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Screening for crystalline salts via mechanochemistry
Andrew V Trask1, Delia A Haynes, W D Samuel Motherwell
1Pfizer Institute for Pharmaceutical Materials Science, Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, UKCB2 1EW.
Chemical Communications (Cambridge, England)
|December 15, 2005
Summary
Neat grinding and solvent-drop grinding effectively screen for crystalline salt formation potential between acid-base pairs. These methods were validated using two pharmaceutical compounds, showing promise for predicting salt formation.
Area of Science:
- Pharmaceutical Science
- Solid-State Chemistry
Background:
- Crystalline salt formation is crucial for optimizing pharmaceutical properties.
- Predicting salt formation requires efficient screening methods.
Purpose of the Study:
- To evaluate neat grinding and solvent-drop grinding as screening tools for crystalline salt formation.
- To demonstrate the applicability of these methods using model pharmaceuticals.
Main Methods:
- Neat grinding: mechanical force applied to solid acid-base pairs.
- Solvent-drop grinding: addition of a small amount of solvent to facilitate grinding.
Main Results:
- Both neat grinding and solvent-drop grinding successfully indicated the potential for crystalline salt formation.
- The methods proved effective for the tested acid-base pairs involving model pharmaceuticals.
Conclusions:
- Neat grinding and solvent-drop grinding are valuable, rapid screening techniques for assessing crystalline salt formation.
- These methods can aid in the early selection of appropriate salt forms for pharmaceutical development.