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Structure, physicochemical properties and pharmacokinetics of resveratrol and piperine cocrystals

Abstract

It was reported that the alkaloid component, piperine (Pip), can drastically improve the bioavailability of resveratrol (RSV) compound when co-administrated. Therefore, the cocrystallization experiments of RSV and Pip were attempted, and four cocrystals are successfully obtained from solution evaporation experiments. Their single crystals are acquired and the structural determination reveals that all the cocrystals contain solvent molecules within the crystals. Confirmed by the VT-PXRD, the cocrystals transformed into amorphous state after desolvation. Considering the toxcity of solvent molecule, only RSV-Pip co-1 was utilized for further dissolution and pharmacokinetic experiments. The dissoluton results demonstrate that RSV-Pip co-1 shows lower dissoluton and apparent solubility compared to RSV constituent under different buffer in presence of different surfactants. The reduced dissolution and apparent solubility have a strong diminishing impact on the absorption of RSV thus leading to unfavorable bioavailability, even though coformer Pip possesses bioenhancer property.

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Publication details

The article was received on 11 Aug 2017, accepted on 13 Sep 2017 and first published on 14 Sep 2017


Article type: Paper
DOI: 10.1039/C7CE01468F
Citation: CrystEngComm, 2017, Accepted Manuscript
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    Structure, physicochemical properties and pharmacokinetics of resveratrol and piperine cocrystals

    H. He, Q. Zhang, J. Wang and X. Mei, CrystEngComm, 2017, Accepted Manuscript , DOI: 10.1039/C7CE01468F

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