Analysis of the effect of in vitro dissolution on the pharmacokinetics of albendazole

Nelly  Castro; Iliana  González-Hernández; Lourdes  Mayet-Cruz; José  Becerril-Vega; Sergio  Soto-Romo; Helgi  Jung-Cook

doi:10.1590/

Authors

Nelly Castro Laboratorio de Neuropsicofarmacología, Instituto Nacional de Neurología y Neurocirugía Manuel Velasco Suárez, Mexico City, Mexico
Iliana González-Hernández Laboratorio de Neuropsicofarmacología, Instituto Nacional de Neurología y Neurocirugía Manuel Velasco Suárez, Mexico City, Mexico https://orcid.org/0000-0001-9229-1121
Lourdes Mayet-Cruz Departamento de Farmacia, Facultad de Química, Universidad Nacional Autónoma de México, Mexico City, Mexico
José Becerril-Vega Departamento de Farmacia, Facultad de Química, Universidad Nacional Autónoma de México, Mexico City, Mexico
Sergio Soto-Romo Departamento de Farmacia, Facultad de Química, Universidad Nacional Autónoma de México, Mexico City, Mexico
Helgi Jung-Cook Departamento de Farmacia, Facultad de Química, Universidad Nacional Autónoma de México, Mexico City, Mexico https://orcid.org/0000-0002-2032-4753

DOI:

https://doi.org/10.1590/

Keywords:

Albendazole, Quality control, Dissolution, Pharmacokinetic modeling

Abstract

Albendazole is an anthelmintic drug commonly used in parenchymal neurocysticercosis and cystic echinococcosis. The aim of this study was to explore whether disparities in the dissolution profiles of albendazole products lead to significant differences in pharmacokinetic parameters. Three generic products and the innovator were evaluated in vitro. Quality control tests were performed, and dissolution profiles were obtained according to the Mexican Pharmacopeia. Although all products passed the quality control tests, none of the generic products complied with the similarity factor (f ₂). The product with the lowest f ₂ value in respect to the reference was chosen for in vivo evaluation. The study was carried out in 12 healthy volunteers who received 400 mg of the generic or reference product according to a crossover design. No significant differences were found in C_max and AUC for albendazole and its main metabolite, albendazole sulfoxide, between products. Two absorption peaks were observed in the pharmacokinetic profile, and a population (22%) with different absorption rates and delay time for the the second peak was found. Based on the results, due to the high variability in the absorption process the differences observed in vitro could not be observed in vivo.

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