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What pKa, logP and solubility can tell you about biopharmaceutics classification
1st July 2008, The Hatton, at etc. venues, London.
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By reviewing carefully measured values for pKa, logP and solubility of about 100 drugs, one can observe useful relationships that provide great insight. Our goal during this workshop will be to explain the behaviour of different classes of compounds and show how these important physicochemical properties correlate with observed biopharmaceutics classification categories. Compounds with enhanced BBB penetration and those with active transport will be noted. Trends will be seen between hydrogen bonding capacity and melting point and their effect on solubility and lipophilicity. Precipitation and dissolution rates will be discussed and their influence on absorption. We will learn how the properties were measured and the consequences of using predicted properties. Finally, we will look at the ability of compounds to supersaturate in solution and discuss possible implications for formulation and how a compound can be moved from one BCS class to another BCS class.
About the Workshop Leaders:  | John Comer co-founded Sirius Analytical Instruments in 1990. Sirius develops and manufactures instruments for the measurement of drug pKa, lipophilicity and solubility, and provides analytical services. He is now the Sirius’ Technical Director, leading a team of Chemists and Software Engineers who are researching into novel aspects of the measurement of physicochemical properties of drugs and other small organic molecules. He has written numerous papers and chapters in the field. John obtained a BSc in Molecular Science from the University of Warwick (UK) and a MSc in Electrochemistry from University of Newcastle upon Tyne (UK). |  | 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, the successful development of new instrumentation and assays for physicochemical property determination, and has been involved with 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). |
About the Organisation: Sirius Analytical Instruments Ltd. specialises in designing and manufacturing unique analytical instrumentation for the pharmaceutical industry. Sirius instruments provide accurate and reliable values for physicochemical parameters such as pKa, logP and solubility (new method, patent applied for), using methods based on pH-metric approaches, pH/UV or liquid-liquid chromatography. 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 physicochemical parameters. Sirius also provides a high quality of standard and customer bespoke analytical service.
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Would your organisation be interested in running an Executive Briefing at a future SMi event?
Executive Briefings are interactive one- or half-day sessions which are attached to a specific conference and are run, on average with between 5 and 10 delegates, to explore a highly-focussed and niche aspect of the overall topic. Running an SMi workshop guarantees you one-to-one access with executives who have actively expressed a keen interest in the subject matter, giving you an excellent opportunity to promote your organisation to your target market.
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