Etoricoxib Coated Tablets: Bioequivalence Assessment between Two Formulations Administered under Fasting Conditions
Etoricoxib is a non-steroidal anti-inflammatory drug with high selectivity for cyclooxygenase 2 (COX-2), exerting a pronounced anti-inflammatory effect with fewer adverse events when compared to COX-1 inhibitors. The present study aimed to evaluate the bioequivalence between two etoricoxib-coated ta...
| Main Authors: | , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2023-11-01
|
| Series: | Pharmaceutics |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1999-4923/15/11/2569 |
| _version_ | 1797458052762304512 |
|---|---|
| author | Jessica Meulman Marcelo Gomes Davanço Débora Renz Barreto Vianna Thalita Martins da Silva Fernando Costa Fernando Bastos Canton Pacheco Milla Emke de Oliveira Celso Francisco Pimentel Vespasiano |
| author_facet | Jessica Meulman Marcelo Gomes Davanço Débora Renz Barreto Vianna Thalita Martins da Silva Fernando Costa Fernando Bastos Canton Pacheco Milla Emke de Oliveira Celso Francisco Pimentel Vespasiano |
| author_sort | Jessica Meulman |
| collection | DOAJ |
| description | Etoricoxib is a non-steroidal anti-inflammatory drug with high selectivity for cyclooxygenase 2 (COX-2), exerting a pronounced anti-inflammatory effect with fewer adverse events when compared to COX-1 inhibitors. The present study aimed to evaluate the bioequivalence between two etoricoxib-coated tablet formulations to meet regulatory requirements for a branded generic product registration in Brazil. A crossover study with an open-label, randomized design and a single-dose regimen with two treatments and two periods was conducted on healthy Brazilians of both genders. Subjects randomly received a single dose of a 90 mg etoricoxib coated tablet of test product Xumer<sup>®</sup> 90 mg (Adium S.A.) and the reference product Arcoxia<sup>®</sup> 90 mg (Merck Sharp & Dohme Farmacêutica Ltda.) under fasting conditions separated by a 14-day period. Blood samples were collected sequentially for up to 96 h following drug administration, and the concentrations of etoricoxib in plasma were determined using a validated UPLC-MS/MS method. Pharmacokinetic parameters were computed utilizing non-compartmental analysis methods. A total of 32 healthy subjects were enrolled, and 25 subjects completed the study. Geometric mean ratios (90% confidence intervals) for C<sub>max</sub>, AUC<sub>0-t</sub>, and AUC<sub>0-inf</sub> were 103.98% (95.63–113.06), 96.82% (91.82–102.09), and 95.79% (90.70–101.16), respectively. In accordance with regulatory standards, the test formulation (Xumer<sup>®</sup> 90 mg) has been deemed bioequivalent to the reference product (Arcoxia<sup>®</sup> 90 mg). As a result, these formulations can be considered interchangeable in clinical practice, with both proving to be safe and well-tolerated. The need for in vivo testing for the Xumer<sup>®</sup> 60 mg strength was waived due to the proportional similarity of the formulations and the similar in vitro dissolution profiles observed across the various strengths. |
| first_indexed | 2024-03-09T16:32:27Z |
| format | Article |
| id | doaj.art-925e1694305a40138acab95e458dbbb8 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T16:32:27Z |
| publishDate | 2023-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-925e1694305a40138acab95e458dbbb82023-11-24T15:00:56ZengMDPI AGPharmaceutics1999-49232023-11-011511256910.3390/pharmaceutics15112569Etoricoxib Coated Tablets: Bioequivalence Assessment between Two Formulations Administered under Fasting ConditionsJessica Meulman0Marcelo Gomes Davanço1Débora Renz Barreto Vianna2Thalita Martins da Silva3Fernando Costa4Fernando Bastos Canton Pacheco5Milla Emke de Oliveira6Celso Francisco Pimentel Vespasiano7Clinical Research Unit, Medical Department, Adium S.A., São Paulo 04794-000, SP, BrazilClinical Research Unit, Medical Department, Adium S.A., São Paulo 04794-000, SP, BrazilClinical Research Unit, Medical Department, Adium S.A., São Paulo 04794-000, SP, BrazilClinical Research Unit, Medical Department, Adium S.A., São Paulo 04794-000, SP, BrazilClinical Studies Management, Research and Development Department, Monte Verde S.A., Munro, Buenos Aires B1605EBQ, ArgentinaBioequivalence Unit, Centro Avançado de Estudos e Pesquisas Ltd., Campinas 13087-567, SP, BrazilBioequivalence Unit, Centro Avançado de Estudos e Pesquisas Ltd., Campinas 13087-567, SP, BrazilClinical Research Unit, Medical Department, Adium S.A., São Paulo 04794-000, SP, BrazilEtoricoxib is a