• Biomolecules & Therapeutics
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• v.11 no.2
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• pp.145-150
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• 2003

The bioequivalence of two tablet formulations of 12.72mg domperidone maleate (Sinil "$Perinal^{\circledR}$" tablets vs. Janssen Korea "Motilium-$M^{\circledR}$" tablets) was assessed in healthy Korean volunteers after oral administration in a randomized crossover study. Blood samples were collected at spccified time intervals, and plasma concentration was measured as the amount of domperidone base using a validated HPLC method. The pharmacokinetic parameters of $AUC_{0{\rightarrow}48},\; C_{max},\;T_{max}$ and $t_{1/2}$ were determined from plasma concentration-time profile of two formulations. Any significant statistical differences were not observed between these two formulations. On the evaluation of bioequivalence according to Korea Food and Drug Administration Guideline, 90％ confidence limits after logmithmic transformation fell within the acceptable range (log 0.8∼log 1.25). Based on these data, it can be concluded that two domperidone maleate tablets showed comparable pharmacokinetic profiles, which means that the Sinil "$Perinal^{\circledR}$" tablet is bioequivalent to the Janssen Korea ""Motilium-M$^{\circledR}$".

• Journal of Pharmaceutical Investigation
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• v.39 no.1
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• pp.65-71
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• 2009

The aim of the present study was to evaluate the bioequivalence of two domperidone maleate tablets, Motilium-$M^{(R)}$ Tablet (Janssen Korea Ltd., reference product) and $Toriem^{(R)}$ Tablet (Daewon Pharm. Co., Ltd., test product). Domperidone was extracted by liquid-liquid extraction using tert-butyl methyl ether and separated in less than 3 min on $C_{18}$ reverse-phase column using an isocratic elution. A tandem mass spectrometer, as detector, was used for quantitative analysis in positive mode by a multiple reaction monitoring mode to monitor the m/z $426.1{\rightarrow}119.1$ and the m/z $837.4{\rightarrow}158.2$ transitions for domperidone and the internal standard (roxithromycin), respectively. Calibration curves, from $0.05{\sim}50$ ng/mL of domperidone, showed correlation coefficients (r) higher than 0.9941. Intra day and inter day precision (C.V. %) for quality control were ranged from 10.04 to 16.09% and from 10.87 to 18.69%, respectively. The lower limit of quantification (LLOQ) of domperidone was 0.05 ng/mL. The method described is precise and sensitive and has been successfully applied to the study of bioequivalence of domperidone in 24 healthy Korean volunteers. Twenty-four healthy male Korean volunteers received a single dose of each medicine ($2{\times}12.72\;mg$ domperidone maleate) in a $2{\times}2$ crossover study. There was a one-week washout period between the doses. Plasma concentrations of domperidone were monitored for over a period of 24 hr after the administration. $AUC_{0-t}$ (the area under the plasma concentration-time curve) was calculated by the linear trapezoidal rule. $C_{max}$ (maximum plasma drug concentration) and $T_{max}$ (time to reach $C_{max}$) were compiled from the plasma concentration-time data. The 90% confidence intervals for the log transformed data were within acceptable range of log 0.8 to log 1.25 (e.g., $log\;0.92{\sim}log\;1.05$ for $AUC_{0-t}$, $log\;0.81{\sim}log\;1.05$ for $C_{max}$). The major parameters, $AUC_{0-t}$ and $C_{max}$ met the criteria of KFDA for bioequivalence indicating that $Toriem^{(R)}$ tablet is bioequivalent to Motilium-$M^{(R)}$ tablet.

• Korean Journal of Clinical Pharmacy
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• v.18 no.2
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• pp.106-113
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• 2008

The aim of this study was to evaluate the bioequivalence of two domperidone preparations. Bioequivalence assessment was conducted on 34 healthy volunteers who received two tablets (Domperidone Maleate, 12.72 mg/tablet) in the fasting state, in a randomized balanced $2{\times}2$ cross-over study design. This whole study was performed according to the implementation guidelines of the Korea Food Drug Administration. After dosing of two tablets, blood samples were collected serially for a period of 36 hours. Plasma was analyzed for domperidone by using LC/MS/MS assay method. The analysis system was validated in specificity, accuracy, precision, and linearity. $AUC_t$, (the area under the plasma concentration-time curve from the zero-time to 36 hr) was calculated through the trapezoidal rule. $C_{max}$ (maximum plasma drug concentration) and $T_{max}$ (time to reach $C_{max}$) were compiled from the plasma domperidone concentration-time data of each volunteer. No significant sequence effect was found for the bioavailability parameters indicating that the cross-over design was properly performed. The 90%-Confidence intervals of the $AUC_t$ ratio and the $C_{max}$ were from log 0.8007 to log 1.1240 and log 0.8645- log 1.2483, respectively. These values were within the acceptable bioequivalence intervals between 0.80 and 1.25. Therefore, this study demonstrated that two formulations have bioequivalence with respect to the rate and extent of absorption.