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目的明确双黄连粉针剂不同剂量给药后有效成分黄芩苷在大鼠体内的动态变化规律及其在唾液中的分布情况。方法大鼠静脉注射双黄连粉针后,反相高效液相色谱法测定黄芩苷的血液、唾液浓度,采用药动学软件MULTI97V10程序进行数据处理,确定药动学参数。结果双黄连粉针剂高、中、低剂量(740,555,370 mg.kg-1)给药后有效成分黄芩苷在大鼠体内符合二室模型分布,其高、中、低剂量主要药动学参数分别如下:t1/2=(0.79±0.12)h,AUC=(1.30±0.13)mg.h.mL-1,Vc=(0.21±0.036)L,CL=(0.19±0.019)L.h-1;t1/2=1.52±0.14 h,AUC=(1.22±0.20)mg.h.mL-1,Vc=(0.36±0.04)L,CL=(0.16±0.030)L.h-1;t1/2=(0.34±0.021)h,AUC=(0.22±0.004)mg.h.mL-1,Vc=(0.33±0.027)L,CL=(0.66±0.014)L.h-1。高剂量给药后黄芩苷唾液浓度范围为:0.11~0.78μg.mL-1,中、低剂量给药后唾液样品中未检测到黄芩苷。结论通过高、中、低剂量及相应的AUC对比,AUC随剂量增加不成比例增加,说明双黄连粉针给药后黄芩苷在体内呈非线性药动学消除过程。另外,黄芩苷向唾液中分布的浓度较血液低的多。
Objective To determine the dynamic changes of baicalin in rats and its distribution in saliva after different doses of Shuanghuanglian injection. Methods After the rats were injected intravenously with Shuanghuanglian injection, the blood and saliva concentrations of baicalin were determined by reversed-phase high performance liquid chromatography. The pharmacokinetic parameters were determined by the software MULTI97V10. Results Shuanghuanglian injection after administration of high, medium and low doses (740,555,370 mg.kg-1) baicalin in rats in line with the two-compartment model distribution, the main pharmacokinetic parameters of high, medium and low doses are as follows (0.21 ± 0.036) L, CL = (0.19 ± 0.019) Lh-1; t1 / 2 = 0.79 ± 0.12 h, AUC = 1.30 ± 0.13 mg.h.mL- = 1.52 ± 0.14 h, AUC = 1.22 ± 0.20 mg.h.mL-1, Vc = 0.36 ± 0.04 L, CL = 0.16 ± 0.030 Lh-1; t1 / 2 = h, AUC = (0.22 ± 0.004) mg.h.mL-1, Vc = (0.33 ± 0.027) L, CL = (0.66 ± 0.014) Lh-1. Saliva concentration of baicalin after high-dose administration ranged from 0.11 to 0.78μg.mL-1. No baicalin was detected in the saliva samples after medium-dose and low-dose administration. CONCLUSIONS: AUC increased disproportionally with high, medium and low doses and the corresponding AUC, indicating that baicalin was abolished by nonlinear pharmacokinetics after Shuanghuanglian injection. In addition, the distribution of baicalin to saliva concentration is much lower than the blood.