Event preview: Crystalline form and drug delivery
Connecting chemistry and drug development, 8 November 2007
 During drug development, oral bioavailability, chemical stability and patent protection are three important factors that are strongly influenced by the crystalline form and solubility of the active pharmaceutical ingredient (API). Unsurprisingly, crystalline form has for many years figured prominently in the nightmares of industrial chemists and pharmacists. For example, in 1998 the supply of the new HIV protease inhibitor, Ritonavir (pictured), was seriously threatened by the appearance of a different crystalline form (polymorph) during the manufacturing process. This new polymorph of Ritonavir exhibited slower aqueous dissolution kinetics and therefore a potentially different oral absorption profile to the original crystalline form. Much to the relief of patients, heroic efforts by pharmaceutical scientists enabled a potentially disastrous situation to be averted.
Today, polymorph screening, salt selection, solubility measurement and formulation are being addressed earlier in the discovery and development process in order to avert such situations arising.
Consequently, medicinal and development chemists are working ever more closely with colleagues in pharmaceutical development in order to optimise the solid form of lead compounds and drug candidates.
‘What a chemist needs to know about crystalline form and drug delivery’ (pdf flyer) is a one day meeting organised by the SCI’s fine chemicals group, to be held at SCI international headquarters on 8 November 2007. Presentations are aimed at medicinal and development chemists who would like to learn more about this area. Attendees will hear leaders in the field of solid form characterisation, salt selection and formulation speaking on the current state of the art.
The objective of this meeting is to bridge the interface between R&D chemistry and pharmaceutical development, thus leaving attendees better equipped to interact with multi-disciplinary project teams.
Roger Davey (University of Manchester) and Chris Frampton (CSO-Pharmorphix) will discuss key aspects of solid form and polymorphism during the drug discovery and development process. Christoph Saal (Merck KGaA) and James Butler (GSK) will discuss modern salt selection and formulation strategies for poorly soluble compounds. Further examples of how these drug delivery strategies have been applied will be presented as case studies by Steve Cosgrove (AstraZeneca).
Organised by: Steven Howard,
SCI Fine Chemicals Group
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