Abstract
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 AUC0-∞, AUC0-t, Vz/F, Cl/F and t1/2λz, whereas a significant difference in Cmax, Tmax 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.
Highlights
Sustained release formulations are one of the famous type of controlled release drug delivery system
The method was validated and applied in the comparative PK analysis of the optimized osmotic formulation of Eperisone in local population with immediate release tablets ingested in a single dose of 150 mg
The Quality Control samples (QCs) having Eperisone concentration of 0.4 ng/ml, 3 ng/ml and 8 ng/ml were coded as QCL, QCM and QCH, respectively
Summary
Sustained release formulations are one of the famous type of controlled release drug delivery system. Eperisone because of its mechanism of action, is comparatively devoid of the undesirable side which are usually associated with intake of centrally acting muscle relaxants[7,8,13,14,15] It is usually administered at an oral dose of 150 mg/day in three divided doses. The characteristics of Eperisone like high aqueous solubility, short duration of activity and variability in PK characteristics make it an excellent candidate to be designed as an oral osmotic drug delivery system. In the current study a sensitive, simple and less time consuming bio-analytical method for determination of Eperisone in human plasma, utilizing chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS/ MS) technique was developed by modifying the previously reported methods. The method was validated and applied in the comparative PK analysis of the optimized osmotic formulation of Eperisone in local population with immediate release tablets ingested in a single dose of 150 mg
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