A group in France has come up with a patented lipid formulation that they claim shows a ~9 fold improvement in the AUC in humans. From the Methods section "The lipid formulation consists of natural t-Res powder (40 mg) dissolved in a complex mixture notably containing polysorbate 20 and polyglyceryl-3-dioleate. This solution is embedded in a caplet as described in patent WO YVERY N° 2010/007252. Other chemicals were purchased from Sigma–Aldrich (France)." It's an interesting read.
Biochimie. 2013 Jan 31. pii: S0300-9084(13)00011-4. doi: 10.1016/j.biochi.2013.01.008. [Epub ahead of print]
Optimization of trans-Resveratrol bioavailability for human therapy.
Amiot MJ, Romier B, Anh Dao TM, Fanciullino R, Ciccolini J, Burcelin R, Pechere L, Emond C, Savouret JF, Seree E.
Source
University Aix Marseille, INRA UMR 1260, 13385 Marseille, France; University Aix Marseille, INSERM UMR 1062, 13385 Marseille, France; University Aix Marseille, Faculte de Medecine La Timone, Marseille F-13385, France.
Abstract
We have developed an innovative soluble galenic form to overcome the low absorption of trans-Resveratrol (t-Res) as a dry powder. We present here data on pharmacokinetics, bioavailability, and toxicity of t-Res in human volunteers treated with this soluble form, plus additional data on biological effects in rodents. Fifteen healthy volunteers of both sexes received 40 mg of t-Res in two forms, the soluble formulation (caplets) and the original powder (capsules), in a crossover design. Blood samples were collected at 15 min, 30 min, and every hour for 5 h. Plasma concentrations of t-Res and its metabolites were analyzed by liquid chromatography and mass spectrometry. The single dose (40 mg) of the soluble t-Res was well absorbed and elicited biologically efficient blood levels (0.1-6 μM) for several hours, despite metabolization into glucuronide and sulfate conjugates coupled to renal elimination. In contrast, t-Res administered as a dry powder barely elicited efficient blood levels for a short duration. The new formulation led to 8.8-fold higher t-Res levels in plasma versus the powder. t-Res metabolism was not modified and neither intolerance nor toxicity were observed during the study and the following week. The soluble formulation elicited a robust anti-inflammatory effect in various tissues of mice fed a high-fat diet, while dry powder t-Res was almost inactive. Our data suggest that significant improvements in t-Res bioavailability and efficiency can be obtained by this soluble galenic form, also allowing lower doses. The use of t-Res in human therapy is thus greatly facilitated and the toxicity risk is reduced.
Copyright © 2013 Elsevier Masson SAS. All rights reserved.
PMID: 23376875
edit for typos...
Edited by malbecman, 11 February 2013 - 05:38 PM.