Bioequivalence Study of Two Oral Methocarbamol Formulations in Healthy Subjects Under Fasting Conditions: A Randomized, Open-Label, Crossover Clinical Trial
<b>Objective:</b> This study aimed to assess the bioequivalence of two oral methocarbamol formulations, as follows: the test (T) methocarbamol 1500 mg tablets and the reference (R) Robaxin<sup>®</sup> 500 mg tablets (3 tablets, total dose: 1500 mg) under fasting conditions, a...
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2025-03-01
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| author | Ana Ascaso-del-Rio Paola Camargo-Mamani Inmaculada Gilaberte Mónica Díez-Hochleitner Leonor Laredo-Velasco Teresa Iglesias-Hernangómez María Rosario Salas-Butrón Laura Galán Caballero Iván Alejandro Díaz-Rengifo Carla Pérez-Ingidua Emilio Vargas-Castrillón Antonio Portolés-Pérez |
| author_facet | Ana Ascaso-del-Rio Paola Camargo-Mamani Inmaculada Gilaberte Mónica Díez-Hochleitner Leonor Laredo-Velasco Teresa Iglesias-Hernangómez María Rosario Salas-Butrón Laura Galán Caballero Iván Alejandro Díaz-Rengifo Carla Pérez-Ingidua Emilio Vargas-Castrillón Antonio Portolés-Pérez |
| author_sort | Ana Ascaso-del-Rio |
| collection | DOAJ |
| description | <b>Objective:</b> This study aimed to assess the bioequivalence of two oral methocarbamol formulations, as follows: the test (T) methocarbamol 1500 mg tablets and the reference (R) Robaxin<sup>®</sup> 500 mg tablets (3 tablets, total dose: 1500 mg) under fasting conditions, and compare their pharmacokinetic performance. <b>Methods:</b> This was a single-center, phase I, randomized, open-label (blinded for analytical determination), two-sequence, two-period, crossover, bioequivalence study. A total of 32 healthy volunteers were randomly assigned to receive the T-R or R-T administration sequence. Each volunteer received a single dose of each methocarbamol formulation (T or R) separated by a washout period of 7 days. To evaluate the pharmacokinetic profile, blood samples were collected at nineteen time points after dosing. <b>Results:</b> The arithmetic mean C<sub>max</sub> was 31.72 µg/mL for R and 32.39 µg/mL for T, and the arithmetic mean AUC<sub>0−t</sub> was 90.25 h × µg/mL and 89.72 h × µg/mL, respectively. All adverse events reported were mild for both formulations. The 90% confidence intervals for the corresponding logarithmically transformed geometric mean ratios of C<sub>max</sub> and AUC<sub>0−t</sub> fell within the acceptance interval of 80.00–125.00%, as their values were 91.67–112.47% for ln(C<sub>max</sub>) and 92.34–103.47% for ln(AUC<sub>0−t</sub>). <b>Conclusion:</b> Therefore, one tablet of methocarbamol 1500 mg was found to be bioequivalent to the Robaxin<sup>®</sup> 500 mg tablets (3 tablets), with comparable tolerability and safety profiles. |
| format | Article |
| id | doaj-art-fe4d01233fb04efb96fecc81e48011bf |
| institution | Kabale University |
| issn | 1424-8247 |
| language | English |
| publishDate | 2025-03-01 |
| publisher | MDPI AG |
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| spelling | doaj-art-fe4d01233fb04efb96fecc81e48011bf2025-08-20T03:43:37ZengMDPI AGPharmaceuticals1424-82472025-03-0118335410.3390/ph18030354Bioequivalence Study of Two Oral Methocarbamol Formulations in Healthy Subjects Under Fasting Conditions: A Randomized, Open-Label, Crossover Clinical TrialAna Ascaso-del-Rio0Paola Camargo-Mamani1Inmaculada Gilaberte2Mónica Díez-Hochleitner3Leonor Laredo-Velasco4Teresa Iglesias-Hernangómez5María Rosario Salas-Butrón6Laura Galán Caballero7Iván Alejandro Díaz-Rengifo8Carla Pérez-Ingidua9Emilio Vargas-Castrillón10Antonio Portolés-Pérez11Clinical Pharmacology Department, Hospital Clínico San Carlos, C/Prof Martín Lagos s/n, 28040 Madrid, SpainClinical Research Department, Faes Farma, Av. Autonomía 10, 48940 Leioa, SpainClinical Research Department, Faes Farma, Av. Autonomía 10, 48940 Leioa, SpainClinical Research Department, Faes Farma, Av. Autonomía 10, 48940 Leioa, SpainClinical Pharmacology Department, Hospital Clínico San Carlos, C/Prof Martín Lagos s/n, 28040 Madrid, SpainClinical Pharmacology Department, Hospital Clínico San Carlos, C/Prof Martín Lagos s/n, 28040 Madrid, SpainClinical Pharmacology