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Chiral bioanalytical methods in bioequivalence studies of intravenous vs. oral formulations of ibuprofen.
Chirality. 2020 09; 32(9):1169-1177.C

Abstract

According to the Ibuprofen Product-Specific Bioequivalence Guidance of the European Medicines Agency, achiral bioanalytical methods are considered acceptable for demonstration of bioequivalence of ibuprofen-containing products. The aim of this investigation is to compare the bioequivalence outcomes obtained with individual R and S ibuprofen enantiomers and the sum of both enantiomers from bioequivalence studies in which new intravenous ibuprofen products were compared with oral ibuprofen products. Bioequivalence was assessed for S and R enantiomers of ibuprofen and the sum of both enantiomers, which was calculated to represent the results that would have been obtained with an achiral assay. The infusion rates of 15, 20, and 30 minutes modify the maximum concentration (Cmax) of the intravenous administrations. In contrast, the time when the maximum concentration is observed (Tmax) was insensitive to detect differences in input rate within this range of infusion times. The eutomer S-ibuprofen is the least sensitive analyte to detect differences in input rate; therefore, the regulatory acceptance of achiral bioanalytical methods for ibuprofen bioequivalence studies is justified because the sum of both enantiomers is more discriminative than the chiral methods where only the eutomer is used for regulatory decisions.

Authors+Show Affiliations

Clinical Pharmacology Department, Hospital Clínico San Carlos, IdISSC, Madrid, Spain.Department of Anaesthesiology, Reanimation and Pain Treatment, Hospital Clínico San Carlos, Madrid, Spain.Clinical Pharmacology Department, Hospital Clínico San Carlos, IdISSC, Madrid, Spain. Pharmacology and Toxicology Department, Complutense University of Madrid, Spain.Department of Essential Medicines and Health Products (EMP), World Health Organization, Geneva, Switzerland.Division of Biopharmaceutics Evaluation, Bureau of Pharmaceutical Sciences, Therapeutic Products Directorate, Health Canada, Ottawa, Canada.Clinical Pharmacology Department, Hospital Clínico San Carlos, IdISSC, Madrid, Spain. Pharmacology and Toxicology Department, Complutense University of Madrid, Spain.Clinical Pharmacology Department, Hospital Clínico San Carlos, IdISSC, Madrid, Spain. Pharmacology and Toxicology Department, Complutense University of Madrid, Spain.Division of Pharmacology and Clinical Evaluation, Department of Human Use Medicines, Spanish Agency for Medicines and Health Care Products, Madrid, Spain.Division of Pharmacology and Clinical Evaluation, Department of Human Use Medicines, Spanish Agency for Medicines and Health Care Products, Madrid, Spain.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

32602190

Citation

González-Rojano, Esperanza, et al. "Chiral Bioanalytical Methods in Bioequivalence Studies of Intravenous Vs. Oral Formulations of Ibuprofen." Chirality, vol. 32, no. 9, 2020, pp. 1169-1177.
González-Rojano E, Marcotegui J, Laredo L, et al. Chiral bioanalytical methods in bioequivalence studies of intravenous vs. oral formulations of ibuprofen. Chirality. 2020;32(9):1169-1177.
González-Rojano, E., Marcotegui, J., Laredo, L., Gwaza, L., Gordon, J., Portolés, A., Vargas, E., Morales-Alcelay, S., & García-Arieta, A. (2020). Chiral bioanalytical methods in bioequivalence studies of intravenous vs. oral formulations of ibuprofen. Chirality, 32(9), 1169-1177. https://doi.org/10.1002/chir.23258
González-Rojano E, et al. Chiral Bioanalytical Methods in Bioequivalence Studies of Intravenous Vs. Oral Formulations of Ibuprofen. Chirality. 2020;32(9):1169-1177. PubMed PMID: 32602190.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Chiral bioanalytical methods in bioequivalence studies of intravenous vs. oral formulations of ibuprofen. AU - González-Rojano,Esperanza, AU - Marcotegui,Julio, AU - Laredo,Leonor, AU - Gwaza,Luther, AU - Gordon,John, AU - Portolés,Antonio, AU - Vargas,Emilio, AU - Morales-Alcelay,Susana, AU - García-Arieta,Alfredo, Y1 - 2020/06/29/ PY - 2020/04/28/received PY - 2020/06/03/revised PY - 2020/06/04/accepted PY - 2020/7/1/pubmed PY - 2020/7/1/medline PY - 2020/7/1/entrez KW - R-ibuprofen KW - S-ibuprofen KW - bioequivalence KW - enantiomer KW - intravenous SP - 1169 EP - 1177 JF - Chirality JO - Chirality VL - 32 IS - 9 N2 - According to the Ibuprofen Product-Specific Bioequivalence Guidance of the European Medicines Agency, achiral bioanalytical methods are considered acceptable for demonstration of bioequivalence of ibuprofen-containing products. The aim of this investigation is to compare the bioequivalence outcomes obtained with individual R and S ibuprofen enantiomers and the sum of both enantiomers from bioequivalence studies in which new intravenous ibuprofen products were compared with oral ibuprofen products. Bioequivalence was assessed for S and R enantiomers of ibuprofen and the sum of both enantiomers, which was calculated to represent the results that would have been obtained with an achiral assay. The infusion rates of 15, 20, and 30 minutes modify the maximum concentration (Cmax) of the intravenous administrations. In contrast, the time when the maximum concentration is observed (Tmax) was insensitive to detect differences in input rate within this range of infusion times. The eutomer S-ibuprofen is the least sensitive analyte to detect differences in input rate; therefore, the regulatory acceptance of achiral bioanalytical methods for ibuprofen bioequivalence studies is justified because the sum of both enantiomers is more discriminative than the chiral methods where only the eutomer is used for regulatory decisions. SN - 1520-636X UR - https://www.unboundmedicine.com/medline/citation/32602190/Chiral_bioanalytical_methods_in_bioequivalence_studies_of_intravenous_vs._oral_formulations_of_ibuprofen L2 - https://doi.org/10.1002/chir.23258 DB - PRIME DP - Unbound Medicine ER -
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