High-Fat Breakfast Increases Bioavailability of Albendazole Compared to Low-Fat Breakfast: Single-Dose Study in Healthy Subjects
Purpose: Albendazole is a benzimidazole carbamate drug with anthelmintic and antiprotozoal activity against intestinal and tissue parasites. It has been described that the administration with meals increases albendazole absorption. Our aim was to compare the systemic exposure in healthy volunteers o...
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2021-04-01
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| Series: | Frontiers in Pharmacology |
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| Online Access: | https://www.frontiersin.org/articles/10.3389/fphar.2021.664465/full |
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| author | Dolores Ochoa Dolores Ochoa Miriam Saiz-Rodríguez Miriam Saiz-Rodríguez Esperanza González-Rojano Manuel Román Manuel Román Sergio Sánchez-Rojas Aneta Wojnicz Ana Ruiz-Nuño Alfredo García-Arieta Francisco Abad-Santos Francisco Abad-Santos |
| author_facet | Dolores Ochoa Dolores Ochoa Miriam Saiz-Rodríguez Miriam Saiz-Rodríguez Esperanza González-Rojano Manuel Román Manuel Román Sergio Sánchez-Rojas Aneta Wojnicz Ana Ruiz-Nuño Alfredo García-Arieta Francisco Abad-Santos Francisco Abad-Santos |
| author_sort | Dolores Ochoa |
| collection | DOAJ |
| description | Purpose: Albendazole is a benzimidazole carbamate drug with anthelmintic and antiprotozoal activity against intestinal and tissue parasites. It has been described that the administration with meals increases albendazole absorption. Our aim was to compare the systemic exposure in healthy volunteers of two albendazole formulations after a single oral dose under fed conditions and to evaluate the effect of breakfast composition on albendazole and albendazole sulfoxide bioavailability.Methods: 12 healthy volunteers were included in a 4-period, 4-sequence, crossover, open, randomized, bioequivalence clinical trial, including two stages to compare two formulations of albendazole. Single oral doses of 400 mg albendazole were administered under fed conditions (a low-fat breakfast in first stage and a high-fat breakfast in the second) separated by 7-day washout periods. Plasma albendazole and albendazole sulfoxide concentrations were measured by HPLC-MS/MS.Findings: Albendazole absorption was clearly influenced by the meal composition. A high-fat breakfast increased albendazole and albendazole sulfoxide area under the concentration–time curve (AUC) and maximum concentration (Cmax) by double, compared to a low-fat breakfast. The bioavailability of the two formulations was very similar, although the sample size was not sufficient to demonstrate bioequivalence because the intraindividual variability of albendazole was approximately 60%.Implications: The higher albendazole and albendazole sulfoxide levels when administered with a high-fat meal could be of importance in clinical practice. Since albendazole labeling recommends its administration with meals, it is necessary to insist on taking it with a fatty meal so that the effectiveness of albendazole is not compromised. |
| first_indexed | 2024-12-13T21:48:44Z |
| format | Article |
| id | doaj.art-b53b5f228a6c43a5b0fb6aaf539537ac |
| institution | Directory Open Access Journal |
| issn | 1663-9812 |
| language | English |
| last_indexed | 2024-12-13T21:48:44Z |
| publishDate | 2021-04-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Pharmacology |
| spelling | doaj.art-b53b5f228a6c43a5b0fb6aaf539537ac2022-12-21T23:30:20ZengFrontiers Media S.A.Frontiers in Pharmacology1663-98122021-04-011210.3389/fphar.2021.664465664465High-Fat Breakfast Increases Bioavailability of Albendazole Compared to Low-Fat Breakfast: Single-Dose Study in Healthy SubjectsDolores Ochoa0Dolores Ochoa1Miriam Saiz-Rodríguez2Miriam Saiz-Rodríguez3Esperanza González-Rojano4Manuel Román5Manuel Román6Sergio Sánchez-Rojas7Aneta Wojnicz8Ana Ruiz-Nuño9Alfredo García-Arieta10Francisco Abad-Santos11Francisco Abad-Santos12Clinical Pharmacology Department, Hospital Universitario de La Princesa, Instituto Teófilo Hernando, Facultad de Medicina, Universidad Autónoma de Madrid (UAM), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, SpainUICEC Hospital Universitario de La Princesa, Plataforma SCReN (Spanish Clinical Reseach Network), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, SpainClinical Pharmacology Department, Hospital Universitario de La Princesa, Instituto Teófilo Hernando, Facultad de Medicina, Universidad Autónoma de Madrid (UAM), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, SpainResearch Unit, Fundación Burgos por La Investigación de La Salud, Hospital Universitario de Burgos, Burgos, SpainClinical Pharmacology Department, Hospital Universitario de La Princesa, Instituto Teófilo Hernando, Facultad de Medicina, Universidad Autónoma de Madrid (UAM), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, SpainClinical Pharmacology Department, Hospital Universitario de La Princesa, Instituto