PHARMACOKINETIC STUDY OF HY-FOLIC AND FOLIC ACID IN HEALTHY VOLUNTEERS
DOI:
https://doi.org/10.22159/ijap.2024v16i6.51874Keywords:
Folic acid, HY-FOLIC, Methyltetrahydrofolate, PharmacokineticsAbstract
Objective: HY-FOLIC® is the active form of Folic Acid (FA) produced by PT Simex Pharmaceutical Indonesia containing (6S)-5-Methyltetrahydrofolate (5-MTHF). We evaluated the pharmacokinetic profiles of HY-FOLIC® versus FA after single oral administration in healthy volunteers.
Methods: A randomized, open-label, 2-way crossover, single-dose design was conducted on 12 healthy subjects with two steps. In the first step, 6 subjects were given 1100 mcg of HY-FOLIC® (1.3 μmol), and 6 subjects were given an equimolar dose of 600 mcg of FA (1.3 μmol) in a fasting condition. Blood samples were taken before, and at 1, 2, 3, 4, 5, 6, 7, and 8 hours after administration of products for measurement of peak concentration (Cmax), the Area Under the Curve at t-time (AUCt) and infinite time (AUCinf). After a washout period of 14 days, the same procedure was repeated in which the first 6 subjects received FA, and the second 6 subjects received HY-FOLIC®. Pharmacokinetic data of 5-MTHF and Unmetabolized Folic Acid (UMFA) were compared with paired t-tests.
Results: Cmax of 5-MTHF (mean + SD) following administration of HY-FOLIC® and FA were 46.91 + 28.16 vs 22.61 + 15.73 nmol/L, respectively (p=0.000); the AUCt were 214.47 + 183.46 vs 112.93 + 112.11 h.mmol/L (p=0.001). Conversely, Cmax of UMFA were 9.49 + 7.89 vs 21.97 + 14.79 nmol/L (p=0.003); AUCt 33.29 + 39.34 vs 78.16 + 58.93 h.nmol/L (p=0.001).
Conclusion: HY-FOLIC® is much more bioavailable than FA as indicated by much higher Cmax and AUCt of the active form of 5-MTHF
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