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 anthelmi ntic effects of albendazole (ABZ) and ricobendazole (RBZ) formulated a s solid dispersions in polyvinylpyrrolidone with regard to ABZ formula ted as a suspension in carboxymethylcellulose, A solid dispersion sign ificantly increased (p < 0.01) the efficacy of the drugs against intes tinal preadult but not against migrating and muscle stages of the para site, 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 formu lation. The pharmacokinetic profiles of ABZSO as measured by HPLC show ed no significant differences in the Cmax and AUC following administra tion of ABZ formulated as a suspension or solid dispersion although th e Tmax was significantly lower for the dispersion.