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Journal of Pharmaceutical Sciences
Article
License: CC BY NC ND
Data sources: UnpayWall
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Journal of Pharmaceutical Sciences
Article . 2016 . Peer-reviewed
License: Elsevier TDM
Data sources: Crossref
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Improving Biopharmaceutical Properties of Vinpocetine Through Cocrystallization

Authors: GOLOB, SAMUEL; Perry, Miranda; Lusi, Matteo; Chierotti, Michele R.; GRABNAR, IZTOK; LASSIANI, LUCIA; VOINOVICH, DARIO; +1 Authors

Improving Biopharmaceutical Properties of Vinpocetine Through Cocrystallization

Abstract

Vinpocetine is a poorly water soluble weakly basic drug (pKa = 7.1) used for the treatment of several cerebrovascular and cognitive disorders. Because existing formulations exhibit poor bioavailability and scarce absorption, a dosage form with improved pharmacokinetic properties is highly desirable. Cocrystallization represents a promising approach to generate diverse novel crystal forms and to improve the aqueous solubility and in turn the oral bioavailability. In this article, a novel ionic cocrystal of vinpocetine is described, using boric acid as a coformer, and fully characterized (by means of differential scanning calorimetry, solid-state nuclear magnetic resonance, powder and single-crystal X-ray diffraction, and powder dissolution test). Pharmacokinetic performance was also tested in a human pilot study. This pharmaceutical ionic cocrystal exhibits superior solubilization kinetics and modulates important pharmacokinetic values such as maximum concentration in plasma (Cmax), time to maximum concentration (tmax), and area under the plasma concentration-time curve (AUC) of the poorly soluble vinpocetine and it therefore offers an innovative approach to improve its bioavailability.

Country
Italy
Keywords

Adult, Male, Calorimetry, Differential Scanning, Vasodilator Agents, ionic cocrystal, Administration, Oral, vinpocetine, Middle Aged, Biopharmaceutics, bioavailability; boric acid; ionic cocrystal; pharmacokinetics; vinpocetine, Boric Acids, X-Ray Diffraction, Humans, pharmacokinetic, bioavailability, Crystallization, Vinca Alkaloids, boric acid

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    popularity
    This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
    Top 10%
    influence
    This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    Top 10%
    impulse
    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
    Top 10%
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selected citations
These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
33
Top 10%
Top 10%
Top 10%
Green
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