Department, Hospital Clínico San Carlos, C/Prof Martín Lagos s/n, 28040 Madrid, SpainClinical Pharmacology Department, Hospital Clínico San Carlos, C/Prof Martín Lagos s/n, 28040 Madrid, SpainInstituto de Investigación Sanitaria del Hospital Clínico San Carlos, C/Prof Martín Lagos s/n, 28040 Madrid, SpainClinical Pharmacology Department, Hospital Clínico San Carlos, C/Prof Martín Lagos s/n, 28040 Madrid, SpainClinical Pharmacology Department, Hospital Clínico San Carlos, C/Prof Martín Lagos s/n, 28040 Madrid, SpainClinical Pharmacology Department, Hospital Clínico San Carlos, C/Prof Martín Lagos s/n, 28040 Madrid, Spain<b>Objective:</b> This study aimed to assess the bioequivalence of two oral methocarbamol formulations, as follows: the test (T) methocarbamol 1500 mg tablets and the reference (R) Robaxin<sup>®</sup> 500 mg tablets (3 tablets, total dose: 1500 mg) under fasting conditions, and compare their pharmacokinetic performance. <b>Methods:</b> This was a single-center, phase I, randomized, open-label (blinded for analytical determination), two-sequence, two-period, crossover, bioequivalence study. A total of 32 healthy volunteers were randomly assigned to receive the T-R or R-T administration sequence. Each volunteer received a single dose of each methocarbamol formulation (T or R) separated by a washout period of 7 days. To evaluate the pharmacokinetic profile, blood samples were collected at nineteen time points after dosing. <b>Results:</b> The arithmetic mean C<sub>max</sub> was 31.72 µg/mL for R and 32.39 µg/mL for T, and the arithmetic mean AUC<sub>0−t</sub> was 90.25 h × µg/mL and 89.72 h × µg/mL, respectively. All adverse events reported were mild for both formulations. The 90% confidence intervals for the corresponding logarithmically transformed geometric mean ratios of C<sub>max</sub> and AUC<sub>0−t</sub> fell within the acceptance interval of 80.00–125.00%, as their values were 91.67–112.47% for ln(C<sub>max</sub>) and 92.34–103.47% for ln(AUC<sub>0−t</sub>). <b>Conclusion:</b> Therefore, one tablet of methocarbamol 1500 mg was found to be bioequivalent to the Robaxin<sup>®</sup> 500 mg tablets (3 tablets), with comparable tolerability and safety profiles.https://www.mdpi.com/1424-8247/18/3/354Robaxinmethocarbamolbioequivalencebioequivalence studymethocarbamol pharmacokineticsmethocarbamol bioequivalence |
| spellingShingle | Ana Ascaso-del-Rio Paola Camargo-Mamani Inmaculada Gilaberte Mónica Díez-Hochleitner Leonor Laredo-Velasco Teresa Iglesias-Hernangómez María Rosario Salas-Butrón Laura Galán Caballero Iván Alejandro Díaz-Rengifo Carla Pérez-Ingidua Emilio Vargas-Castrillón Antonio Portolés-Pérez Bioequivalence Study of Two Oral Methocarbamol Formulations in Healthy Subjects Under Fasting Conditions: A Randomized, Open-Label, Crossover Clinical Trial Pharmaceuticals Robaxin methocarbamol bioequivalence bioequivalence study methocarbamol pharmacokinetics methocarbamol bioequivalence |
| title | Bioequivalence Study of Two Oral Methocarbamol Formulations in Healthy Subjects Under Fasting Conditions: A Randomized, Open-Label, Crossover Clinical Trial |
| title_full | Bioequivalence Study of Two Oral Methocarbamol Formulations in Healthy Subjects Under Fasting Conditions: A Randomized, Open-Label, Crossover Clinical Trial |
| title_fullStr | Bioequivalence Study of Two Oral Methocarbamol Formulations in Healthy Subjects Under Fasting Conditions: A Randomized, Open-Label, Crossover Clinical Trial |
| title_full_unstemmed | Bioequivalence Study of Two Oral Methocarbamol Formulations in Healthy Subjects Under Fasting Conditions: A Randomized, Open-Label, Crossover Clinical Trial |
| title_short | Bioequivalence Study of Two Oral Methocarbamol Formulations in Healthy Subjects Under Fasting Conditions: A Randomized, Open-Label, Crossover Clinical Trial |
| title_sort | bioequivalence study of two oral methocarbamol formulations in healthy subjects under fasting conditions a randomized open label crossover clinical trial |
| topic | Robaxin methocarbamol bioequivalence bioequivalence study methocarbamol pharmacokinetics methocarbamol bioequivalence |
| url | https://www.mdpi.com/1424-8247/18/3/354 |
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