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Thermal Analysis - Articles and news items
Webinars / 4 February 2016 /
In this Webinar, we will discuss the basic principles of DSC purity determination and present some interesting applications…
Whitepapers / 15 January 2016 / Dr. Matthias Wagner, Product Manager, Mettler Toledo
Heated crystalline pharmaceutical compounds undergo morphological changes that can be observed under a microscope. With hot-stage microscopy changes in melting points and ranges or crystallisation can be visualised for research and QC purposes in order to influence drug stability or effectiveness…
Webinars / 2 December 2015 /
In this Webinar, we discuss the basic principles of validation, from equipment qualification and computerised system validation through to analytical method validation…
Principles of Differential Scanning Calorimetry (DSC) – the most used thermal analysis technique in pharmaceuticals
Webinars / 18 September 2015 /
In this Webinar, we discuss the basic principles of Differential Scanning Calorimetry (DSC) – the most used thermal analysis technique in pharmaceuticals…
Supplier news / 10 August 2015 / Mettler Toledo
METTLER TOLEDO is pleased to introduce two new products to the Thermal Analysis Premium portfolio, the DSC3+ and TGA/DSC 3+, for superior results on the most demanding applications…
Webinars / 13 July 2015 / Mettler Toledo
In this webinar, we discuss the basics of calibration and adjustment in thermal analysis whilst offering some useful tips and hints…
Webinars / 26 April 2015 /
Our experts demonstrate how thermal analysis is used to investigate pharmaceutical substances, presenting some typical examples measured by DSC, TGA, TMA or DMA…
Thermally Stimulated Current Spectroscopy (TSC) is a new tool that can be used to analyse pharmaceutically important molecules. TSC studies are usually conducted to provide additional information about molecular mobility in the solid state, and as a result characterise phase transitions that are related to thermal transitions in the crystalline (polymorphic) and amorphous phases. The ability of TSC to probe molecular mobilities, previously undetected in materials, and link them to the stability of different phases has sparked immense scientific interest in this technique.
In the last 10 years, the pharmaceutical market has seen a significant decrease in approved new drug entities. Although many factors may be responsible for this trend, one of them is insufficient information / characterisation of a lead molecule. Consequently, new techniques are often applied in the pharmaceutical field with the simple goal to aid better selection of the drug candidate and dosage form.
Improving the performance of existing drug products is another goal that often requires comprehensive information about the properties of the drug molecules. In recent years, the physical sciences have made great progress towards understanding the properties of pharmaceutically important amorphous and polymorphic materials. The major focus of this work is to utilise the advantages that they may bring to formulated products (e.g. faster solubility of amorphous drugs compared to crystalline counterparts) and at the same time to overcome stability problems (e.g. tendency to recrystallise on storage) that they may demonstrate.
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 chance of producing successful drugs1. This interest has been assisted both by improvements in instrumentation as well as evidence that thermodynamically and kinetically optimised compounds fare better in the clinic2.
Optimisation of the binding affinity, which may have to be improved by several orders of magnitude from initial hit to drug molecule, can be achieved by modifying the individual thermodynamic and kinetic contributions. However, medicinal chemists have, up to now, been reluctant to consider these measurements during hit selection and lead optimisation, because it has been difficult to understand how the different design strategies affect the individual forces resulting in different thermodynamic and kinetic profiles. By incorporating both retrospective analysis and real time data collection in active projects, the value of using these fundamental contributions to guide the selection of chemical start points and how they can be used to influence optimisation strategies will become clear.
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.
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 very few samples that cannot be investigated.
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 progression of micro or nanotechnologies, combinations of different hyphenated techniques, as well as the development of high automated or high throughput systems, the faster new horizons will open in the industrial environment. In addition, the application of sophisticated kinetic software in DSC, calorimetry and reaction calorimetry gives better safety predictions.
ABB Analytical Measurement ABL&E Group ABS Laboratories ACD/Labs ADInstruments Ltd Analytik Jena AG Andor Technology Axis-Shield Diagnostics Ltd Bachem AG Bio-Rad Laboratories Biopharma Group Black Swan Analysis Limited CAMO Software AS Celsis International Charles Ischi AG | Kraemer Elekronik ChemAxon Cherwell Laboratories CI Precision Cobalt Light Systems Comark Instruments Edinburgh Instruments EUROGENTEC F.P.S. Food and Pharma Systems Srl IONICON Analytik GmbH kbiosystems ltd L.B. Bohle Maschinen + Verfahren GmbH LabWare Linkam Scientific Instruments Limited MKS Umetrics Nanosurf New England Biolabs, Inc. Panasonic Biomedical Sales Europe B.V. PerkinElmer Inc Portalis Ltd Powder Systems Limited (PSL) Reach Separations ReAgent Source BioScience Spectrum®Labs.com Stratech Scientific Limited Takara Clontech Thermal Detection Ltd. Tuttnauer Vaisala Ltd Waters Corporation Watson-Marlow Fluid Technology Group Wickham Laboratories Limited Xylem Analytics Ytron-Quadro (UK) Limited Yusen Logistics