Teófilo Hernando, Facultad de Medicina, Universidad Autónoma de Madrid (UAM), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, SpainUICEC Hospital Universitario de La Princesa, Plataforma SCReN (Spanish Clinical Reseach Network), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, SpainClinical Pharmacology Department, Hospital Universitario de La Princesa, Instituto Teófilo Hernando, Facultad de Medicina, Universidad Autónoma de Madrid (UAM), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, SpainClinical Pharmacology Department, Hospital Universitario de La Princesa, Instituto Teófilo Hernando, Facultad de Medicina, Universidad Autónoma de Madrid (UAM), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, SpainClinical Pharmacology Department, Hospital Universitario de La Princesa, Instituto Teófilo Hernando, Facultad de Medicina, Universidad Autónoma de Madrid (UAM), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, SpainService on Pharmacokinetics and Generics, Division of Pharmacology and Clinical Evaluation, Department of Human Use Medicines, Spanish Agency for Medicines and Health Care Products, Madrid, SpainClinical Pharmacology Department, Hospital Universitario de La Princesa, Instituto Teófilo Hernando, Facultad de Medicina, Universidad Autónoma de Madrid (UAM), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, SpainUICEC Hospital Universitario de La Princesa, Plataforma SCReN (Spanish Clinical Reseach Network), Instituto de Investigación Sanitaria La Princesa (IP), Madrid, SpainPurpose: Albendazole is a benzimidazole carbamate drug with anthelmintic and antiprotozoal activity against intestinal and tissue parasites. It has been described that the administration with meals increases albendazole absorption. Our aim was to compare the systemic exposure in healthy volunteers of two albendazole formulations after a single oral dose under fed conditions and to evaluate the effect of breakfast composition on albendazole and albendazole sulfoxide bioavailability.Methods: 12 healthy volunteers were included in a 4-period, 4-sequence, crossover, open, randomized, bioequivalence clinical trial, including two stages to compare two formulations of albendazole. Single oral doses of 400 mg albendazole were administered under fed conditions (a low-fat breakfast in first stage and a high-fat breakfast in the second) separated by 7-day washout periods. Plasma albendazole and albendazole sulfoxide concentrations were measured by HPLC-MS/MS.Findings: Albendazole absorption was clearly influenced by the meal composition. A high-fat breakfast increased albendazole and albendazole sulfoxide area under the concentration–time curve (AUC) and maximum concentration (Cmax) by double, compared to a low-fat breakfast. The bioavailability of the two formulations was very similar, although the sample size was not sufficient to demonstrate bioequivalence because the intraindividual variability of albendazole was approximately 60%.Implications: The higher albendazole and albendazole sulfoxide levels when administered with a high-fat meal could be of importance in clinical practice. Since albendazole labeling recommends its administration with meals, it is necessary to insist on taking it with a fatty meal so that the effectiveness of albendazole is not compromised.https://www.frontiersin.org/articles/10.3389/fphar.2021.664465/fullalbendazolebreakfastbioavailabilityhealthy subjectspharmacokinetic |
| spellingShingle | Dolores Ochoa Dolores Ochoa Miriam Saiz-Rodríguez Miriam Saiz-Rodríguez Esperanza González-Rojano Manuel Román Manuel Román Sergio Sánchez-Rojas Aneta Wojnicz Ana Ruiz-Nuño Alfredo García-Arieta Francisco Abad-Santos Francisco Abad-Santos High-Fat Breakfast Increases Bioavailability of Albendazole Compared to Low-Fat Breakfast: Single-Dose Study in Healthy Subjects Frontiers in Pharmacology albendazole breakfast bioavailability healthy subjects pharmacokinetic |
| title | High-Fat Breakfast Increases Bioavailability of Albendazole Compared to Low-Fat Breakfast: Single-Dose Study in Healthy Subjects |
| title_full | High-Fat Breakfast Increases Bioavailability of Albendazole Compared to Low-Fat Breakfast: Single-Dose Study in Healthy Subjects |
| title_fullStr | High-Fat Breakfast Increases Bioavailability of Albendazole Compared to Low-Fat Breakfast: Single-Dose Study in Healthy Subjects |
| title_full_unstemmed | High-Fat Breakfast Increases Bioavailability of Albendazole Compared to Low-Fat Breakfast: Single-Dose Study in Healthy Subjects |
| title_short | High-Fat Breakfast Increases Bioavailability of Albendazole Compared to Low-Fat Breakfast: Single-Dose Study in Healthy Subjects |
| title_sort | high fat breakfast increases bioavailability of albendazole compared to low fat breakfast single dose study in healthy subjects |
| topic | albendazole breakfast bioavailability healthy subjects pharmacokinetic |
| url | https://www.frontiersin.org/articles/10.3389/fphar.2021.664465/full |
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