Bioequivalence Study of Two Oral Methocarbamol Formulations in Healthy Subjects Under Fasting Conditions: A Randomized, Open-Label, Crossover Clinical Trial

Ascaso-del-Rio, Ana; Camargo-Mamani, Paola; Gilaberte, Inmaculada; Díez-Hochleitner, Mónica; Laredo-Velasco, Leonor; Iglesias-Hernangómez, Teresa; Salas-Butrón, María Rosario; Galán Caballero, Laura; Díaz-Rengifo, Iván Alejandro; Pérez-Ingidua, Carla; Vargas-Castrillón, Emilio; Portolés-Pérez, Antonio

doi:10.3390/ph18030354

Open AccessArticle

Bioequivalence Study of Two Oral Methocarbamol Formulations in Healthy Subjects Under Fasting Conditions: A Randomized, Open-Label, Crossover Clinical Trial

by

Ana Ascaso-del-Rio

^1,2,3

,

Paola Camargo-Mamani

^4,*

,

Inmaculada Gilaberte

⁴,

Mónica Díez-Hochleitner

⁴,

Leonor Laredo-Velasco

^1,2,3,

Teresa Iglesias-Hernangómez

^1,2,

María Rosario Salas-Butrón

^1,2,

Laura Galán Caballero

^1,2,

Iván Alejandro Díaz-Rengifo

²

,

Carla Pérez-Ingidua

^1,2,

Emilio Vargas-Castrillón

^1,2,3

and

Antonio Portolés-Pérez

^1,2,3

¹

Clinical Pharmacology Department, Hospital Clínico San Carlos, C/Prof Martín Lagos s/n, 28040 Madrid, Spain

²

Instituto de Investigación Sanitaria del Hospital Clínico San Carlos, C/Prof Martín Lagos s/n, 28040 Madrid, Spain

³

Pharmacology and Toxicology Department, School of Medicine, Universidad Complutense de Madrid (UCM), 28040 Madrid, Spain

⁴

Clinical Research Department, Faes Farma, Av. Autonomía 10, 48940 Leioa, Spain

^*

Author to whom correspondence should be addressed.

Pharmaceuticals 2025, 18(3), 354; https://doi.org/10.3390/ph18030354

Submission received: 9 January 2025 / Revised: 24 February 2025 / Accepted: 27 February 2025 / Published: 1 March 2025

(This article belongs to the Section Pharmacology)

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Abstract

Objective: 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^® 500 mg tablets (3 tablets, total dose: 1500 mg) under fasting conditions, and compare their pharmacokinetic performance. Methods: 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. Results: The arithmetic mean C_max was 31.72 µg/mL for R and 32.39 µg/mL for T, and the arithmetic mean AUC_0−t 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_max and AUC_0−t fell within the acceptance interval of 80.00–125.00%, as their values were 91.67–112.47% for ln(C_max) and 92.34–103.47% for ln(AUC_0−t). Conclusion: Therefore, one tablet of methocarbamol 1500 mg was found to be bioequivalent to the Robaxin^® 500 mg tablets (3 tablets), with comparable tolerability and safety profiles.

Keywords: Robaxin; methocarbamol; bioequivalence; bioequivalence study; methocarbamol pharmacokinetics; methocarbamol bioequivalence

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MDPI and ACS Style

Ascaso-del-Rio, A.; Camargo-Mamani, P.; Gilaberte, I.; Díez-Hochleitner, M.; Laredo-Velasco, L.; Iglesias-Hernangómez, T.; Salas-Butrón, M.R.; Galán Caballero, L.; Díaz-Rengifo, I.A.; Pérez-Ingidua, C.; et al. Bioequivalence Study of Two Oral Methocarbamol Formulations in Healthy Subjects Under Fasting Conditions: A Randomized, Open-Label, Crossover Clinical Trial. Pharmaceuticals 2025, 18, 354. https://doi.org/10.3390/ph18030354

AMA Style

Ascaso-del-Rio A, Camargo-Mamani P, Gilaberte I, Díez-Hochleitner M, Laredo-Velasco L, Iglesias-Hernangómez T, Salas-Butrón MR, Galán Caballero L, Díaz-Rengifo IA, Pérez-Ingidua C, et al. Bioequivalence Study of Two Oral Methocarbamol Formulations in Healthy Subjects Under Fasting Conditions: A Randomized, Open-Label, Crossover Clinical Trial. Pharmaceuticals. 2025; 18(3):354. https://doi.org/10.3390/ph18030354

Chicago/Turabian Style

Ascaso-del-Rio, Ana, 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, and et al. 2025. "Bioequivalence Study of Two Oral Methocarbamol Formulations in Healthy Subjects Under Fasting Conditions: A Randomized, Open-Label, Crossover Clinical Trial" Pharmaceuticals 18, no. 3: 354. https://doi.org/10.3390/ph18030354

APA Style

Ascaso-del-Rio, A., Camargo-Mamani, P., Gilaberte, I., Díez-Hochleitner, M., Laredo-Velasco, L., Iglesias-Hernangómez, T., Salas-Butrón, M. R., Galán Caballero, L., Díaz-Rengifo, I. A., Pérez-Ingidua, C., Vargas-Castrillón, E., & Portolés-Pérez, A. (2025). Bioequivalence Study of Two Oral Methocarbamol Formulations in Healthy Subjects Under Fasting Conditions: A Randomized, Open-Label, Crossover Clinical Trial. Pharmaceuticals, 18(3), 354. https://doi.org/10.3390/ph18030354

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Bioequivalence Study of Two Oral Methocarbamol Formulations in Healthy Subjects Under Fasting Conditions: A Randomized, Open-Label, Crossover Clinical Trial

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