Improving the Oral Bioavailability of Albendazole in Rabbits by the Solid Dispersion Technique

Abstract

We have investigated the oral bioavailability of granules of albendazole, a drug used for treating echinococcosis in man, prepared by the solid dispersion technique. Rapid dissolution and supersaturation were observed when hydroxypropylmethylcellulose and hydroxypropylmethylcellulose phthalate were used as carriers in the solid dispersion. They inhibited the crystallization of albendazole from the supersaturated solution and maintained an amorphous state for 8 h. Gastric acidity-controlled rabbits were used to evaluate the variation in absorption after oral administration of the albendazole solid dispersion. For rabbits with low gastric acidity the bioavailability of orally administered albendazole in the granular form prepared by solid dispersion was more than three times that of albendazole in physical mixtures. These results suggest that the bioavailability of albendazole in solid dispersions might be high even if there is a great variation in the gastric pH of patients.

Formulation development of an albendazole self-emulsifying drug delivery system (SEDDS) with enhanced systemic exposure / Razvoj samoemulzifirajućeg sustava za isporuku albendazola (SEDDS) s pojačanom sistemskom apsorpcijom

“…The results obtained indicated that apart from the HLB value, other factors such as structure and relative length of hydrophobic chains of surfactants influenced microemulsification. These results are in agreement with the results reported in literature (36,37). Cremophor EL and Tween 20 rendered effective microemulsification and were selected for further study.…”

Improvement of Albendazole Dissolution by Preparing Microparticles Using Spray-Drying Technique

“…Moreover, increased systemic bioavailability of albendazole was reported when the drug co-administered with a fatty meal [11], fruit juice [12], cosolvent [13], or with surfactants [14].…”

Enhanced Bioavailability of Probucol Following the Administration of Solid Dispersion Systems of Probucol-Polyvinylpyrrolidone in Rabbits

“…22) Kohri et al also reported the supersaturated solution by dissolution of the solid dispersion systems of albendazole with hydroxypropylmethylcellulose and hydroxymethylpropylcellulose phthalate. 23) In the absorption study, AUC values well reflected the results of the dissolution studies. The mean value of AUC following the administration of 1 : 9 solid dispersion system containing 100 mg probucol was eight times larger to that following the administration of 500 mg probucol.…”