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Comparative pharmacokinetics of osmotic-controlled and immediate-release Eperisone tablet formulation in healthy human subjects using a sensitive plasma LC-ESI-MS/MS method

To evaluate and compare the pharmacokinetic (PK) characteristics of a newly developed oral osmotically controlled drug delivery system of Eperisone 150 mg tablets with Eperisone immediate release (IR) marketed tablet brand as a reference formulation. It was a single dose, two treatment, two sequence...

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Autores principales: Ahmed, Kamran, Shoaib, Muhammad Harris, Yousuf, Rabia Ismail, Siddiqui, Fahad, Qazi, Faaiza, Iftikhar, Javeria, Ahmed, Farrukh Rafiq, Nasiri, Muhammad Iqbal
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7002734/
https://www.ncbi.nlm.nih.gov/pubmed/32024955
http://dx.doi.org/10.1038/s41598-020-58801-1
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author Ahmed, Kamran
Shoaib, Muhammad Harris
Yousuf, Rabia Ismail
Siddiqui, Fahad
Qazi, Faaiza
Iftikhar, Javeria
Ahmed, Farrukh Rafiq
Nasiri, Muhammad Iqbal
author_facet Ahmed, Kamran
Shoaib, Muhammad Harris
Yousuf, Rabia Ismail
Siddiqui, Fahad
Qazi, Faaiza
Iftikhar, Javeria
Ahmed, Farrukh Rafiq
Nasiri, Muhammad Iqbal
author_sort Ahmed, Kamran
collection PubMed
description To evaluate and compare the pharmacokinetic (PK) characteristics of a newly developed oral osmotically controlled drug delivery system of Eperisone 150 mg tablets with Eperisone immediate release (IR) marketed tablet brand as a reference formulation. It was a single dose, two treatment, two sequence, randomized, crossover study, involving 12 healthy human subjects. A modified, sensitive LC-ESI-MS/MS method was developed and validated as per FDA guidelines for estimation of Eperisone in plasma using a simple extraction and quick protein precipitation method. Non-compartmental pharmacokinetic model was used for PK analysis. Results were statistically compared using logarithmically transformed data, where p > 0.05 was considered as non-significant with 90% CI limit of 0.8–1.25. The bio-analytical method used for estimating drug plasma concentration was found to be simple, selective, linear, accurate and precise with 0.01 ng/ml as limit of detection. The comparative PK analysis revealed an insignificant difference in AUC(0-∞,) AUC(0-t,) V(z)/F, Cl/F and t(1/2λz), whereas a significant difference in C(max), T(max) and MTTs were found. The relative bioavailability of Eperisone osmotic tablet was 109.7%. The osmotic controlled release drug formulation was found to release Eperisone for an extended period with less inter individual fluctuation in pharmacokinetic variables.
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spelling pubmed-70027342020-02-14 Comparative pharmacokinetics of osmotic-controlled and immediate-release Eperisone tablet formulation in healthy human subjects using a sensitive plasma LC-ESI-MS/MS method Ahmed, Kamran Shoaib, Muhammad Harris Yousuf, Rabia Ismail Siddiqui, Fahad Qazi, Faaiza Iftikhar, Javeria Ahmed, Farrukh Rafiq Nasiri, Muhammad Iqbal Sci Rep Article To evaluate and compare the pharmacokinetic (PK) characteristics of a newly developed oral osmotically controlled drug delivery system of Eperisone 150 mg tablets with Eperisone immediate release (IR) marketed tablet brand as a reference formulation. It was a single dose, two treatment, two sequence, randomized, crossover study, involving 12 healthy human subjects. A modified, sensitive LC-ESI-MS/MS method was developed and validated as per FDA guidelines for estimation of Eperisone in plasma using a simple extraction and quick protein precipitation method. Non-compartmental pharmacokinetic model was used for PK analysis. Results were statistically compared using logarithmically transformed data, where p > 0.05 was considered as non-significant with 90% CI limit of 0.8–1.25. The bio-analytical method used for estimating drug plasma concentration was found to be simple, selective, linear, accurate and precise with 0.01 ng/ml as limit of detection. The comparative PK analysis revealed an insignificant difference in AUC(0-∞,) AUC(0-t,) V(z)/F, Cl/F and t(1/2λz), whereas a significant difference in C(max), T(max) and MTTs were found. The relative bioavailability of Eperisone osmotic tablet was 109.7%. The osmotic controlled release drug formulation was found to release Eperisone for an extended period with less inter individual fluctuation in pharmacokinetic variables. Nature Publishing Group UK 2020-02-05 /pmc/articles/PMC7002734/ /pubmed/32024955 http://dx.doi.org/10.1038/s41598-020-58801-1 Text en © The Author(s) 2020 Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.
spellingShingle Article
Ahmed, Kamran
Shoaib, Muhammad Harris
Yousuf, Rabia Ismail
Siddiqui, Fahad
Qazi, Faaiza
Iftikhar, Javeria
Ahmed, Farrukh Rafiq
Nasiri, Muhammad Iqbal
Comparative pharmacokinetics of osmotic-controlled and immediate-release Eperisone tablet formulation in healthy human subjects using a sensitive plasma LC-ESI-MS/MS method
title Comparative pharmacokinetics of osmotic-controlled and immediate-release Eperisone tablet formulation in healthy human subjects using a sensitive plasma LC-ESI-MS/MS method
title_full Comparative pharmacokinetics of osmotic-controlled and immediate-release Eperisone tablet formulation in healthy human subjects using a sensitive plasma LC-ESI-MS/MS method
title_fullStr Comparative pharmacokinetics of osmotic-controlled and immediate-release Eperisone tablet formulation in healthy human subjects using a sensitive plasma LC-ESI-MS/MS method
title_full_unstemmed Comparative pharmacokinetics of osmotic-controlled and immediate-release Eperisone tablet formulation in healthy human subjects using a sensitive plasma LC-ESI-MS/MS method
title_short Comparative pharmacokinetics of osmotic-controlled and immediate-release Eperisone tablet formulation in healthy human subjects using a sensitive plasma LC-ESI-MS/MS method
title_sort comparative pharmacokinetics of osmotic-controlled and immediate-release eperisone tablet formulation in healthy human subjects using a sensitive plasma lc-esi-ms/ms method
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7002734/
https://www.ncbi.nlm.nih.gov/pubmed/32024955
http://dx.doi.org/10.1038/s41598-020-58801-1
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