金果榄中古伦宾在家兔体内的药动学研究

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Abstract Objective To study the pharmacokinetics of columbin from R adix Tinosporae in rabbits in vivo.Methods The columbin was extracted from the dried root of R adix Tinosporae,and the UPLC method for the determination of columbin was established.Chromatographic conditions,column:Acquity UPLCRBEN C18(2.1×100 mm,1.7 μm);mobile phase:0.3%phosphoric acid solution-acetonitrile(65:35);flow rate:1 ml/min;detection wavelength:225 nm;temperature:35°C.The specificity,linearity,quantitative limits,extraction recovery,precision and stability of the method were investigated.The peak area of the standard solution of different concentrations of culumbin was determined,and used to make the standard curve of the concentration of culumbin.The culumbin (50 mg/kg)was gavaged to rabbits,and limbic vein blood collection was conducted at 0,15,30,60,120,180,240,360,480 and 1400 min after administration.The blood concentration-time curve was drawn,and the corresponding pharmacokinetic parameters of culumbin in rabbits were calculated by using WinNonlin 3.3 software.Results Peak shape of the chromatogram showed that the retention time of culumbin was 16 min,with normal peak shape distribution.It was well separated from other peaks,and there was no endogenous material interference.The standard curve equation of culumbin concentration was Y=502967X+0.1501,the correlation coefficient r=0.995,the linear range was 0.00122-2.50000 nmol/L,and the minimum quantitative limit was 1.22×10-3nmol/L.The recovery rate of the plasma solution of culumbin at the mass concentration of 9.77,156.25 and 1250.00 nmol/L was over 80.0%,the average recovery rate was 84.2%,and the relative standard deviation (RSD)=3.1%.The RSD between two days of the 156.25 nmol/L culumbin plasma solution was 3.5%,the first day RSD was 1.7%,the second day RSD was 4.6%.Preserved 24 h at room temperature,repeated freezing,thawing 3 times,and-20℃cryopreservation 14 d average recovery was 90.0%-110.0%.Pharmacokinetic parameters:Tmax=68.9 min,peak concentration(Cmax)=0.0671 nmol/L,terminal elimination half-life(T1/2)=438.67 min,medication in the area under the curve(AUC)=81.49,end eliminate rate(Ke)=0.0017,clearance(CL)=20132.72,bioavailability(F)=14.08%.Conclusion The UPLC method was used to determine the concentration of columbin,and its specificity,extraction recovery and stability all meet the requirements,which is suitable for the systematic study of the pharmacokinetics of columbin in rabbits.

Key words： Columbin Radix Tinosporae Pharmacokinetic study Ultra high performance liquid chromatography

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	ZENG Hao-tao

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ZENG Hao-tao. Pharmacokinetic study of columbin from Radix Tinosporae in rabbits in vivo[J]. 中国当代医药, 2018, 25(26): 13-17.

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http://dangdaiyiyao.com/EN/ OR http://dangdaiyiyao.com/EN/Y2018/V25/I26/13

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