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蒲黄-五灵脂药对配伍前后大鼠口服给药后三种主要生物活性成分的比较药代动力学

Comparative Pharmacokinetics of three major bioactive components in rats after oral administration of Typhae Pollen-Trogopterus Feces drug pair before and after compatibility.

作者信息

Zeng Huiting, Xue Ping, Su Shulan, Huang Xiaochen, Shang Erxin, Guo Jianming, Qian Dawei, Tang Yuping, Duan Jin-ao

机构信息

Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing, 210023, China.

Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Nanjing University of Chinese Medicine, Nanjing, 210023, China.

出版信息

Daru. 2016 Jan 20;24:2. doi: 10.1186/s40199-016-0140-2.

Abstract

BACKGROUND

Typhae Pollen (TP) and Trogopterus Feces (TF) are well-known traditional medicine in china which widely used for thousands of years as drug pair called Shixiao San for treatment of blood stasis syndrome, specially shown great efficacy in gynecological disease. Typhaneoside, vanillic acid and p-coumaric acid are the main bioactive components of Typhae Pollen. This study was carried out for comparing the pharmacokinetic profile of these three major bioactive components in rats after oral administration of Typhae Pollen-Trogopterus Feces (TP-TF) drug pair before and after compatibility.

METHODS

A sensitive and rapid UPLC-TQ/MS method has been developed for simultaneous quantification of the three main bioactive compounds in blood at different time points after oral administration of Typhae Pollen (TP) and the combination with Trogopterus Feces (TF).

RESULTS

There were significant differences of C(max), T(max), T(1/2) and AUC(0~t) for three bioactive compounds among the groups, for typhaneoside with the most highest plasma concentration of 370.86 ± 315.71 ng/mL and more longer T(max) in TP-TF co-decoction group (C(M)); for vanillic acid, TP-TF co-decoction group (C(M)) had a good absorption with C(max) (3870.99 ± 2527.99 ng/mL) and T(max) (1.47 ± 3.20 h); for p-coumaric acid, it had similar pharmacokinetic characteristics with vanillic acid.

CONCLUSIONS

The three bioactive components in Typhae Pollen (TP) were simultaneously determined by UPLC-TQ/MS and had a good absorption in rat plasma after the combination with Trogopterus Feces (TF).

摘要

背景

蒲黄(TP)和五灵脂(TF)是中国著名的传统药物,作为名为失笑散的药对已被广泛使用了数千年,用于治疗血瘀证,尤其在妇科疾病中显示出显著疗效。香蒲新苷、香草酸和对香豆酸是蒲黄的主要生物活性成分。本研究旨在比较大鼠口服蒲黄-五灵脂(TP-TF)药对配伍前后这三种主要生物活性成分的药代动力学特征。

方法

建立了一种灵敏、快速的超高效液相色谱-串联四极杆质谱(UPLC-TQ/MS)方法,用于同时定量口服蒲黄(TP)及其与五灵脂(TF)配伍后不同时间点血液中三种主要生物活性化合物的含量。

结果

各给药组三种生物活性化合物的C(max)、T(max)、T(1/2)和AUC(0~t)存在显著差异,蒲黄-五灵脂合煎组(C(M))中香蒲新苷的血浆浓度最高,为370.86±315.71 ng/mL,T(max)更长;对于香草酸,蒲黄-五灵脂合煎组(C(M))吸收良好,C(max)为3870.99±2527.99 ng/mL,T(max)为1.47±3.20 h;对于对香豆酸,其药代动力学特征与香草酸相似。

结论

采用UPLC-TQ/MS同时测定了蒲黄(TP)中的三种生物活性成分,其与五灵脂(TF)配伍后在大鼠血浆中具有良好的吸收。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/500f/4719211/13eba61dd09b/40199_2016_140_Fig1_HTML.jpg

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