Effect of two formulations of benzimidazole carbamates on the viability of cysts of Echinococcus granulosus in vivo.

Two different preparations, solution and suspension, of three benzimidazole carbamate drugs, mebendazole, albendazole and ricobendazole, were compared by analyzing their in vivo activity against Echinococcus granulosus cysts in a mouse model. Polyvinylpyrrolidone was used for the elaboration of drug solutions and these formulations manifested better results in terms of reduction of number of viable hydatid cysts in mice than the reference drug suspensions. The effect was more prominent on mebendazole-treated mice, at doses of 25-50 mg/kg. There was a correlation between ED50 and pharmacokinetical parameters of AUC0-infinity and Cmax, showing that a significant improvement on solubility affects the in vivo activity of these drugs.

Improvement of albendazole efficacy against enteral, but not against parenteral stages of Trichinella spiralis by preparing solid dispersions in polyvinylpyrrolidone.

A comparison was made, in the Trichinella/mouse model, of the anthelmintic effects of albendazole (ABZ) and ricobendazole (RBZ) formulated as solid dispersions in polyvinylpyrrolidone with regard to ABZ formulated as a suspension in carboxymethylcellulose. A solid dispersion significantly increased (p < 0.01) the efficacy of the drugs against intestinal preadult but not against migrating and muscle stages of the parasite. The anthelmintic efficacy of RBZ given as a solid dispersion was equivalent to (against preadult and encysted larvae) or significantly lower than (against migrating larvae) that of ABZ with the same formulation. The pharmacokinetic profiles of ABZSO as measured by HPLC showed no significant differences in the Cmax and AUC following administration of ABZ formulated as a suspension or solid dispersion although the Tmax was significantly lower for the dispersion.