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Issue 26, 2014
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From discovery to scale-up: α-lipoic acid : nicotinamide co-crystals in a continuous oscillatory baffled crystalliser

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Abstract

The crystalline nutritional supplement α-lipoic acid degrades rapidly on exposure to temperatures above its melting point 65 °C and to light. A small-scale experimental co-crystal screen has produced three novel co-crystals of α-lipoic acid that each display enhanced thermal stability and differences in aqueous solubilities compared to α-lipoic acid. In each case, the initial screening procedure produced tens of milligrams of material enabling initial identification, characterisation and crystal structure determination. The structure of the α-lipoic acid : nicotinamide co-crystal was determined by single crystal X-ray diffraction and used for subsequent phase identification. Scale-up of the co-crystallisation process of α-lipoic acid with nicotinamide was then investigated in a continuous oscillatory baffled crystalliser. Over 1 kg of solid co-crystals was produced using a continuous crystallisation process in a continuous oscillatory baffled crystalliser at a throughput of 350 g h−1 yielding a purity of 99% demonstrating this as an effective route to rapid scale-up of a novel co-crystal system.

Graphical abstract: From discovery to scale-up: α-lipoic acid : nicotinamide co-crystals in a continuous oscillatory baffled crystalliser

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Supplementary files

Article information


Submitted
21 Jan 2014
Accepted
04 Mar 2014
First published
04 Mar 2014

CrystEngComm, 2014,16, 5769-5780
Article type
Paper
Author version available

From discovery to scale-up: α-lipoic acid : nicotinamide co-crystals in a continuous oscillatory baffled crystalliser

L. Zhao, V. Raval, N. E. B. Briggs, R. M. Bhardwaj, T. McGlone, I. D. H. Oswald and A. J. Florence, CrystEngComm, 2014, 16, 5769 DOI: 10.1039/C4CE00154K

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