The effect of polyamidoamine (PAMAM) dendrimers on the solubility and pharmacokinetics of breviscapine / 药学学报
Acta Pharmaceutica Sinica
;
(12): 197-202, 2009.
Article
Dans Chinois
| WPRIM
| ID: wpr-278280
ABSTRACT
To study the solubilization of breviscapine with polyamidoamine (PAMAM) dendrimers and probe the solubilizing mechanism and investigate the influence of PAMAM dendrimers on the pharmacokinetics of breviscapine, the solubilization of breviscapine by PAMAM dendrimers of generations G1, G1.5, G2 and G2.5 with different concentrations were determined and compared in different pH conditions. Twelve rats randomized into 2 groups were separately orally administered breviscapine and breviscapine combining with PAMAM. Drug in plasma was extracted and determined with HPLC. In pH condition lower than 7.0, the solubilization of breviscapine by PAMAM dendrimers enhanced as the generation and concentration of PAMAM dendrimers as well as the pH increased. Its solubilizing mechanism involves an electrostatic interaction between the carboxyl group of breviscapine and the primary amines and tertiary amines of PAMAM dendrimers. The pharmacokinetics parameters Cmax and AUC0-8 h of breviscapine were (119.65 +/- 9.36) ng x mL(-1) and (370.09 +/- 63.08) ng x h x mL(-1). For breviscapine combined with PAMAM dendrimers, the Cmax and AUC0-8 h were (518.17 +/- 17.07) ng x mL(-1) and (1,219.47 +/- 201.87) ng x h x mL(-1), respectively. There were significant differences of AUC0-8 h between breviscapine and breviscapine combined with PAMAM dendrimers (P < 0.01). PAMAM dendrimers can greatly increase the solubility of breviscapine in water and can improve the oral bioavailability of breviscapine significantly.
Texte intégral:
Disponible
Indice:
WPRIM (Pacifique occidental)
Sujet Principal:
Pharmacologie
/
Plantes médicinales
/
Polyamines
/
Solubilité
/
Matériaux biocompatibles
/
Flavonoïdes
/
Vecteurs de médicaments
/
Pharmacocinétique
/
Biodisponibilité
/
Structure moléculaire
Type d'étude:
Étude pronostique
Limites du sujet:
Animaux
langue:
Chinois
Texte intégral:
Acta Pharmaceutica Sinica
Année:
2009
Type:
Article
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