1. Physical Sciences
2013

2. Solid State Services
Polymorph
Polymorph
screens
screens
Preformulation
Preformulation Salt/Cocrystal
Salt/Cocrystal
support
support screens
screens
Routine Amorphous
Routine Solid state
Solid state Amorphous
physicochemical
physicochemical dispersion
dispersion
testing services
services screens
testing screens
Drug substance
Drug substance Crystallisation
Crystallisation
and drug product
and drug product development
development
trouble shooting
trouble shooting
Legal
Legal
support
support
2

3. Purpose
ALMAC Solid
Chemistry Formulation
state
group
Our solid state group acts as a link, for the seamless
transfer of knowledge and understanding of the API
between chemistry and formulation
3

4. Adding value
Form Selection Process development
•Screens for polymorphs, •Crystallization issues
salts, cocrystals and
amorphous forms •Crystal shape / PSD control
•Identify the best physical form •Solid-liquid separation
for development
•Form robustness
•Detailed interpretive report
with recommendations
Product development Scale up
•Purity
•API robustness to process
conditions •Yield
•Qualitative and quantitative •Solvent efficiency
determination of physical form
in dosage forms
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5. Adding value
Range of expert services – Analytical,
biologics, pre-formulation, and
formulation.
Faster and smarter solutions
Efficient development timelines
Producing enhanced products
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6. Almac Advantage
• Vast experience and knowledge gained from years of
industry experience
• Clients range from virtual companies to multinationals
• Studies designed to the customer needs and API
properties
• Significant expertise in supporting Discovery and Early
Clinical phase development projects
• Excellent understanding of the requirements for process
development and drug product development
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7. In house Technologies
formufast™
rapid formulation micro screens for preclinical formulations
• Ideal for use where material is limited
• Identify excipients based on solubilising capacity
• A rational formulation development program for poorly soluble drugs
• The risks associated with drug precipitation can be minimised.
• Not just solubility in media, but the solubilising capacity in the GI tract
The following screens are available
• formufast™ PO
• formufast™ IV
• formufast™ SD
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8. Research at Almac
• PhD sponsored at QUB titled - Raman studies of the formation and
structure of pharmaceutically relevant crystals.
• Identified the following
– Crystal orientation was identified to effect the reproducibility of Raman data, investigated
methods to remove these effects.
– PCA identified a consistent component which is strongly indicative of the presence of nuclei
at the preliminary stages of crystal formation.
– XRD / Raman the combination of these two techniques provides valuable information about
the crystal.
Excitation
Crystal
Excitation
Solution
Ex
1600 1400 1200 1000 800 600 400 cit
at ion
XXII International Conference On Raman Spectroscopy, Volume 1267, 724-725, 2010
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9. Research at Almac
• Cocrystals are unique crystalline solids made from stoichiometric
amounts of API and pharmaceutically-acceptable coformers
• New, patentable solid forms that can exhibit improved properties
– Crystallinity, solubility, stability, flow properties, hygroscopicity
• Study to improve solubility/BA of poorly soluble Fenamic acids
– Pharmaceutically-acceptable coformers selected
– Screening generated cocrystals for several fenamic acids with different
coformers
• Improved aqueous stability of cocrystals
• Robust crystallisations developed using phase diagrams
Crystal Growth & Design, 11(8), 3522-3528, 2011
9

10. Research at Almac
• Cocrystals are unique crystalline solids made from stoichiometric
amounts of API and pharmaceutically-acceptable coformers
• New, patentable solid forms that can exhibit improved properties
– Crystallinity, solubility, stability, flow properties, hygroscopicity
• Study to improve solubility/BA of poorly soluble Fenamic acids
– Pharmaceutically-acceptable coformers selected
– Screening generated cocrystals for several fenamic acids with different
coformers
• Improved aqueous stability of cocrystals
• Robust crystallisations developed using phase diagrams
Crystal Growth & Design, 11(8), 3522-3528, 2011
9