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European Journal of Pharmaceutical Sciences
Article . 2016 . Peer-reviewed
License: Elsevier TDM
Data sources: Crossref
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Improving the solubility of dexlansoprazole by cocrystallization with isonicotinamide

Authors: Jianhui Li; Lianyan Wang; Yue Qi Ye; Xue Fu; Qinghua Ren; Hailu Zhang; Zongwu Deng;

Improving the solubility of dexlansoprazole by cocrystallization with isonicotinamide

Abstract

Cocrystallization of an active pharmaceutical ingredient (API) with a cocrystal former (co-former) is widely used to tailor the physicochemical properties of parent APIs. For proton-pump inhibitors (PPIs), the isolation of cocrystals has not been widely investigated. Here, a 1:1 cocrystal of a PPI molecule, dexlansoprazole (DLS), was obtained by solvent crystallization with isonicotinamide (INM). The product was characterized by X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), solid-state and liquid NMR, as well as Fourier transform infrared spectroscopy (FTIR) techniques. A two-point R2(2)(9) hetero-synthon was proposed to exist in the cocrystal, where intermolecular hydrogen bonding occurs between NH, SO groups of DLS and amide of INM. The dissolution profiles of DLS and DLS-INM in water were also collected, and the results demonstrate the cocrystal exhibits superior apparent maximum solubility relative to the pure drug.

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Keywords

Niacinamide, Magnetic Resonance Spectroscopy, Calorimetry, Differential Scanning, Hydrogen Bonding, Proton Pump Inhibitors, Solubility, X-Ray Diffraction, Spectroscopy, Fourier Transform Infrared, Solvents, Dexlansoprazole, Crystallization, Powder Diffraction

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    popularity
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    influence
    This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
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    impulse
    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
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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!
21
Top 10%
Top 10%
Top 10%
gold