ABSTRACT
Albendazole is a poorly water soluble drug, with low oral bioavailability, used in pharmacological treatment of a systemic disease as hydatid parasitosis. Lipidic matrices of Gelucires (44/14 and 35/02) were developed. After "in vitro" studies, one formulation was chosen for a single dose study in 8 healthy volunteers, with a cross-over and randomised design, taking a commercially available tablet as reference. Drug absorption was followed by albendazole sulphoxide dosage in urine by high pressure liquid chromatography. Neither albendazole nor albendazole sulphoxide were recovered in urine after tablet administration while 0.18% (+/- 0.06) of dose was recovered after lipidic matrix administration in the first 24 hours. Besides ageing control were performed up to 18 months post-elaboration. Lipidic matrix with Gelucire 44/14 was revealed as a promising attempt for oral pharmaceutical form in albendazole systemic treatment.
Subject(s)
Albendazole/administration & dosage , Anthelmintics/administration & dosage , Administration, Oral , Adult , Albendazole/pharmacokinetics , Animals , Anthelmintics/pharmacokinetics , Biological Availability , Cross-Over Studies , Double-Blind Method , Drug Stability , Echinococcosis/drug therapy , Humans , Polyethylene GlycolsABSTRACT
As albendazole sulphoxide (ABZS) shows better dissolution properties than albendazole (ABZ), a lipidic matrix with this drug was formulated in order to evaluate if its absorption and so systemic infection chemotherapy could be improved. A cross-over, randomised study in 8 healthy volunteers was carried out, after single administration of 1 g of albendazole or albendazole sulphoxide in lipidic matrix of Gelucire 44/14 (ABZLM and ABZSLM). Absorption was followed performing albendazole sulphoxide dosage in urine samples by high pressure liquid chromatography analysis, during 48 hours. Significant differences were found (p = 0.02) between the urinary recoveries (% E48), being 1.74% and 0.19% the percentage of dose recovered when ABZSLM or of ABZLM were respectively administered. In a previous study of our group similar values were obtained of urinary recovery percentages after albendazole sulphoxide powder administered to another group of healthy volunteers. Lipidic matrix does not improve the physicochemical properties of albendazole sulphoxide powder.
