Title: Pharmacokinetic comparison of metronidazole colon-targeted sustained-release tablets with conventional tablets in healthy volunteers
Abstract: Objective:To determine metronidazole in human plasma by RP-HPLC method,and compare the pharmacokinetics of metronidazole colon-targeted sustained-release tablets with conventional tablets in Chinese healthy volunteers.Methods:Twelve healthy volunteers were enrolled to receive single dose and multiple-dose of metronidazole colon-targeted sustained-release tablets and conventional tablets according to a randomized cross-over design.Metronidazole concentration in plasma was determined by RP-HPLC method,and the pharmacokinetic parameters were calculated by DAS 2.0 software.Statistical analysis was performed by SPSS 17.0 program.Results:The main pharmacokinetic parameters of metronidazole test and reference preparations after a single dose were as follows:Tmax(19.50±3.43) h and(1.52±0.56) h,Cmax(1.083±0.710) mg·L-1 and(4.536±0.964) mg·L-1,AUC0~t(22.69±15.96) mg·L-1·h and(62.90±14.51) mg·L-1·h,t1/2z(10.60±1.62) h and(9.83±2.02) h,CLz/F(25.22±44.90) L·h-1 and(3.21±0.70) L·h-1,Vz/F(378.59±661.63) L and(44.18±7.90) L,respectively.The parameters after the multi-dose were:Tmax(11.25±4.58) h and(1.05±0.57) h,Cmax(3.84±1.32) mg·L-1 and(7.96±1.33) mg·L-1,AUC0~t(116.81±46.90) mg·L-1·h and(115.48±31.64) mg·L-1·h,AUCss(39.88±14.33) mg·L-1·h and(60.07±12.03) mg·L-1·h,t1/2z(10.65±1.64) h and(10.13±2.27) h,CLz/F(1.97±0.82) L·h-1 and(1.80±0.55) L·h-1,Vz/F(29.49±11.04) L and(24.94±4.45) L,respectively.Conclusion:Metronidazole colon-targeted sustained-release tablets have delayed Tmax and lower Cmax in healthy Chinese volunteers,showing the typical sustained release characteristics.
Publication Year: 2013
Publication Date: 2013-01-01
Language: en
Type: article
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