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Modular microfluidic platform for solubility measurement, nucleation statistics and polymorph screening of active pharmaceutical ingredients: Irbesartan, Rimonabant, Aripiprazole and Sulfathiazole.

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Title: Modular microfluidic platform for solubility measurement, nucleation statistics and polymorph screening of active pharmaceutical ingredients: Irbesartan, Rimonabant, Aripiprazole and Sulfathiazole.
Authors: Lambert, Mathilde1,2 (AUTHOR), Grossier, Romain1 (AUTHOR) romain.grossier@cnrs.fr, Lagaize, Mehdi1 (AUTHOR), Bactivelane, Thirou1 (AUTHOR), Heresanu, Vasile1 (AUTHOR), Robert, Benoît2 (AUTHOR), Candoni, Nadine1 (AUTHOR) nadine.candoni@univ-amu.fr, Veesler, Stéphane1 (AUTHOR) stephane.veesler@cnrs.fr
Source: Journal of Crystal Growth. Aug2023, Vol. 616, pN.PAG-N.PAG. 1p.
Subjects: Nucleation, Rimonabant, Aripiprazole, Irbesartan, Drug efficacy, Supersaturation, Crystallization
Abstract: Drug efficacy strongly relies on the solid state of the active pharmaceutical ingredient. Classical solid-state screening methods involve different solvent compositions and supersaturations. Moreover, the many repeated experiments needed to address the stochasticity of nucleation make this approach costly. This paper presents a newly developed modular microfluidic platform that provides a universal and flexible plug-and-play tool for crystallisation studies without use of surfactants. By dissolving a powder, our set-up generates saturated solutions that can be used for solubility measurements or distributed in microdroplets. Here, we describe solubility measurements performed on different forms, stable and metastable, of pharmaceutical molecules (Irbesartan, Rimonabant and Aripiprazole) in organic and aqueous solvents. In addition, we provide nucleation statistics obtained for Sulfathiazole in water and in acetonitrile. Reporting polymorph screening on Sulfathiazole and statistics for nucleated forms, we find that the cooling rate influences both nucleation and polymorphism results, reflecting the competition between thermodynamics and kinetics. Three unknown forms were discovered, with XRD patterns and Raman spectra that do not match any referenced form. We also demonstrate the limitations of microfluidics for crystallisation by cooling: reducing the crystalliser volume considerably increases nucleation induction time. [ABSTRACT FROM AUTHOR]
Copyright of Journal of Crystal Growth is the property of Elsevier B.V. and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)
Database: Engineering Source
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Header DbId: egs
DbLabel: Engineering Source
An: 164155729
AccessLevel: 6
PubType: Academic Journal
PubTypeId: academicJournal
PreciseRelevancyScore: 0
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  Data: Modular microfluidic platform for solubility measurement, nucleation statistics and polymorph screening of active pharmaceutical ingredients: Irbesartan, Rimonabant, Aripiprazole and Sulfathiazole.
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  Data: <searchLink fieldCode="AR" term="%22Lambert%2C+Mathilde%22">Lambert, Mathilde</searchLink><relatesTo>1,2</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Grossier%2C+Romain%22">Grossier, Romain</searchLink><relatesTo>1</relatesTo> (AUTHOR)<i> romain.grossier@cnrs.fr</i><br /><searchLink fieldCode="AR" term="%22Lagaize%2C+Mehdi%22">Lagaize, Mehdi</searchLink><relatesTo>1</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Bactivelane%2C+Thirou%22">Bactivelane, Thirou</searchLink><relatesTo>1</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Heresanu%2C+Vasile%22">Heresanu, Vasile</searchLink><relatesTo>1</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Robert%2C+Benoît%22">Robert, Benoît</searchLink><relatesTo>2</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Candoni%2C+Nadine%22">Candoni, Nadine</searchLink><relatesTo>1</relatesTo> (AUTHOR)<i> nadine.candoni@univ-amu.fr</i><br /><searchLink fieldCode="AR" term="%22Veesler%2C+Stéphane%22">Veesler, Stéphane</searchLink><relatesTo>1</relatesTo> (AUTHOR)<i> stephane.veesler@cnrs.fr</i>
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  Data: <searchLink fieldCode="JN" term="%22Journal+of+Crystal+Growth%22">Journal of Crystal Growth</searchLink>. Aug2023, Vol. 616, pN.PAG-N.PAG. 1p.
