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Synthesis of haloperidol prodrugs and their hydrolysis by porcine liver esterase

Morris, Andrew, Brain, Keith Roger and Heard, Charles Martin 2008. Synthesis of haloperidol prodrugs and their hydrolysis by porcine liver esterase. Drug Metabolism Letters 2 (4) , pp. 275-279. 10.2174/187231208786734111

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Abstract

In probing enhancement of the transdermal delivery of the anti-psychotic drug haloperidol, five prodrugs (ethanoate, propanoate, butanoate, octanoate and decanoate) were synthesised and their relative rates of hydrolysis determined in the presence of porcine liver esterase (PLE), a model for cutaneous esterases. H NMR, MS and elemental analysis confirmed the successful synthesis of each prodrug in high purity, and each was found to hydrolyse in the presence of PLE with the hydrolytic rate reaching a maximum with haloperidol octanoate (C8) at 2.31 ± 0.06 nmol ml- h- (p < 0.001).

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Subjects: R Medicine > RS Pharmacy and materia medica
ISSN: 1872-3128
Last Modified: 04 Jun 2017 06:29
URI: http://orca.cf.ac.uk/id/eprint/60728

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