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生白术与炮制白术口服后苍术素的测定及药代动力学比较

Determination and Pharmacokinetic Comparisons of Atractylodin after Oral Administration of Crude and Processed Atractylodis rhizoma.

作者信息

Xiao-Wen Chang, Chen-Xi Xu, Yu-Qiang Liu, Cai Qian

机构信息

Department of Medicine, Liaoning University of Traditional Chinese Medicine, Dalian 116600, China.

出版信息

Pharmacogn Mag. 2016 Jan-Mar;12(45):80-3. doi: 10.4103/0973-1296.176062.

Abstract

BACKGROUND

In traditional Chinese medicine, Atractylodis rhizoma is the dried rhizome of Atractylodes lancea (Thunb.) DC. or Atractylodes chinensis (DC.) Koidz. After being processed, the dryness of A. rhizoma decreased, and the function of tonifying spleen increased. Therefore, the processed A. rhizoma is the best choice of clinical application. As the main active components, polyethylene alkynes exhibits various desirable pharmacological effects including anti-inflammatory, anti-bacterial and anti-arrhythmia activity. However, there is no report on the pharmacokinetic comparisons of atractylodin, one of polyethylene alkynes, in bio-samples after oral administration of crude and processed A. rhizoma until now. The in vivo study of active components of A. rhizoma would be necessary and helpful for clinical application and clarification of processing principle.

OBJECTIVE

To compare the pharmacokinetic parameters of atractylodin after oral administration of crude and processed A. rhizoma, and clarify the processing principle of A. rhizoma.

MATERIALS AND METHODS

Plasma concentrations of atractylodin in rats were determined by reversed-phase high-performance liquid chromatogram and the main pharmacokinetic parameters were estimated with Drug and Statistics 2.0 Software Package (Chinese Pharmacological Society, Shanghai, China).

RESULTS

The AUC0-t, AUC0→∞, Tmax, and Cmax of processed A. rhizoma were increased significantly (P < 0.05) compared with that in crude A. rhizoma after using Student's t-test.

CONCLUSIONS

Processing A. rhizoma with wheat bran by stir-frying can promote and accelerate the absorption of atractylodin.

SUMMARY

In this paper, a RP-HPLC method with UV detection for quantification of atractylodin (a main active component in Atractylodis Rhizoma) in rat plasma has been developed and applied to a preliminary pharmacokinetic study of atractylodin after oral administration of crude and processed Atractylodis Rhizoma respectively. The result indicates that processing Atractylodis Rhizoma with wheat-bran can promote and accelerate the absorption of atractylodin.

摘要

背景

在传统中医中,白术是茅苍术或北苍术的干燥根茎。炮制后,白术的燥性降低,补脾功能增强。因此,炮制后的白术是临床应用的最佳选择。聚乙炔类化合物作为其主要活性成分,具有多种理想的药理作用,包括抗炎、抗菌和抗心律失常活性。然而,截至目前,尚无关于口服生白术和炮制白术后生物样品中聚乙炔类化合物之一苍术素的药代动力学比较的报道。白术活性成分的体内研究对于临床应用和炮制原理的阐明是必要且有帮助的。

目的

比较口服生白术和炮制白术后苍术素的药代动力学参数,阐明白术的炮制原理。

材料与方法

采用反相高效液相色谱法测定大鼠血浆中苍术素的浓度,并使用药物统计学2.0软件包(中国药理学会,上海,中国)估算主要药代动力学参数。

结果

经学生t检验,炮制白术的AUC0-t、AUC0→∞、Tmax和Cmax与生白术相比显著增加(P < 0.05)。

结论

用麸皮炒白术可促进和加速苍术素的吸收。

总结

本文建立了一种采用紫外检测的反相高效液相色谱法用于定量大鼠血浆中苍术素(白术的主要活性成分),并分别应用于口服生白术和炮制白术后苍术素的初步药代动力学研究。结果表明,用麸皮炮制白术可促进和加速苍术素的吸收。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e352/4787342/bcf0e8d20bdd/PM-12-80-g001.jpg

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