Synthesis of haloperidol prodrugs and their hydrolysis by porcine liver esterase

Morris, Andrew ORCID: https://orcid.org/0000-0002-6315-7553, Brain, Keith Roger and Heard, Charles Martin ORCID: https://orcid.org/0000-0001-9703-9777 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:	Schools > Pharmacy
Subjects:	R Medicine > RS Pharmacy and materia medica
ISSN:	1872-3128
Last Modified:	25 Oct 2022 09:59
URI:	https://orca.cardiff.ac.uk/id/eprint/60728

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