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目的:对泽泻中主要成分23-乙酰泽泻醇B进行不同给药方式的药代动力学和口服生物利用度研究。方法:大鼠分别注射和灌服23-乙酰泽泻醇B,于不同时间点采血;采用HPLC-UV法检测血浆中23-乙酰泽泻醇B,流动相为乙腈-水(80∶20),检测波长210 nm,流速1.0 mL·min-1;绘制药时曲线,建立药代动力学模型,计算药动学参数和绝对生物利用度(F)。结果:主要药动学参数为口服:Tmax(122.15±15.23)min,Cmax(9.89±0.87)mg·L-1,t1/2(58.72±6.23)min,AUC0-t(1 854.970±142.31)μg.min·mL-1,AUC0-∞(1 875.81±144.27)μg.min·mL-1,CL/F(2.89±0.13)mL·min-1;静脉注射:Tmax(10.04±0.78)min,Cmax(42.59±3.47)μg·mL-1,t1/2(32.05±2.53)min,AUC0-t(2 810.08±178.70)μg.min-1·mL-1,AUC0-∞(2 812.41±224.63)μg·min-1·mL-1,CL/F(1.74±0.54)mL·min-1;平均F为44.46%。结论:23-乙酰泽泻醇B在大鼠体内吸收缓慢但较完全,消除相对较快。说明23-乙酰泽泻醇B具有良好的药代动力学特征,便于开发成临床使用方便的药物。
OBJECTIVE: To study pharmacokinetics and oral bioavailability of 23-acetyl-alisol B, a major component of Alisma orientalis, in different administration modes. Methods: Rats were injected and orally administered 23-acetyl estradiol B at different time points. The plasma 23-acetyl estradiol B was detected by HPLC-UV with the mobile phase of acetonitrile-water (80:20) , The detection wavelength was 210 nm and the flow rate was 1.0 mL · min-1. The pharmacokinetic model was established and the pharmacokinetic parameters and absolute bioavailability (F) were calculated. RESULTS: The main pharmacokinetic parameters were oral: Tmax (122.15 ± 15.23) min, Cmax (9.89 ± 0.87) mg · L-1, t1 / 2 (58.72 ± 6.23) min and AUC0-t (1 854.970 ± 142.31) μg (10.87 ± 0.41) mL · min-1, AUC0-∞ (1875.81 ± 144.27) μg.min · mL-1 and CL / F (42.59 ± 3.47) μg · mL-1, t1 / 2 (32.05 ± 2.53) min, AUC0-t (2 810.08 ± 178.70) μg.min-1 · mL-1 and AUC0-∞ (2 812.41 ± 224.63) μg · Min-1 · mL-1, CL / F (1.74 ± 0.54) mL · min-1; average F was 44.46%. Conclusion: 23-Acetyl-alisol B absorbed slowly but completely in rats, eliminating relatively fast. Description 23-acetyl alispalol B has good pharmacokinetic characteristics, easy to develop into clinical easy-to-use drugs.