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OVERVIEW
This master class will review the lipophilicity and solubility behaviour of ionisable marketed drugs and look at their location in the biopharmaceutics classification system (BCS). Compounds with enhanced BBB penetration and those with active transport will be noted. Trends will be observed between hydrogen bonding capacity and melting point and their effect on solubility and crystallisation behaviour. Methods will be described for determination of kinetic and intrinsic solubility and how to assess the amount of supersaturation present in the system by studying precipitation events. We will study the effects of bio-relevant media (e.g., simulated intestinal fluids) on solubility behaviour. Finally, we will demonstrate solubility enhancement in the presence of formulation excipients and how this could be used as a potential opportunity for promoting a molecules BCS class.
ABOUT THE MASTER CLASS LEADERS
Karl Box
Karl Box is the Scientific Team Leader at Sirius and one of the inventors of the CheqSol method for solubility measurement. He has been with Sirius since 1993 and is an expert in the field of physicochemical measurements. During this time he has been involved in running an Analytical Service Laboratory, customer training and installations, successful development of new instrumentation and assays for physicochemical property determination, and involvement in property prediction software. Karl has over 20 peer reviewed publications in scientific journals and is an experienced speaker. Karl obtained a BSc in Chemistry from the University of Bath (UK).
Jon Mole
Jon Mole obtained his Chemistry degree at the University of Bath and joined Sirius in 2002 as an application chemist, running samples on in-house instruments for Sirius’ Analytical Service. He also took up a role in providing customer support and training for users of the Sirius products for pKa, logP, solubility and dissolution measurement. Jon has installed instruments worldwide, provided training and support to hundreds of Sirius clients, and analysed thousands of drug compounds with Sirius’ analytical service. From 2008 he has taken on a new role as Sirius Technical Sales Manager, with overall responsibility for Sirius’ worldwide sales efforts.
ABOUT SIRIUS ANALYTICAL
Sirius Analytical Ltd specialize in designing and manufacturing unique analytical instrumentation for the pharmaceutical industry. Sirius instruments provide accurate and reliable values for pKa, logP, logD, solubility and dissolution, using methods based on highly automated potentiometric and spectroscopic titration. The ability of New Chemical Entities to cross biological membranes such as the gastro-intestinal tract, blood-brain barrier, skin and cell walls in general, depends on these critical physicochemical parameters. Sirius also offer an analytical service for high quality physchem outsourcing, used by thousands of clients worldwide.
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