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Efficient Screening of Pharmaceutical Cocrystals by Microspacing In-Air Sublimation
Huimin Li1, Lei Wang1, Xin Ye1
1State Key Laboratory of Crystal Materials, Institute of Crystal Materials, Shandong University, Jinan 250100, P. R. China.
Journal of the American Chemical Society
|April 17, 2024
Summary
Microspacing in-air sublimation (MAS) rapidly screens pharmaceutical cocrystals and grows high-quality single crystals. This user-friendly method, effective for thermolabile molecules, discovered a novel favipiravir-salicylamide cocrystal with enhanced properties.
Area of Science:
- Pharmaceutical Science
- Materials Science
- Crystallography
Background:
- Cocrystal screening and single-crystal growth are critical but challenging steps in pharmaceutical development.
- Existing methods often face limitations in speed, efficiency, and applicability to thermolabile compounds.
Purpose of the Study:
- To introduce a novel, rapid, and versatile method for pharmaceutical cocrystal screening and single-crystal growth.
- To demonstrate the efficacy of the new method for both drug-drug cocrystals and cocrystals of active pharmaceutical ingredients with common coformers.
Main Methods:
- Development and application of microspacing in-air sublimation (MAS) for cocrystal formation and single-crystal growth.
- Precise control of growth temperature and distance to optimize crystal cultivation.
- Structural determination of newly discovered cocrystals.
Main Results:
- Successful discovery and rapid single-crystal growth of a novel favipiravir (FPV)-salicylamide (SAA) drug-drug cocrystal with improved physiochemical properties.
- Efficient cultivation of single crystals for FPV-isonicotinamide, FPV-urea, FPV-nicotinamide, and FPV-tromethamine cocrystals, with structures determined for the first time.
- Versatile application demonstrated by achieving single crystals of 10 different paracetamol and piracetam cocrystals.
Conclusions:
- Microspacing in-air sublimation (MAS) offers a highly efficient, user-friendly, and versatile approach for pharmaceutical cocrystal screening and single-crystal growth.
- The MAS method is particularly advantageous for handling thermolabile molecules and accelerating the discovery of novel cocrystals.
- This technique significantly advances the development pipeline for new cocrystal forms of existing and novel pharmaceutical compounds.
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