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炮制对口服何首乌典型成分药代动力学的影响。

Influence of processing on pharmacokinetic of typical constituents in radix polygoni multiflori after oral administration by LC-ESI-MS/MS.

机构信息

Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China.

出版信息

J Ethnopharmacol. 2013 Jun 21;148(1):246-53. doi: 10.1016/j.jep.2013.04.020. Epub 2013 Apr 19.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

The processed radix polygoni multiflori (P-RPM) are produced from the raw radix polygoni multiflori (R-RPM) steamed with black bean juice, but the two traditional Chinese medicines are used to treat the different diseases in clinic. In order to clarify the influence of processing on pharmacological properties of radix polygoni multiflori, an investigation was carried out to compare the pharmacokinetics of typical constituents after oral administration of P-RPM and R-RPM extracts

MATERIALS AND METHODS

A simple, rapid and sensitive high performance liquid chromatography-tandem mass spectroscopy (LC-MS/MS) was developed and validated for the simultaneous determination of gallic acid, polydatin, 2,3,5,4'-tetrahydroxystilbene-2-O-β-d-glucoside (PM-SG), resveratrol, and emodin in rat plasma. Male Sprague-Dawley rats were orally administered the two extracts with approximately the same dosage.

RESULTS

It was found that gallic acid was distributed as opened one-compartment model while polydatin, PM-SG and emodin were fitted to an open two-compartment model after oral administration of raw and processed radix polygoni multiflori extract. Cmax and AUC of gallic acid were increased (P<0.01), but Cmax and AUC of PM-SG were descreased (P<0.05). AUC of polydatin and emodin were similar with that of PM-SG. However, resveratrol was not detected in plasma collected at certain intervals following oral administration of the two extracts.

CONCLUSIONS

These results indicate that influence of the processing could improve the bioavailability of gallic acid and reduce the absorption of PM-SG, polydatin and emodin in rats. The LC-MS/MS method could be used to evaluate the effect of processing on pharmacokinetic of typical constituents in radix polygoni multiflori after oral administration.

摘要

民族药理学相关性

制首乌(P-RPM)是由生首乌(R-RPM)用黑豆汁蒸制而成的,但这两种中药在临床上用于治疗不同的疾病。为了阐明炮制对何首乌药理性质的影响,本研究考察了口服 P-RPM 和 R-RPM 提取物后典型成分的药代动力学差异。

材料与方法

建立并验证了一种简单、快速、灵敏的高效液相色谱-串联质谱(LC-MS/MS)法,用于同时测定大鼠血浆中没食子酸、虎杖苷、2,3,5,4'-四羟基二苯乙烯-2-O-β-D-葡萄糖苷(PM-SG)、白藜芦醇和大黄素的含量。雄性 Sprague-Dawley 大鼠口服给予两种提取物,剂量大致相同。

结果

发现口服生、制何首乌提取物后,没食子酸呈开放一室模型分布,而虎杖苷、PM-SG 和大黄素符合开放二室模型。(P<0.01),但 PM-SG 的 Cmax 和 AUC 降低(P<0.05)。与 PM-SG 相比,虎杖苷和大黄素的 AUC 相似。然而,口服两种提取物后,在某些时间点采集的血浆中未检测到白藜芦醇。

结论

这些结果表明,炮制可以提高没食子酸的生物利用度,降低大鼠对 PM-SG、虎杖苷和大黄素的吸收。LC-MS/MS 法可用于评价炮制对大鼠口服何首乌典型成分药代动力学的影响。

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