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| home > epc > autumn 2004 > physical characterisation of powders. why has it become so important and what advances have occurred? |
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European Pharmaceutical Contractor
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The desire to characterise the physical properties of materials has swelled in recent years: in this article the reasons for this shift are considered, along with some of the advances in measurement techniques. Amongst the main reasons for increased interest are: the change in the process of NCE development; the demands of different drug delivery routes; the awareness of regulators; the increased awareness of how physical form can be protected as intellectual property; the improvement in the measurement techniques that are available; and a better understanding of what they show.
Changes in the Development of NCEs
Multinationals are anxious to decrease the time between filing a patent and launching a product, and this has resulted in the use of combinatorial chemistry, high-throughput screening and new views over what would constitute a development candidate. In an ideal world, combinatorial chemistry will yield a plentiful supply of candidates. These will subsequently be checked for activity and toxicity, followed by a preformulation screening, all on very small quantities of drug. The feedback will produce optimised candidates and rapid development. This is, of course, the ideal scenario.
In reality, there are few reports of combinatorial chemistry yielding great successes as yet, but certainly it has focused minds and improved both the thought processes and the science of candidate screening for developability. The desired properties have been known for a long time; the drug should be active, safe, chemically stable; have some aqueous solubility (preferably more than 10mg/ml); and have a dose that will allow easy manufacture (not so small as to give mixing problems, not so big that it can influence compact formation and so on).
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By Professor Graham Buckton, Chief Executive Officer of Pharmaterials Ltd
Professor Graham Buckton is Chief Executive Officer of Pharmaterials Ltd. Having joined the staff of King's College London as a Lecturer in Pharmacy in 1984, in 1989 he moved to the School of Pharmacy, University of London. Recognised for his use of isothermal microcalorimetry and vapour sorption techniques to assess the physical properties of materials, Professor Buckton now has a large research group of postgraduate and postdoctoral scientists, whose research relates to the amorphous state, powder processing, surface science, solid oral dosage forms, inhalation drug delivery and modified release dosage forms. Professor Buckton has received, among others, the Pfizer award and the British Pharmaceutical Conference Science Medal. He is also Editor of the International Journal of Pharmaceutics and is a past Chairman of the Pharmaceutical Sciences Group of the Royal Pharmaceutical Society.
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