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目的:研究苦参碱肌肉注射给药在大鼠体内的药代动力学。方法:采用高效液相色谱法测定苦参碱的血药浓度,Shim-pack VP-ODS色谱柱(4.6 mm×150 mm,5μm);流动相乙腈-0.02 mol.L-1乙酸铵水溶液-三乙胺(30∶70∶0.04);流速1 mL.min-1;检测波长220 nm;柱温40℃;进样量20μL。用DAS 2.1.1药动学程序处理苦参碱的血药浓度-时间数据。结果:苦参碱在大鼠体内的药代动力学符合二室开放模型,Cmax为21.113 9 mg.L-1,tmax为0.75 h,t1/2α为1.34 h,t1/2β为3.509h,AUC0～t为90.984 mg.h-1.L-1,AUC0～∞为100.346 mg.h-1.L-1。结论:与口服给药相比,肌肉注射给药的苦参碱吸收较好,从中央室到周边室的分布也较快;其绝对生物利用度也比口服给药高,推测其药理作用的强度比口服给药强,维持时间也比口服给药长。
Objective: To study the pharmacokinetics of matrine administered intramuscularly in rats. Methods: The plasma concentration of matrine was determined by HPLC. Shim-pack VP-ODS column (4.6 mm × 150 mm, 5 μm) was used. The mobile phase was acetonitrile-0.02 mol·L-1 ammonium acetate aqueous solution- Ethylamine (30:70:0.04); flow rate 1 mL.min-1; detection wavelength 220 nm; column temperature 40 ℃; injection volume 20μL. Maternal plasma concentration-time data was processed using the DAS 2.1.1 pharmacokinetic program. Results: The pharmacokinetics of matrine in rats were in accordance with the two-compartment open model with Cmax of 21.113 9 mg.L-1, tmax of 0.75 h, t1 / 2α of 1.34 h, t1 / 2β of 3.509 h and AUC0 ~ T was 90.984 mg.h-1.L-1, AUC0 ~ ∞ was 100.346 mg.h-1.L-1. Conclusion: Compared with the oral administration, intramuscular injection of matrine is better absorbed from the central chamber to the peripheral compartment distribution faster; its absolute bioavailability than oral administration, speculated that its pharmacological effects Strength than oral administration, maintenance time is also longer than oral administration.