[Pharmacokinetics and bioequivalence of eperisone hydrochloride tablet in healthy subjects].
OBJECTIVE
To develop a HPLC-ESI-MS assay for determination of eperisone hydrochloride in human plasma and investigate the pharmacokinetics and bioequivalence of two eperisone hydrochloride tablets in human.


METHODS
Buflomedil hydrochloride was used as the internal standard. After alkalized with saturated sodium bicarbonate solution, plasma was extracted with diethylether-cyclohexane (1:1) and separated using HPLC on a reversed-phase C18 column with a mobile phase of 10 mmol x L(-1) ammonium acetate buffer solution (adjusted to pH 3.88 with acetic acid)-methanol (20:80). HPLC-ESI-MS was performed in the selected ion monitoring (SIM) mode using target ions at m/z 260 for eperisone and m/z 308 for the internal standard. A randomized crossover design was performed in 20 healthy volunteers. In the two study periods, a single 100 mg dose of each tablet was administered to each volunteer.


RESULTS
Calibration curve was linear over the range of 0.02-20 microg x L(-1). The limit of quantification for eperisone hydrochloride in plasma was 0.02 microg x L(-1). The main pharmacokinetics parameters T1/2, Tmax and Cmax were (2.7 +/- 0.4) h, (1.1 +/- 0.5) h and (2.8 +/- 2.8) microg x L(-1) for the reference tablet; (2.8 +/- 0.5) h, (1.1 +/- 0.4) h and (3 +/- 4) microg x L(-1) for the test tablet, respectively. The relative bioavalability of the test tablet was (101 +/- 13)%.


CONCLUSIONS
The assay was proved to be sensitive, accurate and convenient. The two formulations were bioequivalent.
Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing 210009, China.
Xin
X
Wei
Li
L
Ding
Jia-min
JM
Gao
Jun
J
Li
Sheng-qiang
SQ
Zhang
Jian-ping
JP
Shen
Yin-di
YD
Zhang
D000328:Adult; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D008297:Male; D011427:Propiophenones / Q000008:administration & dosage / Q000493:pharmacokinetics*; D021241:Spectrometry, Mass, Electrospray Ionization; D013607:Tablets; D013810:Therapeutic Equivalency
D011427:Propiophenones; D013607:Tablets; C030848:eperisone