[青藤碱在比格犬体内的药代动力学及绝对生物利用度研究]

[Study on pharmacokinetics and absolute bioavailability of sinomenine in beagle dogs].

作者信息

Chen Wanyi, Zhou Yuanda, Kang Jiping, Li Qiubo, Feng Xiaoke

机构信息

Department of Clinical Pharmacology, First Affiliated Hospital of Chongqing University of Medical Sciences, Chongqing 400016, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2009 Feb;34(4):468-71.

PMID:19459314

Abstract

OBJECTIVE

To study pharmacokinetic parameters and absolute bioavailability for oral use of sinomenine tablet in beagle dogs.

METHOD

Applying to double cycle self crossover design, a single oral or intravenous dose of 10 mg x kg(-1) sinomenine was given to 10 beagle dogs. Drug concentrations in plasma were determined by HPLC. The pharmacokinetic parameters were calculated by 3P97 pharmacokinetic program.

RESULT

The concentration-time curves of oral administration fitted to one compartment model in the beagle dogs. The T(max), C(max), t1/2 and AUC(0-T) was (82.5 +/- 13.9) min, (0.15 +/- 0.027) mg x L(-1), (87.6 +/- 28.3) min and (28.43 +/- 3.48) mg x min x L(-1), respectively. The concentration -time curves of i.v. fitted to two compartment model in the beagle dogs. The t1/2beta and AUC(0-T) was (106.7 +/- 120.2) min and (93.32 +/- 82.08) mg x min x L(-1). The absolute bioavailability for oral use was (30.46 +/- 4.24)%.

CONCLUSION

The absolute bioavailability of sinomenine is low, and the elimination of sinomenine tablet is fast.

摘要

目的

研究青藤碱片在比格犬体内的药代动力学参数及绝对生物利用度。

方法

采用双周期自身交叉设计，对10只比格犬单次口服或静脉注射10mg·kg⁻¹青藤碱。用高效液相色谱法测定血浆中药物浓度，通过3P97药代动力学程序计算药代动力学参数。

结果

比格犬口服给药的浓度-时间曲线符合一室模型。T(max)、C(max)、t1/2和AUC(0-T)分别为(82.5±13.9)min、(0.15±0.027)mg·L⁻¹、(87.6±28.3)min和(28.43±3.48)mg·min·L⁻¹。静脉注射的浓度-时间曲线符合二室模型。t1/2β和AUC(0-T)分别为(106.7±120.2)min和(93.32±82.08)mg·min·L⁻¹。口服绝对生物利用度为(30.46±4.24)%。