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  Data: <searchLink fieldCode="DE" term="%22Nucleation%22">Nucleation</searchLink><br /><searchLink fieldCode="DE" term="%22Rimonabant%22">Rimonabant</searchLink><br /><searchLink fieldCode="DE" term="%22Aripiprazole%22">Aripiprazole</searchLink><br /><searchLink fieldCode="DE" term="%22Irbesartan%22">Irbesartan</searchLink><br /><searchLink fieldCode="DE" term="%22Drug+efficacy%22">Drug efficacy</searchLink><br /><searchLink fieldCode="DE" term="%22Supersaturation%22">Supersaturation</searchLink><br /><searchLink fieldCode="DE" term="%22Crystallization%22">Crystallization</searchLink>
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  Label: Abstract
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  Data: Drug efficacy strongly relies on the solid state of the active pharmaceutical ingredient. Classical solid-state screening methods involve different solvent compositions and supersaturations. Moreover, the many repeated experiments needed to address the stochasticity of nucleation make this approach costly. This paper presents a newly developed modular microfluidic platform that provides a universal and flexible plug-and-play tool for crystallisation studies without use of surfactants. By dissolving a powder, our set-up generates saturated solutions that can be used for solubility measurements or distributed in microdroplets. Here, we describe solubility measurements performed on different forms, stable and metastable, of pharmaceutical molecules (Irbesartan, Rimonabant and Aripiprazole) in organic and aqueous solvents. In addition, we provide nucleation statistics obtained for Sulfathiazole in water and in acetonitrile. Reporting polymorph screening on Sulfathiazole and statistics for nucleated forms, we find that the cooling rate influences both nucleation and polymorphism results, reflecting the competition between thermodynamics and kinetics. Three unknown forms were discovered, with XRD patterns and Raman spectra that do not match any referenced form. We also demonstrate the limitations of microfluidics for crystallisation by cooling: reducing the crystalliser volume considerably increases nucleation induction time. [ABSTRACT FROM AUTHOR]
– Name: AbstractSuppliedCopyright
  Label:
  Group: Ab
  Data: <i>Copyright of Journal of Crystal Growth is the property of Elsevier B.V. and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract.</i> (Copyright applies to all Abstracts.)
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RecordInfo BibRecord:
  BibEntity:
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      – Type: doi
        Value: 10.1016/j.jcrysgro.2023.127252
    Languages:
      – Code: eng
        Text: English
    PhysicalDescription:
      Pagination:
        PageCount: 1
        StartPage: N.PAG
    Subjects:
      – SubjectFull: Nucleation
        Type: general
      – SubjectFull: Rimonabant
        Type: general
      – SubjectFull: Aripiprazole
        Type: general
      – SubjectFull: Irbesartan
        Type: general
      – SubjectFull: Drug efficacy
        Type: general
      – SubjectFull: Supersaturation
        Type: general
      – SubjectFull: Crystallization
        Type: general
    Titles:
      – TitleFull: Modular microfluidic platform for solubility measurement, nucleation statistics and polymorph screening of active pharmaceutical ingredients: Irbesartan, Rimonabant, Aripiprazole and Sulfathiazole.
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            NameFull: Lambert, Mathilde
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            NameFull: Grossier, Romain
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            NameFull: Lagaize, Mehdi
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            NameFull: Bactivelane, Thirou
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            NameFull: Heresanu, Vasile
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          Dates:
            – D: 15
              M: 08
              Text: Aug2023
              Type: published
              Y: 2023
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              Value: 00220248
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              Value: 616
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