Improvements in physicochemical properties can be achieved by altering the physical forms of a given compound such as polymorphs, solvates, amorphous, salts, cocrystals, and/or hydrates, etc.
At APSL, we have over 20 years of experience in solid state science including polymorph screening and development, salt screening, enantiomeric screening, X-ray diffraction, crystallization, and amorphous dispersions.
Solvent screening
- Solvent screening
- Polymorph studies will be performed with the API material
- Solvent screening will be performed with the below solvents - ICH-3: Ethyl acetate, n- Butyl acetate, IPA, MTBE, MIBK, Acetone, Heptane, n-Butanol, IPAC and 2- Methyl THF, DMSO etc.
ICH-2: Acetonitrile, Dichloromethane, Hexane, Methanol, Tetrahydrofuran, Toluene, 1, 4-Dioxane, Di –Isopropyl ether, cyclohexane etc. - Detailed solvent screening at different temperatures to classify the solvents for Anti and co-solvents
- Solubility curve generation, identification of Metastable Zone Width (MSZW)
- The solubility studies are intended to be performed with ~95% pure material
Studies for polymorph screening and crystallization
Crystallization experiments would be attempted to understand the process conditions to get the different morphs. It could be either solvated, non-solvated, hydrated, or hemihydrate. Various crystallization techniques will be used for screening the solid forms:
- Cooling crystallization
- Anti-solvent crystallization
- Seeding crystallization (Seed point evaluation)
- Evaporative crystallization
Polymorph-slurry mediated transformations
Various forms of the test compounds will be subjected to slurry-mediated transformation studies in organic solvents which are having optimum solubility -
- Slurring media, volume, and solid content will be appropriately adjusted to make sure that always excess solid is present.
- Time points of the slurry experiments can be decided as per requirements. Solid forms that remained after slurring either in organic solvents or aqueous phase mixtures will be separated and will be subjected to solid-form characterization (PXRD, DSC, and TGA).
Polymorph or crystallization process optimization
- Crystallization process will be optimized with PAT like FBRM (Focused Beam Reflectance Measurement) which shows online particle counts and chord length distributions of the particles and PVM (Particle Vision Microscope) which shows online particle shape
- Process finalization to achieve desired yield and quality parameters
- ATFD studies if required, in case of amorphous forms and heat-sensitive materials
Optimization of filtration, drying and particle size distribution
- Filtration and drying studies from a scale-up point of view optimize the conditions
- Particle size distribution & milling studies shall be performed based on the requirement
- Stress studies for solids (polymorph stability with milling and micronation)
- We have all the associated lab and plant infrastructure with multi-mills, centrifuges, micronizes, and ANFDs
Why Aurigene Crystallization and Polymorphism Services?
Expertise and experience of 20+ years
Comprehensive infrastructure at lab and plant for a full suite of services
State-of-the-art PAT tools, and QbD approach to support optimization
Phase-appropriate development approach
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