2. Academic Validation
  3. Pharmacological evaluation and preliminary pharmacokinetics studies of a new diclofenac prodrug without gastric ulceration effect

Pharmacological evaluation and preliminary pharmacokinetics studies of a new diclofenac prodrug without gastric ulceration effect

  • Int J Mol Sci. 2012 Nov 19;13(11):15305-20. doi: 10.3390/ijms131115305.
Jean Leandro Dos Santos 1,  Vanessa Moreira,  Michel Leandro Campos,  Rafael Consolin Chelucci,  Karina Pereira Barbieri,  Pollyana Cristina Maggio de Castro Souto,  Márcio Hideki Matsubara,  Catarina Teixeira,  Priscila Longhin Bosquesi,  Rosângela Gonçalves Peccinini,  Chung Man Chin
Affiliations

Affiliation

  • 1 Lapdesf-Laboratory of Research and Drug Development, Drugs and Medicines Department, School of Pharmaceutical Science-UNESP Rodovia Araraquara Jaú Km. 01, 14801-902, Araraquara, SP, Brazil. santosjl@fcfar.unesp.br.
PMID: 23203127 DOI: 10.3390/ijms131115305
Abstract

Long-term nonsteroidal anti-inflammatory drugs (NSAIDs) therapy has been associated with several adverse effects such as gastric ulceration and cardiovascular events. Among the molecular modifications strategies, the prodrug approach is a useful tool to discover new safe NSAIDs. The 1-(2,6-dichlorophenyl)indolin-2-one is a diclofenac prodrug which demonstrated relevant anti-inflammatory properties without gastro ulceration effect. In addition, the prodrug decreases PGE(2) levels, COX-2 expression and cellular influx into peritoneal cavity induced by carrageenan treatment. Preliminary pharmacokinetic studies have shown in vivo bioconversion of prodrug to diclofenac. This prodrug is a new nonulcerogenic NSAID useful to treat inflammatory events by long-term therapy.

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