W. Ling
2010
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Journal
West China Journal of Pharmaceutical Sciences
Abstract
OBJECTIVE To develop a sensitive and rapid method to determine of the concentration of Benproperine phosphate in human plasma,and apply it in the relative bioavailability study of Benproperine Phosphate Sustained-release formulations.METHODS The human plasma from 24 healthy volunteers were collected at various time points after administration with single oral dose of 40 mg Benproperine Phosphate Sustained-release capsules and the tablets under fasted conditions.Plasma samples were pretreated by liquid-liquid extraction procedure and the concentration of Benproperine phosphate in human plasma was determined by LC-MS/MS.The pharmacokinetic parameters and statistic analysis were calculated by DAS ver 2.1.1 program.RESULTS The calibration curve was linear in the range from 0.25 to 500 ng·mL-1 with r = 0.9997.The lower limit of quantification of benproperine phosphate was 0.25 ng·mL-1.The RSD of LLOQ was 8.78%.The absolute recoveries of benproperine phosphate and ampicillin were above 75%.The average recoveries of Benproperine phosphate from the different concentration plasmas were 100.41%,100.81%,105.96%,respectively.Both the intra-day and inter-day RSD were less than 11%.The main pharmacokinetic parameters of Benproperine Phosphate Sustained-release capsules and the tablets were as follows:Tmax was 4.21 ± 0.55,4.19 ± 0.51 h;Cmax was 82.12 ± 14.27,78.43 ± 10.44 ng·mL-1;AUC0-72 was 2113.45 ± 770.19,2076.89 ± 818.25 μg·h·L-1.CONCLUSION The method is simple,rapid,sensitive and precise,which is more suitable for pharmacokinetic studies in human than the reported methods.Based on the calculated results,there was no statistically significant difference for benproperine phosphate between the two formulations on pharmacokinetic parameters.