[红花中羟基红花黄色素A及其复方制剂在大鼠体内的药代动力学研究]

[Studies on pharmacokinetics of hydroxysafflor yellow A in Carthamus tinctorius and its compound preparation in rat].

作者信息

Tang Jianming, Ouyang Zhen, Feng Xu, Fang Jing, Cao Xu

机构信息

College of Pharmaceutical, Jiangsu University, Zhenjiang 212013, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2011 Aug;36(16):2246-9.

PMID:22097340

Abstract

OBJECTIVE

To develop a RP-HPLC method for the determination of the concentration of hydroxysafflor yellow A in rat plasma, to study the pharmacokinetics of Carthamus tinctorius extration and Naodesheng tablet, and to investigate the effect of other components on the pharmacokinetics of hydroxysafflor yellow A.

METHOD

The rats were orally treated with Carthamus tinctorius extration and Naodesheng capsule respectively. Blood samples were collected in heparinized eppendorf tube via the oculi chorioideae vein. Plasma was separated by centrifugation at 10 000 r x min(-1) for 10 min, and two-times methanol in volume was added to deposit proteins. After centrifugation, the upper liquid was transferred to filter. The concentration of hydroxysafflor yellow A in serum was determined by RP-HPLC. The stationary phase was C18, and methanol-acetonitrile-0.7% orthophosphoric acid (26: 2:72) was taken as the mobile phase, A UV detector was used at 403 nm. The pharmacokinetic parameters were calculated with 3p97 program.

RESULT

A good linear relationship of hydroxysafflor yellow A was obtained in the range of 0.03 and 2.56 mg x L(-1), the lowest limit of determination was 10 microg x L(-1), and the lowest limit of quantitation was 30 microg x L(-1). The mean recoveries were (99.3 +/- 1.4)%, (92.8 +/- 1.8)%, (98.4 +/- 2.0)% for high, middle, low concentrations of the samples respectively. The plasma concentration-time curves of hydroxysafflor yellow A were fitted with two-compartments model. The AUC)0-t), AUC(0-infinity), C(max) and T(max) of hydroxysafflor yellow A were increased in the Naodesheng group, compared with 50 mg x kg(-1) C. tinctorius extract group.

CONCLUSION

The HPLC method was selective, accurate and sensitive. The results indicated that the other herbs improved the absorption of hydroxysafflor yellow A and increased the bioavailability of hydroxysafflor yellow A significantly.

摘要

目的

建立大鼠血浆中羟基红花黄色素A浓度的反相高效液相色谱测定方法，研究红花提取物及脑得生片的药代动力学，考察其他成分对羟基红花黄色素A药代动力学特征的影响。

方法

大鼠分别灌胃给予红花提取物及脑得生胶囊。经脉络丛静脉取血，置于肝素化的离心管中。以10000r×min⁻¹离心10min分离血浆，加入2倍体积的甲醇沉淀蛋白。离心后，将上层清液转移至滤器。采用反相高效液相色谱法测定血清中羟基红花黄色素A的浓度。固定相为C18，流动相为甲醇-乙腈-0.7%正磷酸（26∶2∶72），采用紫外检测器，检测波长为403nm。用3p97程序计算药代动力学参数。

结果

羟基红花黄色素A在0.03～2.56mg×L⁻¹范围内线性关系良好，最低检测限为10μg×L⁻¹，最低定量限为30μg×L⁻¹。高、中、低浓度样品的平均回收率分别为（99.3±1.4）%、（92.8±1.8）%、（98.4±2.0）%。羟基红花黄色素A的血浆浓度-时间曲线符合二室模型。与50mg×kg⁻¹红花提取物组比较，脑得生组羟基红花黄色素A的AUC(0-t)、AUC(0-∞)、C(max)和T(max)均升高。