Relationship between lactone ratios of 9-nitrocamptothecin and their lactone/carboxylate equilibria in vitro and in vivo

 

Autores
Chen, Jun; Hu, Rongrong; Yang, Xixiong; Tian, Rong; Gu, Wei; Chen, Zhipeng; Cai, Baochang
Tipo de recurso
artículo
Estado
Versión publicada
Año de publicación
2012
País
Argentina
Institución
Universidad Nacional de La Plata
Repositorio
SEDICI (UNLP)
Descripción
The aim of this study was to evaluate the effect of lactone ratios on the lactone/carboxylate equilibria of 9-nitrocamptothecin (9-NC) in vitro and in vivo. The interconversion of lactone and carboxylate forms of 9-NC was studied. Then the lactone ratio vs time profiles of these 9-NC solutions were further investigated in pH 7.4 PBS, rat plasma and blood. 9-NC solutions with different lactone ratios (lactone ratios=100 %, 75 %, 50 %, 25 % and 0 %, respectively) were obtained by modifying the pH of solution and it was found that the effects on lactone/carboxylate equilibrium were in the order: blood cells > plasma albumin > pH. After i.v. administration, between the groups of 100 % and 75 % lactone ratios, the AUC0-t values of lactone 9-NC were almost equal. Therefore, there might be no difference between the anticancer activities of 9-NC solution in the range of 75~100 % lactone ratios.
Idioma
inglés
OAI Identifier
oai:sedici.unlp.edu.ar:10915/25743
Enlace del recurso
http://sedici.unlp.edu.ar/handle/10915/25743
http://hdl.handle.net/10915/25743
http://www.latamjpharm.org/resumenes/31/7/LAJOP_31_7_1_10.pdf
Nivel de acceso
Acceso abierto
Materia
Farmacia
9-nitrocamptothecin
Intravenous injection
Lactone
Pharmacokinetics