Issue 8, 2010

Nutraceutical cocrystals: utilizing pterostilbene as a cocrystal former

Abstract

The nutraceutical compound pterostilbene is investigated for its propensity to form cocrystalline materials with active pharmaceutical ingredients. Three cocrystals of a 1 : 1 stoichiometric molar ratio of pterostilbene with caffeine (two polymorphs, Form I and Form II) and carbamazepine were prepared and characterized by crystallographic (XRPD, single-crystal) and thermoanalytical (TGA, DSC) techniques. Physical stability of the cocrystals with respect to relative humidity (RH) was examined and found to be dramatically improved in relationship to caffeine or carbamazepine. The carbamazepine : pterostilbene cocrystal was stable upon slurrying in water for 3 days; therefore, aqueous equilibrium solubility measurements were carried out, revealing that the cocrystal solubility was 7× lower than carbamazepine dihydrate and 2.5× lower than pterostilbene. Slurrying the caffeine : pterostilbene cocrystal (Form I) in water led to a solution that was supersaturated with respect to pterostilbene, resulting in the precipitation of pterostilbene after three days; therefore concentrations at specific time points were measured as opposed to equilibrium solubility. At five hours the concentration of the caffeine cocrystal was 33× lower than the caffeine hydrate solubility, but was 27× higher than the pterostilbene solubility.

Graphical abstract: Nutraceutical cocrystals: utilizing pterostilbene as a cocrystal former

  • This article is part of the themed collection: New Talent

Supplementary files

Article information

Article type
Paper
Submitted
04 Feb 2010
Accepted
14 Apr 2010
First published
24 May 2010

CrystEngComm, 2010,12, 2436-2442

Nutraceutical cocrystals: utilizing pterostilbene as a cocrystal former

N. Schultheiss, S. Bethune and J. Henck, CrystEngComm, 2010, 12, 2436 DOI: 10.1039/C002045A

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