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[醒脑静滴鼻剂滴鼻给药家兔栀子苷的药代动力学研究]

[Study on pharmacokinetics of jasminoidin in rabbits administered xingnaojing naristillae by nasal medication].

作者信息

Yao Zongling, Lu Yang, Du Shouying, Chen Xiaolan, Wang Yue

机构信息

School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2010 Jul;35(14):1871-3. doi: 10.4268/cjcmm20101423.

DOI:10.4268/cjcmm20101423
PMID:20939288
Abstract

OBJECTIVE

To develop an HPLC method for the determination of plasma concentration of jasminoidin and study the pharmacokinetics of jasminoidin in rabbits administered Xingnaojing naristillae by nasal medication.

METHOD

After sampling blood from the left arteria carotis of rabbits which were administered Xingnaojing naristillae medication by nasal by 12 mg x kg(-1) (counted by gardenia extract) at 1, 3, 5, 10, 20, 30, 45, 60, 90, 120, 240 min, the plasma samples were dealt with acetonitrile precipitation and HPLC was used to determine the plasma concentration of jasminoidin. The pharmacokinetic parameters were computed by Kinetica software.

RESULT

The calibration curve was linear (r = 0.999 6) within the range of 0.136 5-2.73 mg x L(-1) for jasminoidin in plasma. The average recovery was (97.14 +/- 3.78)%, (95.06 +/- 2.95)%, (91.50 +/- 1.82)%. The within-day and between-day precision met the requirements, because the RSD were both less than 4%. Jasminoidin was fitted to a two-compartment open pharmacokinetic model in rabbits. The mainly pharmacokinetic parameters were: C(max) = (2.013 +/- 0.563) mg x L(-1), T(max) = (6.405 +/- 1.764) min, K(e) = (0.032 5 +/- 0.013 3) min(-1), CL = (0.059 3 +/- 0.0246) L x min(-1) x kg(-1), AUC = (116.89 +/- 50.19) mg x min(-1) x L(-1), MRT = (84.447 +/- 19.420) min.

CONCLUSION

The method can be used to determine the concentration and to investigate the pharmacokinetics of jasminoidin in rabbits. Jasminoidin was absorbed rapidly by nasal medication and has a good perspective.

摘要

目的

建立高效液相色谱法测定栀子苷血浆浓度,并研究醒脑静滴鼻剂滴鼻给药后栀子苷在兔体内的药代动力学。

方法

将醒脑静滴鼻剂按12 mg·kg⁻¹(以栀子提取物计)滴鼻给予兔,于给药后1、3、5、10、20、30、45、60、90、120、240 min从兔左耳动脉采血,血浆样品经乙腈沉淀处理后,采用高效液相色谱法测定血浆中栀子苷的浓度,药代动力学参数用Kinetica软件计算。

结果

血浆中栀子苷在0.136 5~2.73 mg·L⁻¹范围内线性关系良好(r = 0.999 6)。平均回收率分别为(97.14±3.78)%、(95.06±2.95)%、(91.50±1.82)%。日内和日间精密度均符合要求,相对标准偏差均小于4%。栀子苷在兔体内符合二室开放药代动力学模型。主要药代动力学参数为:C(max) =(2.013±0.563)mg·L⁻¹,T(max) =(6.405±1.764)min,K(e) =(0.032 5±0.013 3)min⁻¹,CL =(0.059 3±0.0246)L·min⁻¹·kg⁻¹,AUC =(116.89±50.19)mg·min⁻¹·L⁻¹,MRT =(84.447±19.420)min。

结论

该方法可用于测定兔体内栀子苷的浓度并研究其药代动力学。栀子苷滴鼻给药吸收迅速,具有良好的应用前景。

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