The higher the dissolution rate, the higher an API’s effectiveness. Yet due to their chemical structure a large percentage of new and existing APIs are poorly water soluble. This presentation examines whether a new granulation technique developed by Ghent University has the potential to improve dissolution rates and obtain supersaturated API solutions.

1. Can improved water solubility
give API’s a new lease of life?
Dr. Jef Verplaetse
Managing Director/Owner
Laboratoria Smeets
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2. API Solubility: Importance
Solubility: Water solubility is important. Biological fluids are water-based
systems. Any biological absorption happens in a water
rich environment. Hence water is the solvent of choice for liquid
pharmaceutical formulations.
Rate of Dissolution: Important for practical reasons. If an API takes hours to
dissolve, it is not practical mainly for administration via drinking water.
Bioavailability: Essential for therapeutic effectiveness.
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3. API Solubility: Techniques
Physical modification:
• Particle Size
• Crystalline structure modification
• Drug dispersion in carriers
• Use of surfactants
Chemical modification:
• pH – use of buffers
• Salt formation
• Chemical derivate
Others:
• Co-crystallisation
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4. API Solubility: Benefits
• Continuous granulation process and also
small batches possible
• Pharmaceutically acceptable excipients
• Low temperature operation
• No up-scaling of production process
necessary (Time is the only variable)
• Drug loading: up to 60%
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5. API Solubility: Markets
Veterinary Market
• Medicated drinking water (antibiotics,
analgesics, monensin)
Human Market
• Water soluble for oral delivery, improving
bioavailability
Potential For Old Molecules
• New application enables new stage in life
cycle
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6. API Solubility: Methods
Twin Screw Thermofisher 24mm
• Screw profile : two kneading blocks
• Separate entry for liquids.
Blending
• Powder fraction : PEG 4000 (Melting point between 45.2 C - 67.2 C)
• Maltodextrin
• API
• Liquid fraction
• PEG 400 (Helps to lower melting point of the PEG 4000)
• Tween
Extrusion
• First powder blend then liquid fed into the second kneading block.
• Operating temperature max 50 C
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7. API Solubility: Conclusion
Continuous granulation creates new opportunities
Collaboration between Ghent University, Orotech and Laboratoria Smeets
will lead to more innovative projects
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8. Find Out More…
To learn more about API solubility please join our
FREE webinar on 17.10.13
http://bit.ly/17ggQLi
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9. CONTACT
Kate Marston
WTG Webinars
www.wtgwebinars.com
+44 (0) 20 7202 7705
Kate.marston@wtgevents.com
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