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Polymorphs - Articles and news items

How the implementation of Exalt™ for evaporative crystallisation studies improves stability and controlled delivery in drug development.

How the implementation of Exalt™ for evaporative crystallisation studies improves stability and controlled delivery in drug development.

Supplier news / 12 July 2016 / Biopharma Group

Polymorph screening is an important stage of drug development. The aim is to identify the different crystalline structures or polymorphs that a drug may appropriate…

New technique for fast low-level polymorph API quantification using non-destructive transmission Raman spectroscopy

New technique for fast low-level polymorph API quantification using non-destructive transmission Raman spectroscopy

Supplier news / 27 May 2016 / Cobalt Light Systems

A new technique for measuring low-levels of crystalline polymorphic materials offers many advantages over industry standard techniques….

Kaiser whitepaper - Monitoring a Pharmaceutical Crystal Transformation In Situ

Whitepaper: Monitoring a pharmaceutical crystal transformation in situ

Whitepapers / 1 March 2016 / Kaiser Optical Systems Inc.

Many organic compounds can crystallize in several different forms called polymorphs…

Improving solubility with promiscuous multi-component drug crystals

Improving solubility with promiscuous multi-component drug crystals

Issue 5 2015, Polymers / 22 October 2015 / Masataka Ito, Kiyohiko Sugano and Katsuhide Terada Faculty of Pharmaceutical Sciences, Toho University

The physicochemical properties of active pharmaceutical ingredients (APIs) are critical to the success of drug development. Most of the APIs in oral solid dosage forms are contained as drug crystals. Drug crystals can be categorised as single and multiple component systems, the latter of which include salts, co-crystals and solvates. When the solvent is water, the drug solvate is referred to as a hydrate. Salts formation is defined as proton transfer from a drug molecule to a guest molecule and the guest molecule (i.e., a counter-ion) is bonded to the drug molecule (i.e., a drug) by one or several ionic bonds. In a co-crystal and a solvate, a guest molecule (a co-crystal co-former or a solvent) is bonded to the drug via inter-molecular interactions other than the ionic bond, such as with hydrogen bonds. Co-crystal co-formers are non-volatile molecules at ambient conditions. In most cases, the drug solvates of APIs are hydrates; however, they can be organic solvents…

Terry Threlfall, Senior Research Fellow, University of Southampton

Polymorphism – Polymorph myths and misperceptions

Issue 3 2014, Polymers / 3 July 2014 / Terry Threlfall, Senior Research Fellow, University of Southampton

The past quarter of a century has seen an enormous increase in the number of papers on the behaviour of the organic solid state, particularly those concerning pharmaceutical polymorphs and solvates. High profile patent cases (ranitidine hydrochloride, paroxetine hydrochloride) combined with product polymorph issues (ritonavir), all of which have carried astronomical monetary implications have undoubtedly contributed to this proliferation. This increasing awareness and accessibility of polymorph information has been unfortunately accompanied by illusions about polymorphs and their behaviour. Since this is not a witch-hunt, references to examples of gross misunderstandings will not be provided, but many examples will be seen by the observant…

 

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