论文部分内容阅读
目的研究槐果碱的人体药代动力学,为临床应用提供依据。方法采用高效液相色谱法测定人血清槐果碱浓度,并对其药代动力学进行研究。结果槐果碱的绝对回收率>70%,相对回收率为100.7%~108.7%,日内精密度和<4%,日间精密度均<5%,血药浓度在0.625~20.0μg/mL范围内呈线性相关(r=0.99998)。10名健康志愿者静脉滴注槐果碱6 mg/kg后,血清样本检测显和药时曲线符合二室开放模型,T1/2α为27.459 m in,T1/2β为228.16 m in,CL(s)为0.0073 L.kg-1.m in-1,Vc为1.5182 L/kg,Tm ax:30 m in,Cm ax:(3.5445±0.9876)μg/mL;尿样检测发现,24 h内64.77%的槐果碱以原形由尿排出,故其主要排泄器官为肾脏。结论临床给予槐果碱6 mg/kg的剂量是安全的。
Objective To study the human pharmacokinetics of sophocarpine and provide basis for clinical application. Methods Human serum sophocarpine concentration was determined by high performance liquid chromatography and its pharmacokinetics was studied. Results The absolute recovery of somaline was more than 70%, the relative recovery was 100.7%-108.7%, the intraday precision was less than 4%, the intraday precision was less than 5%, and the plasma concentration was in the range of 0.625-20.0μg/mL. There was a linear correlation (r=0.99998). After intravenous infusion of sophocarpine 6 mg/kg in 10 healthy volunteers, the serum test and drug-time curve of serum samples met the two-compartment open model, T1/2α was 27.459 min, T1/2β was 228.16 min, CL(s). ) was 0.0073 L.kg-1.m in-1, Vc was 1.5182 L/kg, Tm ax: 30 m in, Cm ax: (3.5445±0.9876) μg/mL; urine samples detected 64.77% within 24 h. The sophocarpine is excreted in urine by its original form, so its main excretory organ is the kidney. Conclusion The clinical dose of sophocarpine 6 mg/kg is safe.