Abstract

Background: Cyclobenzaprine is a skeletal muscle relaxant used in management of focal muscular disturbances and as an adjunct to physical therapy for relief of muscle spasm.

Aim: Establishment of a bio-analytical method in order to quantify cyclobenzaprine in plasma and investigate cyclobenzaprine pharmacokinetics in human plasma and its application in clinical studies including comparative bioavailability studies.

Methods: After extraction of cyclobenzaprine from plasma, analysis was performed with mobile phase ratio of acetonitrile: 0.1% formic acid 90:10 at a flow rate of 0.5 ml/min, ESI positive mode, and m/z 276.6à216.4 for cyclobenzaprine, and 325.1à109 for escitalopram (IS). The bioequivalence study was involving 24 volunteers in a crossover pattern. Pharmacokinetic parameters AUC_0-t, AUC_0-inf, C_max and T_max used for assessment of bioequivalence of the generic and reference products_.

Results: The developed bioanalytical method showed that the average recovery of cyclobenzaprine from plasma was 82.883%, LLOQ 0.05 ng/ml. Correlation coefficient (r²) 0.9998. Analysis of variance showed that there was no significant difference between generic and reference products.

Conclusion: The established LC/MS/MS method is fully validated for the determination of cyclobenzaprine in biological samples and is suitable for clinical pharmacokinetic studies, clinical trials and monitoring drug levels in plasma to ensure clinical efficacy and safety, avoid therapeutic failure or incidence of adverse events. Moreover, generic product was found to provide the same rate and extent of drug absorption as the reference product.

Keywords: Cyclobenzaprine; LC/MS/MS; Muscle Spasm; Sustained Release Capsule; Therapeutic Drug Monitoring

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Citation

Citation: Nagwa A Sabri., et al. “Quantification of Cyclobenzaprine in Human Plasma by LC/MS/MS and its Pharmacokinetics Application". Acta Scientific Pharmaceutical Sciences 4.11 (2020): 90-96.

Copyright

Copyright: © 2020 Nagwa A Sabri., et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.