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黄连解毒汤对2型糖尿病大鼠和正常大鼠灌胃给药后黄芩苷和汉黄芩苷的比较药代动力学研究

Comparative pharmacokinetic investigation on baicalin and wogonoside in type 2 diabetic and normal rats after oral administration of traditional Chinese medicine Huanglian Jiedu decoction.

作者信息

He Meng-Yun, Deng Yuan-Xiong, Shi Qun-Zhi, Zhang Xiao-Jie, Lv Yuan

机构信息

Department of Pharmaceutical Science, Medical College of Hunan Normal University, Changsha 410013, PR China.

Department of Pharmaceutical Science, Medical College of Hunan Normal University, Changsha 410013, PR China.

出版信息

J Ethnopharmacol. 2014 Aug 8;155(1):334-42. doi: 10.1016/j.jep.2014.05.033. Epub 2014 Jun 5.

DOI:10.1016/j.jep.2014.05.033
PMID:24910405
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Huanglian Jiedu decoction (HLJDD) is used traditionally in China for the treatment of diabetes mellitus in clinical practice, which has been proved to be effective. The purpose of this study was to investigate the pharmacokinetic characteristics (especially the area under the curve, AUC) of baicalin and wogonoside in type 2 diabetic rats after oral administration of HLJDD extract and to explore its possible mechanism.

MATERIALS AND METHODS

HLJDD extract and Radix scutellariae extract were prepared and the contents of baicalin and wogonoside contained in two extracts were assayed with high performance liquid chromatography (HPLC). Type 2 diabetic rats were induced by high fat diet and intraperitoneal injection of streptozotocin. Pharmacokinetics of baicalin and wogonoside in type 2 diabetic and normal control rats after oral administration of HLJDD extract or Radix scutellariae extract were investigated. Pharmacokinetics of baicalin in type 2 diabetic and normal rats after oral administration of pure baicalin was also investigated.

RESULTS

The pharmacokinetic parameters (especially AUCs) of baicalin and wogonoside in type 2 diabetic rats after oral administration of HLJDD extract were remarkably different from those in normal rats. And the alterations of the AUCs of baicalin and wogonoside in type 2 diabetic rats after oral administration of Radix scutellariae extract were similar to those after oral administration of HLJDD extract. Moreover, the increase of the AUC of baicalin in type 2 diabetic rats after oral administration of pure baicalin was similar to that after oral administration of HLJDD extract or Radix scutellariae extract.

CONCLUSION

The pharmacokinetic behaviors of baicalin and wogonoside (especially the systemic exposure [AUCs] of baicalin and wogonoside) were significantly altered in type 2 diabetic rats after orally administrated HLJDD extract. And the increased AUCs of baicalin and wogonoside in type 2 diabetic rats after oral administration of HLJDD extract resulted from neither the effects of other herbs contained in HLJDD nor the effects of other components contained in Radix scutellariae. It might result from the effects of the pathological status of type 2 diabetes mellitus.

摘要

民族药理学相关性

黄连解毒汤(HLJDD)在中国传统临床实践中用于治疗糖尿病,已被证明是有效的。本研究的目的是研究2型糖尿病大鼠口服HLJDD提取物后黄芩苷和汉黄芩苷的药代动力学特征(尤其是曲线下面积,AUC),并探讨其可能的机制。

材料与方法

制备HLJDD提取物和黄芩提取物,采用高效液相色谱法(HPLC)测定两种提取物中黄芩苷和汉黄芩苷的含量。通过高脂饮食和腹腔注射链脲佐菌素诱导2型糖尿病大鼠。研究2型糖尿病大鼠和正常对照大鼠口服HLJDD提取物或黄芩提取物后黄芩苷和汉黄芩苷的药代动力学。还研究了2型糖尿病大鼠和正常大鼠口服纯黄芩苷后的药代动力学。

结果

2型糖尿病大鼠口服HLJDD提取物后黄芩苷和汉黄芩苷的药代动力学参数(尤其是AUC)与正常大鼠有显著差异。2型糖尿病大鼠口服黄芩提取物后黄芩苷和汉黄芩苷AUC的变化与口服HLJDD提取物后的变化相似。此外,2型糖尿病大鼠口服纯黄芩苷后黄芩苷AUC的增加与口服HLJDD提取物或黄芩提取物后的增加相似。

结论

2型糖尿病大鼠口服HLJDD提取物后,黄芩苷和汉黄芩苷的药代动力学行为(尤其是黄芩苷和汉黄芩苷的全身暴露量[AUC])发生了显著改变。2型糖尿病大鼠口服HLJDD提取物后黄芩苷和汉黄芩苷AUC的增加既不是由于HLJDD中其他草药的作用,也不是由于黄芩中其他成分的作用。这可能是由于2型糖尿病的病理状态所致。

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