Issue 37, 2013
From the journal:

RSC Advances

Novel N-5-(acyloxyalkoxy)carbonyl prodrugs of olanzapine with physicochemical properties for extended-release†

Laura C. Blumberg,*a   Tarek A. Zeidan,*a   Adrian Maddaford,b   Nicole C. Warrenb  and  Panee Hutchisonb  

* Corresponding authors

a Alkermes, Inc, 852 Winter St., Waltham, MA 02451, USA
E-mail: laura.blumberg@alkermes.com, tarek.zeidan@alkermes.com
Fax: 1-781-609-5200
Tel: 1-781-609-6428 (LB)

b Peakdale Molecular Ltd, Peakdale Science Park, Sheffield Road, Chapel-en-le-Frith, High Peak, UK

Abstract

An unexpected regioisomer was observed during the synthesis of olanzapine prodrugs. N-5-(acyloxyalkoxy)carbonyl-functionalized olanzapine derivatives were found to have favorable physicochemical properties, such as crystallinity, melting points, solubility and plasma conversion profiles suitable for formulation as extended-release injections.

Graphical abstract: Novel N-5-(acyloxyalkoxy)carbonyl prodrugs of olanzapine with physicochemical properties for extended-release

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Article information

DOI
https://doi.org/10.1039/C3RA41967C
Article type
Communication
Submitted
22 Apr 2013
Accepted
12 Jul 2013
First published
17 Jul 2013

RSC Adv., 2013,3, 16270-16278

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Novel N-5-(acyloxyalkoxy)carbonyl prodrugs of olanzapine with physicochemical properties for extended-release

L. C. Blumberg, T. A. Zeidan, A. Maddaford, N. C. Warren and P. Hutchison, RSC Adv., 2013, 3, 16270 DOI: 10.1039/C3RA41967C

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