Acetaminophen Prodrug: Microwave-Assisted Synthesis and in vitro Metabolism Evaluation by Mass Spectrometry

Autor: Murie,Valter E., Marques,Lucas M. M., Souza,Glória E. P., Oliveira,Anderson R. M., Lopes,Norberto P., Clososki,Giuliano C.
Jazyk: angličtina
Rok vydání: 2016
Předmět:
Zdroj: Journal of the Brazilian Chemical Society, Volume: 27, Issue: 6, Pages: 1121-1128, Published: JUN 2016
Journal of the Brazilian Chemical Society v.27 n.6 2016
Journal of the Brazilian Chemical Society
Sociedade Brasileira de Química (SBQ)
instacron:SBQ
Popis: Propacetamol is an acetaminophen prodrug of intravenous administration used to control fever and pain of perioperative period in multimodal analgesia therapy. After injection, it is completely converted by plasma esterases into N,N-diethylglycine and acetaminophen, its active metabolite whose mechanism of action is the inhibition of prostaglandin synthesis. Herein, we report an improved protocol for the synthesis of propacetamol hydrochloride that allows the isolation of the active pharmaceutical ingredient (API) with high purity and yield. In addition, the in vitro metabolism of propacetamol in a microssomal reaction was evaluated by ion trap tandem mass spectrometry.
Databáze: OpenAIRE