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Thiabendazole and Flubendazole
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Flubendazole is a benzimidazole anthelmintic synthesized in 1969 by Janssen Pharmaceutica (Beerse, Belgium). It is an analog of mebendazole in which the benzoyl group is replaced by a p-fluorobenzoyl group. Flubendazole is a white/off-white, odorless powder that is insoluble in water and only slightly soluble in alcohol and other organic solvents. It has the chemical formula methyl N-[6-(4-fluorobenzoyl)-1H-benzimidazol-2-yl]carbamate (C16H12FN3O3) with a molecular weight of 313.3. Its molecular structure is shown in Figure 202.2.
Nano-crystallization of flubendazole for enhanced dissolution rate and improved in vivo efficacy against Trichinella spiralis
Published in Pharmaceutical Development and Technology, 2023
Ahmed S. Kamel, Soha M. El-Masry, Haidy Abbas, Fatma Mkh Ibrahim, Hager S. Zoghroban, Gamal M. El Maghraby
Flubendazole is one of the most widely prescribed antiparasitic agents. It showed promising activity against Trichinella spiralis. However, its activity depended on the time of administration post infection with early administration being essential. This means that the drug will be effective on the intestinal phase of the disease but not on the migrating larvae or encysted phases. This can be attributed to its poor bioavailability which is dissolution limited and is also affected by first pass effect (El-Temsahi and El-Mansoury 1995). Authors tried to enhance oral absorption of flubendazole through amorphization approaches or adsorption on mesoporous silica (Vialpando et al. 2016), formation of nanofibrous solid dispersion in presence of hydroxylpropyl β − cyclodextrin and polyvinyl pyrrolidone (Vigh et al. 2017) and finally, extrusion with copovidone by hot melting (de Assis et al. 2022). Another study studied co-crystals with maleic acid through solvent assisted milling (de Araujo et al. 2018). Formulation of biodegradable nanoparticles (Farhadi et al. 2018) and nano-emulsion were also studied (Yukuyama et al. 2021). To the best of our knowledge, Anti-solvent precipitation technique to enhance dissolution rate of flubendazole through nanocrystal formation and evaluate its in vivo efficacy through oral administration was not investigated before.