Bioavailability and efficacy characteristics of two different oral liquid formulations of albendazole.
The oral bioavailability and anthelmintic efficacy in mice of a new formulation of albendazole (ABZ) dissolved in a solution of hydroxypropyl-beta-cyclodextrin (HPCD) are compared with a conventional ABZ suspension of carboxymethylcellulose. Plasma concentrations of ABZ and albendazole sulphoxide (ABZ-SO), its active and main metabolite, were assayed by HPLC. The AUC(0- infinity ) and C(max) values obtained for both ABZ and ABZ-SO, after administration of the ABZ-HPCD solution were significantly higher (P<0.01) than those obtained from the ABZ suspension. Although, the differences between the ABZ and ABZ-SO-T(max) values were found not to be significant, regardless of the formulation. The anthelmintic activities against enteral (pre-adult) and parenteral (migrating and encysted larvae) stages of Trichinella spiralis were studied in mice. The ABZ solution was more efficient against pre-adult and encysted larvae than the ABZ suspension. The efficacy differences between both formulations against the migrating larvae, were found to be not significant (P<0.05). For the migrating parasite stage, there was a linear correlation between the anthelmintic activity and pharmacokinetical parameters with respect to the ABZ-AUC(0- infinity ) value. Meanwhile, for the muscular encysted parasite stage, better relationships were obtained for AUC(0- infinity ) and C(max) values from ABZ-SO, which had correlation coefficients of 0.996 and 0.987, respectively.
García
Juan José
JJ
Departamento de Parasitologi;a, Facultad de Farmacia, Universidad Complutense de Madrid, Plaza Ramón y Cajal, 28040, Madrid, Spain.
Bolás
Francisco
F
Torrado
Juan José
JJ
D000284:Administration, Oral; D015766:Albendazole / Q000008:administration & dosage* / Q000097:blood / Q000627:therapeutic use*; D000818:Animals; D000871:Anthelmintics / Q000008:administration & dosage* / Q000097:blood / Q000627:therapeutic use*; D019540:Area Under Curve; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D007814:Larva / Q000187:drug effects; D051379:Mice; D019999:Pharmaceutical Solutions; D017160:Trichinella spiralis / Q000187:drug effects; D014235:Trichinellosis / Q000097:blood / Q000188:drug therapy
D000871:Anthelmintics; D019999:Pharmaceutical Solutions; D015766:Albendazole