A high oxfendazole dose to control porcine cysticercosis: Pharmacokinetics and tissue residue profiles

L. Moreno; M. T. Lopez-Urbina; C. Farias; G. Domingue; M. Donadeu; B. Dungu; H. H. García; L. A. Gomez-Puerta; C. Lanusse; A. E. González

doi:10.1016/j.fct.2012.07.023

A high oxfendazole dose to control porcine cysticercosis: Pharmacokinetics and tissue residue profiles

L. Moreno, M. T. Lopez-Urbina, C. Farias, G. Domingue, M. Donadeu, B. Dungu, H. H. García, L. A. Gomez-Puerta, C. Lanusse, A. E. González

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Abstract

Oxfendazole (OFZ) is efficacious for porcine cysticercosis at 30mg/kg. OFZ is not registered to be used at this dose. The assessment of the OFZ and metabolites [(fenbendazole sulphone (FBZSO₂), fenbendazole (FBZ)] plasma pharmacokinetic and tissue residue profiles after its oral administration to pigs and the withdrawal period for human consumption were reported. Forty-eight pigs allocated into two groups received OFZ (30mg/kg) orally as a commercial (CF) or as experimental formulation (SMF). Samples (blood, muscle, liver, kidney and fat) were collected over 30days post-treatment and analyzed by HPLC. OFZ was the main compound recovered in plasma, followed by FBZSO₂ and low FBZ concentrations. OFZ AUC_0-LOQ (209.9±33.9μg·h/ml) and C_max (5.40±0.65μg/ml) parameters for the CF tended to be higher than those for the SMF (AUC_0-LOQ: 159.4±18.3μgh/ml, C_max: 3.80±0.35μg/ml). The highest total residue (OFZ+FBZSO₂+FBZ) concentrations were quantified in liver, followed by kidney, muscle and fat tissue. FBZSO₂ residue levels were the highest found in muscle (0.68±0.39μg/g) and fat (0.69±0.39μg/g). In liver and kidney the highest residues corresponded to FBZ (5.29±4.36μg/g) and OFZ (2.86±0.75μg/g), respectively. A withdrawal time of 17days post-treatment was established before tissues are delivered for human consumption.

Original language	English
Pages (from-to)	3819-3825
Number of pages	7
Journal	Food and Chemical Toxicology
Volume	50
Issue number	10
DOIs	https://doi.org/10.1016/j.fct.2012.07.023
State	Published - Oct 2012

Bibliographical note

Funding Information:
Funding: This work was funded by the Bill and Melinda Gates Foundation through grants number 1016506 and 23981 and also funds from the Department for International Development (DFID) UK. HG is a Wellcome Trust Senior Research Fellow in Public Health. The funders had no role in study design; data collection, analysis, or interpretation; in writing the report, or in the decision to submit the article for publication.

Keywords

Cysticercosis
Oxfendazole
Pharmacokinetics
Tissue residues
Withdrawal time

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10.1016/j.fct.2012.07.023

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title = "A high oxfendazole dose to control porcine cysticercosis: Pharmacokinetics and tissue residue profiles",

abstract = "Oxfendazole (OFZ) is efficacious for porcine cysticercosis at 30mg/kg. OFZ is not registered to be used at this dose. The assessment of the OFZ and metabolites [(fenbendazole sulphone (FBZSO2), fenbendazole (FBZ)] plasma pharmacokinetic and tissue residue profiles after its oral administration to pigs and the withdrawal period for human consumption were reported. Forty-eight pigs allocated into two groups received OFZ (30mg/kg) orally as a commercial (CF) or as experimental formulation (SMF). Samples (blood, muscle, liver, kidney and fat) were collected over 30days post-treatment and analyzed by HPLC. OFZ was the main compound recovered in plasma, followed by FBZSO2 and low FBZ concentrations. OFZ AUC0-LOQ (209.9±33.9μg·h/ml) and Cmax (5.40±0.65μg/ml) parameters for the CF tended to be higher than those for the SMF (AUC0-LOQ: 159.4±18.3μgh/ml, Cmax: 3.80±0.35μg/ml). The highest total residue (OFZ+FBZSO2+FBZ) concentrations were quantified in liver, followed by kidney, muscle and fat tissue. FBZSO2 residue levels were the highest found in muscle (0.68±0.39μg/g) and fat (0.69±0.39μg/g). In liver and kidney the highest residues corresponded to FBZ (5.29±4.36μg/g) and OFZ (2.86±0.75μg/g), respectively. A withdrawal time of 17days post-treatment was established before tissues are delivered for human consumption.",

keywords = "Cysticercosis, Oxfendazole, Pharmacokinetics, Tissue residues, Withdrawal time",

