bioavaliability

Bioavailability & pharmacokinetics

HMRlignan™ Effectively Elevates Plasma Enterolactone

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Bioavailability & Pharmacokinetics

Study 1

A pharmacokinetic (PK) study followed by an 8-week dose comparison study was conducted in postmenopausal women (natural or surgical menopause ≥1 year; age 50-75 years; BMI ≥25 and ≤35 kg/m2).1 The PK study was conducted with 12 women who took a single dose of 36 mg of HMRlignan followed by blood sampling up to 72 hours. The dose comparison study included 22 women randomized into two groups – 36 mg/day and 72 mg/day doses. Blood and urine were collected at baseline, after 4 weeks and 8 weeks.

The PK study demonstrated significant increases in plasma concentrations of 7-hydroxymatairesinol (7-HMR) (peak at 1 hour) and the metabolite enterolactone (ENL) (peak at 24 hours). In the dose-comparison study, 7-HMR and ENL levels increased at week 8 in comparison to baseline following intake of 36 mg/day and 72 mg/day of HMRlignan.

Study 2

A single dose, parallel-group, double-blind study, HMRlignan was given to healthy male volunteers (n=38) in ascending doses (1 to 1200 mg). Subjects were on a lignan-poor diet one week prior to the study and for 3 days after. Plasma concentrations of hydroxymatairesinol (HMR) and enterolactone (ENL) were measured on days -7, -3, and right before HMRlignan administration and at 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 30, 48, and 72 hours thereafter.

HMRlignan was rapidly absorbed Plasma concentrations increased with increasing dose and the increases in AUC and C(max) values appeared to be linear. The apparent mean elimination half-life ranged from 2.6 to 5.1 hours. ENL was detected as the main metabolite and was dose-dependently elevated – doses as low as 10 mg produced a marked elevation in ENL concentrations.

 

1. Udani JK, Brown DJ, Tan MOC, Hardy M. Pharmacokinetics and bioavailability of plant lignin 7-hydroxymatairesinol and effects on serum enterolactone and clinical symptoms in postmenopausal women: A single-blinded, parallel, dose-comparison study. J Amer Coll Nutr 2013;32:428-35.