non-steroidal anti-inflammatory drug with high selectivity for cyclooxygenase 2 (COX-2), exerting a pronounced anti-inflammatory effect with fewer adverse events when compared to COX-1 inhibitors. The present study aimed to evaluate the bioequivalence between two etoricoxib-coated tablet formulations to meet regulatory requirements for a branded generic product registration in Brazil. A crossover study with an open-label, randomized design and a single-dose regimen with two treatments and two periods was conducted on healthy Brazilians of both genders. Subjects randomly received a single dose of a 90 mg etoricoxib coated tablet of test product Xumer<sup>®</sup> 90 mg (Adium S.A.) and the reference product Arcoxia<sup>®</sup> 90 mg (Merck Sharp & Dohme Farmacêutica Ltda.) under fasting conditions separated by a 14-day period. Blood samples were collected sequentially for up to 96 h following drug administration, and the concentrations of etoricoxib in plasma were determined using a validated UPLC-MS/MS method. Pharmacokinetic parameters were computed utilizing non-compartmental analysis methods. A total of 32 healthy subjects were enrolled, and 25 subjects completed the study. Geometric mean ratios (90% confidence intervals) for C<sub>max</sub>, AUC<sub>0-t</sub>, and AUC<sub>0-inf</sub> were 103.98% (95.63–113.06), 96.82% (91.82–102.09), and 95.79% (90.70–101.16), respectively. In accordance with regulatory standards, the test formulation (Xumer<sup>®</sup> 90 mg) has been deemed bioequivalent to the reference product (Arcoxia<sup>®</sup> 90 mg). As a result, these formulations can be considered interchangeable in clinical practice, with both proving to be safe and well-tolerated. The need for in vivo testing for the Xumer<sup>®</sup> 60 mg strength was waived due to the proportional similarity of the formulations and the similar in vitro dissolution profiles observed across the various strengths.https://www.mdpi.com/1999-4923/15/11/2569etoricoxibanti-inflammatory agentsnon-steroidalcyclooxygenase 2 inhibitorsbioequivalencepharmacokinetics |
| spellingShingle | Jessica Meulman Marcelo Gomes Davanço Débora Renz Barreto Vianna Thalita Martins da Silva Fernando Costa Fernando Bastos Canton Pacheco Milla Emke de Oliveira Celso Francisco Pimentel Vespasiano Etoricoxib Coated Tablets: Bioequivalence Assessment between Two Formulations Administered under Fasting Conditions Pharmaceutics etoricoxib anti-inflammatory agents non-steroidal cyclooxygenase 2 inhibitors bioequivalence pharmacokinetics |
| title | Etoricoxib Coated Tablets: Bioequivalence Assessment between Two Formulations Administered under Fasting Conditions |
| title_full | Etoricoxib Coated Tablets: Bioequivalence Assessment between Two Formulations Administered under Fasting Conditions |
| title_fullStr | Etoricoxib Coated Tablets: Bioequivalence Assessment between Two Formulations Administered under Fasting Conditions |
| title_full_unstemmed | Etoricoxib Coated Tablets: Bioequivalence Assessment between Two Formulations Administered under Fasting Conditions |
| title_short | Etoricoxib Coated Tablets: Bioequivalence Assessment between Two Formulations Administered under Fasting Conditions |
| title_sort | etoricoxib coated tablets bioequivalence assessment between two formulations administered under fasting conditions |
| topic | etoricoxib anti-inflammatory agents non-steroidal cyclooxygenase 2 inhibitors bioequivalence pharmacokinetics |
| url | https://www.mdpi.com/1999-4923/15/11/2569 |
| work_keys_str_mv | AT jessicameulman etoricoxibcoatedtabletsbioequivalenceassessmentbetweentwoformulationsadministeredunderfastingconditions AT marcelogomesdavanco etoricoxibcoatedtabletsbioequivalenceassessmentbetweentwoformulationsadministeredunderfastingconditions AT deborarenzbarretovianna etoricoxibcoatedtabletsbioequivalenceassessmentbetweentwoformulationsadministeredunderfastingconditions AT thalitamartinsdasilva etoricoxibcoatedtabletsbioequivalenceassessmentbetweentwoformulationsadministeredunderfastingconditions AT fernandocosta etoricoxibcoatedtabletsbioequivalenceassessmentbetweentwoformulationsadministeredunderfastingconditions AT fernandobastoscantonpacheco etoricoxibcoatedtabletsbioequivalenceassessmentbetweentwoformulationsadministeredunderfastingconditions AT millaemkedeoliveira etoricoxibcoatedtabletsbioequivalenceassessmentbetweentwoformulationsadministeredunderfastingconditions AT celsofranciscopimentelvespasiano etoricoxibcoatedtabletsbioequivalenceassessmentbetweentwoformulationsadministeredunderfastingconditions |