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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Bibliographic Details
Published in:	Scientific reports 2020-02, Vol.10 (1), p.1867, Article 1867
Main Authors:	Ahmed, Kamran, Shoaib, Muhammad Harris, Yousuf, Rabia Ismail, Siddiqui, Fahad, Qazi, Faaiza, Iftikhar, Javeria, Ahmed, Farrukh Rafiq, Nasiri, Muhammad Iqbal
Format:	Article
Language:	eng
Subjects:	Adolescent Area Under Curve Bioavailability Biological Availability Chemistry, Pharmaceutical - methods Chromatography, Liquid - methods Controlled release Cross-Over Studies Drug delivery Healthy Volunteers Human subjects Humans Male Osmosis - physiology Pharmacokinetics Plasma - metabolism Propiophenones - blood Propiophenones - pharmacokinetics Tablets - pharmacokinetics Tandem Mass Spectrometry - methods Young Adult
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Summary:	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 AUC V /F, Cl/F and t , whereas a significant difference in C , T 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.
ISSN:	2045-2322 2045-2322