灯盏花素单次静脉注射后在犬和兔体内的药代动力学

[Pharmacokinetics of breviscapine in dogs and rabbits following single intravenous administration].

作者信息

Liu Qingfei, Luo Guoan, Wang Yiming, Ma Yuhui, Zhang Rongli

机构信息

Institute of Material Medica, Tsinghua University, Beijing 100084.

出版信息

Zhong Yao Cai. 2005 Oct;28(10):913-6.

PMID:16479930

Abstract

OBJECTIVE

To study pharmacokinetics of breviscapine in dogs and rabbits after iv. single dose.

METHODS

Lc/Lc extract was used to prepare test samples and HPLC was used to determine breviscapine.

RESULTS

Breviscaplin was fitted to double-department model in dogs and rabbits after iv. single dose. The main parameters in dogs were: A = 56.93 +/- 23.14, B = 1.61 +/- 1.11, alpha = 0.2328 +/- 0.1321 min, beta = 0.0255 +/- 0.0187 min(-1), t(1/2alpha) = 2.98 +/- 1.42 min, t(1/2beta) = 27.14 +/- 14.35 min, K21 = 0.10312 +/- 0.0112 min(-1), K10 = 0.1904 +/- 0.1319 min(-1), K12 = 0.0367 +/- 0.0306 min(-1), CL = 39.41 +/- 20.44 ml x min(-1), AUC = 3074 +/- 1055 mg x min x L(-1), respectively. The main parameters in rabbits were:A = 2.64 +/- 1.12, B = 0.28 +/- 0.12, alpha = 0.1439 +/- 0.0681 min(-1), beta = 0.0162 +/- 0.0456 min(-1), t1/2alpha = 4.82 +/- 1.65 min, th1/2beta = 42.66 +/- 18.77 min, K21 = 0.0285 +/- 0.0147 min(-1), K10 = 0.0820 +/- 0.00378 min(-1), K12 = 0.0496 +/- 0.0241 min, CL = 337.05 +/- 156.48ml x min(-1), AUC = 356 +/- 114 mg x min x L(-1), respectively.

CONCLUSION

Breviscapine has short half-life after intravenous administration to dogs and rabbits,which show breviscapine is eliminated rapidly and has short action time.

摘要

目的

研究灯盏花素静脉注射单剂量后在犬和兔体内的药代动力学。

方法

采用Lc/Lc提取物制备供试品溶液，用高效液相色谱法测定灯盏花素含量。

结果

灯盏花素静脉注射单剂量后在犬和兔体内符合二室模型。犬的主要药代动力学参数为：A = 56.93±23.14，B = 1.61±1.11，α = 0.2328±0.1321 min，β = 0.0255±0.0187 min⁻¹，t₁/₂α = 2.98±1.42 min，t₁/₂β = 27.14±14.35 min，K₂₁ = 0.10312±0.0112 min⁻¹，K₁₀ = 0.1904±0.1319 min⁻¹，K₁₂ = 0.0367±0.0306 min⁻¹，CL = 39.41±20.44 ml·min⁻¹，AUC = 3074±1055 mg·min·L⁻¹。兔的主要药代动力学参数为：A = 2.64±1.12，B = 0.28±0.12，α = 0.1439±0.0681 min⁻¹，β = 0.0162±0.0456 min⁻¹，t₁/₂α = 4.82±1.65 min，t₁/₂β = 42.66±18.77 min，K₂₁ = 0.0285±0.0147 min⁻¹，K₁₀ = 0.0820±0.00378 min⁻¹，K₁₂ = 0.0496±0.0241 min，CL = 337.05±156.48 ml·min⁻¹，AUC = 356±114 mg·min·L⁻¹。