author = "L. Moreno and Lopez-Urbina, {M. T.} and C. Farias and G. Domingue and M. Donadeu and B. Dungu and Garc{\'i}a, {H. H.} and Gomez-Puerta, {L. A.} and C. Lanusse and Gonz{\'a}lez, {A. E.}",

note = "Funding Information: Funding: This work was funded by the Bill and Melinda Gates Foundation through grants number 1016506 and 23981 and also funds from the Department for International Development (DFID) UK. HG is a Wellcome Trust Senior Research Fellow in Public Health. The funders had no role in study design; data collection, analysis, or interpretation; in writing the report, or in the decision to submit the article for publication. ",

year = "2012",

month = oct,

doi = "10.1016/j.fct.2012.07.023",

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T2 - Pharmacokinetics and tissue residue profiles

AU - Moreno, L.

AU - Lopez-Urbina, M. T.

AU - Farias, C.

AU - Domingue, G.

AU - Donadeu, M.

AU - Dungu, B.

AU - García, H. H.

AU - Gomez-Puerta, L. A.

AU - Lanusse, C.

AU - González, A. E.

N1 - Funding Information: Funding: This work was funded by the Bill and Melinda Gates Foundation through grants number 1016506 and 23981 and also funds from the Department for International Development (DFID) UK. HG is a Wellcome Trust Senior Research Fellow in Public Health. The funders had no role in study design; data collection, analysis, or interpretation; in writing the report, or in the decision to submit the article for publication.

PY - 2012/10

Y1 - 2012/10

N2 - Oxfendazole (OFZ) is efficacious for porcine cysticercosis at 30mg/kg. OFZ is not registered to be used at this dose. The assessment of the OFZ and metabolites [(fenbendazole sulphone (FBZSO2), fenbendazole (FBZ)] plasma pharmacokinetic and tissue residue profiles after its oral administration to pigs and the withdrawal period for human consumption were reported. Forty-eight pigs allocated into two groups received OFZ (30mg/kg) orally as a commercial (CF) or as experimental formulation (SMF). Samples (blood, muscle, liver, kidney and fat) were collected over 30days post-treatment and analyzed by HPLC. OFZ was the main compound recovered in plasma, followed by FBZSO2 and low FBZ concentrations. OFZ AUC0-LOQ (209.9±33.9μg·h/ml) and Cmax (5.40±0.65μg/ml) parameters for the CF tended to be higher than those for the SMF (AUC0-LOQ: 159.4±18.3μgh/ml, Cmax: 3.80±0.35μg/ml). The highest total residue (OFZ+FBZSO2+FBZ) concentrations were quantified in liver, followed by kidney, muscle and fat tissue. FBZSO2 residue levels were the highest found in muscle (0.68±0.39μg/g) and fat (0.69±0.39μg/g). In liver and kidney the highest residues corresponded to FBZ (5.29±4.36μg/g) and OFZ (2.86±0.75μg/g), respectively. A withdrawal time of 17days post-treatment was established before tissues are delivered for human consumption.

AB - Oxfendazole (OFZ) is efficacious for porcine cysticercosis at 30mg/kg. OFZ is not registered to be used at this dose. The assessment of the OFZ and metabolites [(fenbendazole sulphone (FBZSO2), fenbendazole (FBZ)] plasma pharmacokinetic and tissue residue profiles after its oral administration to pigs and the withdrawal period for human consumption were reported. Forty-eight pigs allocated into two groups received OFZ (30mg/kg) orally as a commercial (CF) or as experimental formulation (SMF). Samples (blood, muscle, liver, kidney and fat) were collected over 30days post-treatment and analyzed by HPLC. OFZ was the main compound recovered in plasma, followed by FBZSO2 and low FBZ concentrations. OFZ AUC0-LOQ (209.9±33.9μg·h/ml) and Cmax (5.40±0.65μg/ml) parameters for the CF tended to be higher than those for the SMF (AUC0-LOQ: 159.4±18.3μgh/ml, Cmax: 3.80±0.35μg/ml). The highest total residue (OFZ+FBZSO2+FBZ) concentrations were quantified in liver, followed by kidney, muscle and fat tissue. FBZSO2 residue levels were the highest found in muscle (0.68±0.39μg/g) and fat (0.69±0.39μg/g). In liver and kidney the highest residues corresponded to FBZ (5.29±4.36μg/g) and OFZ (2.86±0.75μg/g), respectively. A withdrawal time of 17days post-treatment was established before tissues are delivered for human consumption.

KW - Cysticercosis

KW - Oxfendazole

KW - Pharmacokinetics

KW - Tissue residues

KW - Withdrawal time

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ER -

A high oxfendazole dose to control porcine cysticercosis: Pharmacokinetics and tissue residue profiles

Abstract

Bibliographical note

Keywords

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