List view / Grid view
31 August 2011 | By Geoff Holdgate, AstraZeneca
Recently, there has been renewed interest in using thermodynamic and kinetic data, alongside empirical rules (particularly focused upon cLogP and molecular weight) and guiding metrics such as ligand efficiency and lipophilic ligand efficiency developed for fragments, leads and drugs in order to facilitate the design of compounds with a greater…
7 February 2009 | By
During the optimisation of drug candidates, improvements in affinity and selectivity play a critical role. This task is usually accomplished by establishing accurate correlations between the affinity/selectivity of different chemical scaffolds and through chemical modifications to a selected scaffold.
2 August 2008 | By
Differential scanning calorimetry (DSC) is a widely used technique within the pharmaceutical industry because the range of phase transitions it can measure usually allows near complete physical characterisation of a new active principal early during preformulation. In addition, because DSC measures a property change that is ubiquitous† (heat) there are…
19 March 2008 | By Danielle Giron, Chemical Research & Development, Novartis Pharma AG, Basel, Switzerland
Thermal analysis techniques cover all methods in which a physical property is monitored as a function of temperature or time, whilst the sample is being heated or cooled under controlled conditions. Calorimetric methods measure the energy involved in every process. The quicker new developments attain the market, such as the…
23 November 2007 | By
The determination of accurate thermodynamic data for the interactions of biomolecules has been enhanced over the last decade by the use of isothermal titration calorimetric (ITC) instrumentation. These instruments are now standard kits in many biophysical/structural biochemistry laboratories of pharmaceutical companies. Despite this, there is little evidence for the input…
21 September 2007 | By Dr Ernesto Freire, Faculty Professor, Johns Hopkins University, Baltimore
Drug development involves the identification and subsequent optimisation of low molecular weight compounds with a desired biological activity. Often, the initial binding affinity of those compounds towards their intended target needs to be improved by five or more orders of magnitude before they become viable drug candidates; a process that…
23 May 2007 | By Simon Gaisford PhD and Rita Ramos PhD, School of Pharmacy, University of London
In the previous article (European Pharmaceutical Review, Issue 2, 2007) an introduction to calorimetry was given and its application to polymorph characterisation, discussed. Another area of application of growing importance is quantification of (usually small) amorphous contents. A requirement to demonstrate the presence or absence of amorphous material is becoming…
27 March 2007 | By Simon Gaisford PhD., School of Pharmacy, University of London and Michael AA O’Neill PhD., Department of Pharmacy and Pharmacology, University of Bath
Characterising the properties of a material, understanding how these properties change in relation to local environment and quantifying potential interactions with other species are facets central to any drug development programme. Not understanding and, more importantly, not controlling these factors can have serious consequences for a pharmaceutical, from irreproducible processing…
28 September 2006 | By Dr Danielle Giron, President, Swiss Society for Thermal Analysis & Calorimetry
Thermal analysis methods and coupled techniques are well established procedures in material science. Due to the different information delivered, thermal analysis methods are concurrent or complementary to other analytical techniques such as spectroscopy, chromatography, melting point determination, loss on drying, assay, for identification, purity and quantitation. They are basic methods…
20 July 2006 | By Prof. P. A. Barnes, School of Applied Sciences, Prof. E. L. Charsley, Head of the Centre for Thermal Studies and Dr G. M. B. Parkes, Senior Lecturer in Analytical Science, University of Huddersfield
The determination of the key physical and chemical properties of a new material is essential. The melting point, glass transition temperature, the number and identification of the different phases it may have, and the temperatures at which they are formed are all of great value, not only in assessing its…
11 November 2005 | By Dr Paul G. Royall, Lecturer in Pharmaceutics, School of Chemical Sciences & Pharmacy University of East Anglia, See-wah Jai Tang, Pharmaceutical Science Research Division, King’s College London
Thermal analysis equipment can be found in nearly all of the analytical, development, formulation and QA laboratories within the pharmaceutical industry. However, these work horse instruments are learning to run faster and to analyse an ever more varied field of samples.
