Human pharmacokinetics of the muscle relaxant, eperisone hydrochloride by liquid chromatography–electrospray tandem mass spectrometry

  • Barbara Melilli
  • Cateno Piazza
  • Daniela Cristina Vitale
  • Maria Rosa Marano
  • Andrea Pecori
  • Paolo Mattana
  • Valentina Li Volsi
  • Carmelo Iuculano
  • Francesco Cardì
  • Filippo Drago
Original Paper


Eperisone hydrochloride (4′-ethyl-2-methyl-3-piperidinopropiophenone hydrochloride) is a muscle relaxant agent, widely used in the treatment of patients with muscular contractures, low back pain or spasticity. Because of its mechanism of action (inhibition of gamma-efferent firing and local vasodilatation activity), side effects on central nervous system are rarely observed. A sensitive liquid chromatography–electrospray ionization-mass spectrometry method for determination of eperisone in human plasma has been developed, with a lower limit of quantification of 0.01 ng/mL. The method was applied to a pharmacokinetic study in 12 healthy volunteers given eperisone 100 mg as single dose on day 1 and three times daily on days 2 to 4. Eperisone was rapidly absorbed after oral administration (Tmax = 1.6 h) as it was expected by its fast-onset relaxant activity. Moreover, eperisone underwent a rapid elimination from the body (biological half-life 1.87 h), which was not modified during the repeated dosing as suggested by the Cmax cumulation observed, not different from that expected for a t1/2 of 1.87 h as suggested by the similar and negligible plasma concentration values (0.063 and 0.067 ng/mL) measured on day 4 before the morning dose and 12 h after evening dose, thus ruling out any potential risk for drug accumulation. Thus, the pharmacokinetic characteristics of eperisone provide further justification for its tolerability in patients with low back pain or spastic palsy, in which the drug is given for periods ranging from few days to several months, respectively.


Eperisone Pharmacokinetics Tandem mass spectrometry Human plasma 



Low back pain


Central nervous system








Time of maximum concentration


Maximum plasma concentration








Lower limits of quantification


Liquid chromatography–mass spectrometry triple quadrupole mass spectrometry


University of Catania Medical Center


Good clinical practice




Hepatitis B virus


Hepatitis C virus


Human immunodeficiency virus


Plasma concentration half-life


Summary of product characteristics


Revolutions per minute




High performance liquid chromatography


Electrospray ionization








Volume to volume


Mass to charge


Area under the plasma concentration curve administration to last observed concentration at time t


Terminal elimination rate constant


Area under the plasma concentration curve extrapolated to infinity time


Last quantified concentration


Analysis of variance


Area under the plasma concentration curve


Coefficient of variation


Standard deviation





We thank Dr. Giacomo Spignoli for his kind help.


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Copyright information

© Springer-Verlag France 2011

Authors and Affiliations

  • Barbara Melilli
    • 1
  • Cateno Piazza
    • 1
  • Daniela Cristina Vitale
    • 1
  • Maria Rosa Marano
    • 1
  • Andrea Pecori
    • 2
  • Paolo Mattana
    • 3
  • Valentina Li Volsi
    • 4
  • Carmelo Iuculano
    • 4
  • Francesco Cardì
    • 5
  • Filippo Drago
    • 6
  1. 1.Pharmacokinetic Unit, Unifarm Research CenterUniversity of CataniaCataniaItaly
  2. 2.EisaiSan Donato Milanese MilanoItaly
  3. 3.Alfa WassermannBolognaItaly
  4. 4.PhD School of NeuropharmacologyUniversity of CataniaCataniaItaly
  5. 5.Polyclinic Vittorio Emanuele University of CataniaCataniaItaly
  6. 6.Department of Experimental and Clinical PharmacologyUniversity of CataniaCataniaItaly

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