The inhibitory effect of pluronic on P-glycoprotein drug pump / 药学学报
Acta Pharmaceutica Sinica
;
(12): 989-994, 2007.
Artigo
em Chinês
| WPRIM
| ID: wpr-268541
ABSTRACT
To investigate the inhibitory effect of Pluronic on P-glycoprotein (P-gp) drug efflux pump, Caco-2 cells and animal models were established to study the influence of Pluronic on celiprolol transport across Caco-2 cell monolayer and intestinal mucous membrane with verapamil set as a positive control. Drug concentration was measured by HPLC and the apparent permeability coefficient (P(app)), absorption rate constant (k(a)) and the effective permeability coefficient (P(eff)) were calculated. P(app) of basolateral to apical side and apical to basolateral side was (2.10 +/- 0.13) x 10(-6) and (0.333 +/- 0.018) x 10(-6) cm x s(-1), respectively. Transports of celiprolol across Caco-2 cell monolayer were influenced by both verapamil and Pluronic. The absorption constants (k(a)) of celiprolol at duodenum, jejunum, ileum, and colon were (0.09 +/- 0.03), (0.14 +/- 0.04), (0.11 +/- 0.03) and (0.05 +/- 0.02) h(-1), k(a) of celiprolol in verapamil group were (0.14 +/- 0.03), (0.24 +/- 0.02), (0.25 +/- 0.03) and (0.23 +/- 0.02) h(-1), and k(a) of celiprolol in Pluronic group were (0.13 +/- 0.02), (0.22 +/- 0.02), (0.22 +/- 0.03) and (0.20 +/- 0.03) h(-1), respectively. Pluronic showed significant effect on inhibiting P-gp of Caco-2 cell and intestinal mucosa in rats.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Permeabilidade
/
Farmacologia
/
Transporte Biológico
/
Farmacocinética
/
Ratos Sprague-Dawley
/
Celiprolol
/
Membro 1 da Subfamília B de Cassetes de Ligação de ATP
/
Células CACO-2
/
Poloxâmero
/
Excipientes
Limite:
Animais
/
Humanos
/
Masculino
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2007
Tipo de documento:
Artigo
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