RESUMO
An improved high performance liquid chromatography–tandem mass spectrometry (LC–MS/MS) method has been developed for sensitive and rapid determination of albendazole (ABZ) and its active metabolite, albendazole sulfoxide (ABZSO), in the positive ionization mode. The method utilized solid phase ex-traction (SPE) for sample preparation of the analytes and their deuterated internal standards (ISs) from 100 mL human plasma. The chromatography was carried out on Hypurity C18 column using acetonitrile-2.0 mM ammonium acetate, pH 5.0 (80:20, v/v) as the mobile phase. The assay exhibited a linear re-sponse over the concentration range of 0.200–50.0 ng/mL for ABZ and 3.00–600 ng/mL for ABZSO. The recoveries of the analytes and ISs ranged from 86.03%–89.66% and 89.85%–98.94%, respectively. Matrix effect, expressed as IS-normalized matrix factors, ranged from 0.985 to 1.042 for the both analytes. The method was successfully applied for two separate studies in healthy subjects using single dose of 400 mg conventional tablets and 400 mg chewable ABZ tablets, respectively.
RESUMO
Screening scale studies were performed to biotransform anthelmintic drug albendazole by using twelve bacterial strains representing six genera and five actinomycetes cultures. Among the cultures studied, Bacillus subtilis MTCC 619, Escherichia coli MTCC 118 and Klebsiella pneumoniae MTCC 109 could transform albendazole to one metabolite whereas, Enterobacter aerogenes NCIM 2695, Klebsiella aerogenes NCIM 2258, Pseudomonas aeruginosa NCIM 2074 and Streptomyces griseus NCIM 2622 could transform albendazole into two metabolites in significant quantities. The transformation of albendazole was identified by HPLC. Based on LC-MS-MS data, the two metabolites were predicted to be albendazole sulfoxide (M1) and albendazole sulfone (M2), the major mammalian metabolites reported previously. Since M1 is active metabolite, the results prove the versatility of microorganisms to perform industrially attractive chemical reactions.
RESUMO
Objective To investigate in vitro anti-hydatid efficacy on Echinococcus granulosus protoscolex(EgPSC) by using albendazole sulfoxide(ASOX) and its two enantiomeric antipodes, L-ASOX and D-ASOX.Methods Eg protoscoleces were divided into eight groups and cultured in the DMEM culture media under two concentrations(50 ?g/ml and 100 ?g/ml) of ASOX, L-ASOX and D-ASOX respectively.The appropriate controls included(i) a culture containing an equal amount of DMSO and(ii) a culture medium alone.The mortality of EgPSC in each group was daily counted until 100% EgPSC death in some groups.Results Significant difference of EgPSC mortality was found among the three drugs with various concentrations compared to control group(P0.05), but between ASOX group and L-ASOX group(P