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[马钱子炮制后种子生物碱在大鼠体内的药代动力学]

[Pharmacokinetics of the alkaloids from the processed seeds of Strychnos nux-vomica in rats].

作者信息

Xu Xiao-yue, Cai Bao-chang, Pan Yang, Wang Tian-shan

机构信息

Institute for Drug Control of Henan Province, Zhengzhou 450003, China.

出版信息

Yao Xue Xue Bao. 2003 Jun;38(6):458-61.

PMID:14513809
Abstract

AIM

To study the pharmacokinetic process about the concentration in rat plasma of the alkaloids from processed seeds of Strychnos nux-vomica with RP-HPLC method.

METHODS

Hypersil BDS C18 column was used and the mobile phase consisted of acetonitrile-water at the flow rate of 0.8 mL.min-1. The UV detection wave length was 254 nm.

RESULTS

The concentration-time data of strychnine, brucine, strychnine N-oxide and brucine N-oxide were all in accordance with an open two-compartment model after i.v. alkaloids. Their parameters were as follows: T1/2 alpha were (8 +/- 5), (4 +/- 3), (6.2 +/- 1.7) and (3.0 +/- 0.8) min, T1/2 beta were (262 +/- 125), (416 +/- 131), (285 +/- 50) and (342 +/- 141) min, CL were (17 +/- 4), (21 +/- 12), (1.9 +/- 1.8) and (2.8 +/- 1.1) mL.min-1, Vc were (1.4 +/- 0.5), (1.7 +/- 1.1), (0.24 +/- 0.16) and (0.23 +/- 0.06) L.kg-1, Vd were (6.0 +/- 1.2), (12 +/- 7), (0.8 +/- 0.6) and (1.5 +/- 0.6) L.kg-1, AUC were (57,578 +/- 25,578), (35,240 +/- 15,616), (93,088 +/- 22,375) and (177,712 +/- 120,110) h.microgram.L-1, respectively.

CONCLUSION

The method is a good reference for pharmacokinetics in human bodies.

摘要

目的

采用反相高效液相色谱法研究马钱子炮制后种子生物碱在大鼠血浆中的药代动力学过程。

方法

采用Hypersil BDS C18柱,流动相为乙腈-水,流速为0.8 mL·min-1,紫外检测波长为254 nm。

结果

静脉注射生物碱后,士的宁、马钱子碱、士的宁氮氧化物和马钱子碱氮氧化物的浓度-时间数据均符合开放二室模型。其参数如下:T1/2α分别为(8±5)、(4±3)、(6.2±1.7)和(3.0±0.8)分钟,T1/2β分别为(262±125)、(416±131)、(285±50)和(342±141)分钟,CL分别为(17±4)、(21±12)、(1.9±1.8)和(2.8±1.1) mL·min-1,Vc分别为(1.4±0.5)、(1.7±1.1)、(0.24±0.16)和(0.23±0.06) L·kg-1,Vd分别为(6.0±1.2)、(12±7)、(0.8±0.6)和(1.5±0.6) L·kg-1,AUC分别为(57,578±25,578)、(35,240±15,616)、(93,088±22,375)和(177,712±120,110) h·μg·L-1。

结论

该方法为人体药代动力学研究提供了良好的参考。

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