[高效液相色谱法测定胡芦巴碱及其药代动力学研究]

[Determination of trigonelline by HPLC and study on its pharmacokinetics].

作者信息

Zhao Huai-qing, Qu Yan, Wang Xue-ya, Lu Xin-yan, Zhang Xue-hang, Hattori Masao

机构信息

Pharmaceutical College, Shenyang Pharmaceutical University, Shenyang 110016, China.

出版信息

Yao Xue Xue Bao. 2003 Apr;38(4):279-82.

PMID:12889128

Abstract

AIM

To develop a sensitive and specific HPLC method for determination of trigonelline in rabbit plasma, and study the pharmacokinetics in rabbit.

METHODS

After ig of fenugreek extract and i.v. of trigonelline in rabbit, the biological samples could be well purified after precipitation of protein with methanol and acetonitrile. Asahipak NH2P-50 column was used, the mobile phase consisted of acetonitrile-water (90:10) at a flow-rate of 1.2 mL.min-1, and detection wavelength was set at UV 265 nm. The column temperature is 30 degrees C.

RESULTS

The calibration curve was linear in the range from 0.98 mg.L-1 to 31.28 mg.L-1, with r = 0.9986, the detection limit of this method was 50 micrograms.L-1. The concentration-time curves of trigonelline in rabbits after ig and i.v. administration were shown to fit one-compartment and two-compartment open model, respectively. The main parameters after ig of fenugreek extract were as follow: T1/2(Ka) was 0.9 h, T1/2(Ke) was 2.2 h, V was 0.64 L.kg-1, AUC was 1.93 mg.min.L-1. The main parameters after i.v. of trigonelline were as follows: T1/2 alpha was 10.8 min, T1/2 beta was 44.0 min, K21 was 0.044 min-1, K10 was 0.026 min-1, K12 was 0.017 min-1, AUC was 931.0 mg.min.L-1.

CONCLUSION

Trigonelline showed a middle rate of absorption and fast rate of elimination in rabbit. Meanwhile, the method is simple, accurate, with a good reproducibility, and it provide a basic method for the investigation of trigonelline and fenugreek pharmacokinetics.

摘要

目的

建立一种灵敏、特异的高效液相色谱法测定兔血浆中胡芦巴碱含量，并研究其在兔体内的药代动力学。

方法

给兔灌胃胡芦巴提取物及静脉注射胡芦巴碱后，用甲醇和乙腈沉淀蛋白可对生物样品进行良好纯化。采用Asahipak NH2P - 50柱，流动相为乙腈 - 水（90:10），流速为1.2 mL·min-1，检测波长设定为紫外265 nm。柱温为30℃。

结果

校准曲线在0.98 mg·L-1至31.28 mg·L-1范围内呈线性，r = 0.9986，该方法的检测限为50 μg·L-1。兔灌胃和静脉注射胡芦巴碱后，其浓度 - 时间曲线分别符合一室和二室开放模型。灌胃胡芦巴提取物后的主要参数如下：吸收半衰期（T1/2(Ka)）为0.9 h，消除半衰期（T1/2(Ke)）为2.2 h，分布容积（V）为0.64 L·kg-1，曲线下面积（AUC）为1.93 mg·min·L-1。静脉注射胡芦巴碱后的主要参数如下：分布相半衰期（T1/2α）为10.8 min，消除相半衰期（T1/2β）为44.0 min，转运速率常数（K21）为0.044 min-1，消除速率常数（K10）为0.026 min-1，转运速率常数（K12）为0.017 min-1，AUC为931.0 mg·min·L-1。