Economic Sciences, Ulm University of Applied Sciences, Albert-Einstein-Allee 55, D-89081 Ulm, Germany
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Department of Internal Medicine, Amsterdam UMC, Location VUmc, 1081 HV Amsterdam, The Netherlands
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Merck & Cie, Im Laternenacker 5, CH-8200 Schaffhausen, Switzerland
*
Author to whom correspondence should be addressed.
Nutrients 2020, 12(12), 3623; https://doi.org/10.3390/nu12123623
Received: 14 September 2020 / Revised: 22 November 2020 / Accepted: 23 November 2020 / Published: 25 November 2020
(This article belongs to the Section Clinical Nutrition)
(6S)-5-Methyltetrahydrofolic acid ((6S)-5-Methyl-THF) salts and folic acid may differ in their abilities to raise plasma (6S)-5-Methyl-THF levels. We compared the area under the curve (AUC), Cmax, and Tmax of plasma (6S)-5-Methyl-THF after intakes of (6S)-5-Methyl-THF-Na salt (Arcofolin®) and folic acid. Moreover, we compared the AUCs after intakes of (6S)-5-Methyl-THF-Na and the calcium salt, (6S)-5-Methyl-THF-Ca, that were tested against folic acid in two independent studies. The study was randomized, double blind, and cross over. Twenty-four adults (12 men and 12 women) received a single oral dose of 436 µg (6S)-5-Methyl-THF-Na and an equimolar dose of folic acid (400 µg) on two kinetic days with two weeks washout period in between. The plasma concentrations of (6S)-5-Methyl-THF were measured at 9 time points between 0 and 8 h. We found that the AUC0–8 h of plasma (6S)-5-Methyl-THF (mean (SD) = 126.0 (33.6) vs. 56.0 (25.3) nmol/L*h) and Cmax (36.8 (10.8) vs. 11.1 (4.1) nmol/L) were higher after administration of (6S)-5-Methyl-THF-Na than after the administration of folic acid (p < 0.001 for both). These differences were present in men and women. Only administration of folic acid resulted in a transient increase in plasma unmetabolized folic acid (2.5 (2.0) nmol/L after 0.5 h and 4.7 (2.9) nmol/L after 1 h). Intake of (6S)-5-Methyl-THF-Na was safe. The ratios of the AUC0–8 h for (6S)-5-Methyl-THF-Na and (6S)-5-Methyl-THF-Ca to the corresponding folic acid reference group and the delta of these AUC0–8 h did not differ between the studies. In conclusion, a single oral dose of (6S)-5-Methyl-THF-Na caused higher AUC0–8 h and Cmax of plasma (6S)-5-Methyl-THF compared to folic acid. The Na- and Ca- salts of (6S)-5-Methyl-THF are not likely to differ in their pharmacokinetics. Further studies may investigate whether supplementation of the compounds for a longer time will lead to differences in circulating or intracellular/tissue folate concentrations. View Full-Text
Keywords: Arcofolin®; bioavailability; homocysteine; folic acid; Metafolin®; (6S)-5-Methyl-THF; plasma folate; red blood cell folate Arcofolin®; bioavailability; homocysteine; folic acid; Metafolin®; (6S)-5-Methyl-THF; plasma folate; red blood cell folate
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MDPI and ACS Style

Obeid, R.; Schön, C.; Pietrzik, K.; Menzel, D.; Wilhelm, M.; Smulders, Y.; Knapp, J.-P.; Böhni, R. Pharmacokinetics of Sodium and Calcium Salts of (6S)-5-Methyltetrahydrofolic Acid Compared to Folic Acid and Indirect Comparison of the Two Salts. Nutrients 2020, 12, 3623. https://doi.org/10.3390/nu12123623

AMA Style

Obeid R, Schön C, Pietrzik K, Menzel D, Wilhelm M, Smulders Y, Knapp J-P, Böhni R. Pharmacokinetics of Sodium and Calcium Salts of (6S)-5-Methyltetrahydrofolic Acid Compared to Folic Acid and Indirect Comparison of the Two Salts. Nutrients. 2020; 12(12):3623. https://doi.org/10.3390/nu12123623

Chicago/Turabian Style

Obeid, Rima; Schön, Christiane; Pietrzik, Klaus; Menzel, Daniel; Wilhelm, Manfred; Smulders, Yvo; Knapp, Jean-Pierre; Böhni, Ruth. 2020. "Pharmacokinetics of Sodium and Calcium Salts of (6S)-5-Methyltetrahydrofolic Acid Compared to Folic Acid and Indirect Comparison of the Two Salts" Nutrients 12, no. 12: 3623. https://doi.org/10.3390/nu12123623

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