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Cocrystallization via planetary milling: enhancing throughput of solid-state screening methods.

Stephen R Bysouth1, Joanna A Bis, David Igo

  • 1Automaxion SARL, L'Auvrairie, 50250 Varenguebec, France. stephen.bysouth@automaxionltd.com

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Summary
This summary is machine-generated.

A new parallel milling system enables rapid screening of pharmaceutical cocrystals. This high-throughput method efficiently processes limited samples without vessel decontamination, streamlining drug discovery.

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Area of Science:

  • Materials Science
  • Pharmaceutical Technology
  • Chemical Engineering

Background:

  • Pharmaceutical cocrystal screening is crucial for drug development.
  • Traditional methods can be time-consuming and require significant sample amounts.
  • Efficient screening platforms are needed to accelerate the discovery of new drug forms.

Purpose of the Study:

  • To demonstrate a novel modified planetary mill for rapid, parallel screening of pharmaceutical cocrystals.
  • To evaluate the system's suitability for handling limited sample availability.
  • To discuss the integration of the mill into an automated, high-throughput screening workflow.

Main Methods:

  • Utilized a modified planetary mill capable of processing 48 samples simultaneously.
  • Conducted cocrystal synthesis via grinding for carbamazepine/saccharin, caffeine/oxalic acid, and caffeine/maleic acid.
  • Performed milling directly in standard glass vials to prevent sample loss and eliminate decontamination steps.

Main Results:

  • Successfully demonstrated the rapid screening of multiple pharmaceutical cocrystal systems.
  • Showcased the system's efficiency with limited sample quantities due to successive processing.
  • Highlighted the elimination of vessel decontamination and sample loss by milling in vials.

Conclusions:

  • The novel parallel milling system offers a rapid and efficient approach for pharmaceutical cocrystal screening.
  • Its design is advantageous for handling scarce compounds and integrating into automated workflows.
  • This technology has the potential to accelerate the identification of promising cocrystal candidates in drug discovery.