Albendazole (Preclinical stage - big animals)
A comparative evaluation of the therapeutic efficacy and oral pharmacokinetics of the anthelmintic Albendazole formulation, prepared by Solumer™ methodology, and the commercial formulation Albazen (Rubikon, Belarus) was performed.
Table 1: Physico-Chemical Characteristics of the Solu-Albendazole Formulation
An efficacy and Pharmacokinetics tests were performed for the best Solu-ABZ formulation. Two dose regimes were chosen for Solu-ABZ and the reference. The experiment was performed on pigs, 10 animals in each group. The pigs were spontaneously infected by nematodes; the faeces and blood samples were collected for efficacy and PK parameters estimation.
As clearly seen in Figure 1A the Solubest formulation shows 2-3 fold better absorption of Albendazole into the pigs' blood stream than the reference. The average values summarized in Figure 1 demonstrate that the ratio test/reference AUC0-24 for dose of a 5 mg/kg is equal to 1.97 and for a dose of 10 mg/kg - 2.77. The corresponding ratios of Cmax for dose of 5 mg/kg are equal to 1.95 and for adose of 10 mg/kg - 3.35.
Efficacy of SoluAlbendazole
The analysis of the efficacy results reveals that administration of SoluAlbendazole in single oral doses of 5 and 10 mg/kg leads to dehelmintization of 50 and 80 % of the animals respectively in 5 days; and to full dehelmintization of 100% of animals in 10 days, for both doses. In comparison , Albazen suspension has very low efficacy in the dose of 5 mg/kg throughout the period of observation and, even the high dose of this drug (10 mg/kg ) leads to only 70% dehelmintization in 10 days after oral administration.