Zhang Yifan, Yuan Jin, Wang Ying, Wang Yue, An Rui, Wang Xinhong
Department of Chemistry, School of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, China ; Department of Pharmacy, Institute of Health Science, Shanghai - 201 318, China.
Department of Chemistry, School of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, China.
Pharmacogn Mag. 2014 Jul;10(39):241-8. doi: 10.4103/0973-1296.137363.
Gegenqinlian decoction (GQD) is a famous traditional medicine recipe. It is composed of four herbs including Radix Puerariae (GG), Radix Scutellariae (HQ), Rhizoma Coptidis (HL) and Radix Glycyrrhizae (GC), which is widely used for treating gastro-intestinal disorders in the clinical practice of Traditional Chinese medicine (TCM). The aim of this study was to compare the pharmacokinetics of puerarin and daidzein in rats following oral administration of Gegenqinlian Decoction and Radix Puerariae extract. Thus, a sensitive and selective liquid chromatography/tandem mass spectrometry (LC-MS/MS) method was developed and validated for simultaneous determination of puerarin and daidzein in rat plasma following oral administration of Gegenqinlian Decoction and Radix Puerariae extract.
Chromatographic separation was performed on a Shiseido CAPCELL PAK C18 analytical column (100 mm × 2.0 mm i.d., 5 μm) by linear gradient elution, with water (0.1% formic acid)-acetonitrile (0.1% formic acid) as mobile phase. Detection was carried out by multiple reaction monitoring (MRM) mode using electrospray ionization in the positive ion mode.
The calibration curves were linear over a range of 7.80-1560 ng/mL for puerarin and 6.30-1260 ng/mL for daidzein. The intra- and inter-day precision values were less than 13.6% and their average recoveries was in the range of 77.8% and 88.6% for puerarin and was between 76.3 and 86.8% for daidzein, respectively.
The validated method was applied to the comparative pharmacokinetic studies of puerarin and daidzein after oral administration of Gegenqinlian Decoction and Radix Puerariae extract. The pharmacokinetic parameters showed that puerarin and daidzein from Gegenqinlian Decoction were absorbed more effectively with slower elimination in rat plasma than that from Radix Puerariae extract. These results revealed that as far as the Radix Puerariae extract was concerned, it is very valuable to be used as a clinical directions of Gegenqinlian Decoction.
葛根芩连汤（GQD）是一种著名的传统中药方剂。它由葛根（GG）、黄芩（HQ）、黄连（HL）和甘草（GC）四味草药组成，在中医临床实践中广泛用于治疗胃肠道疾病。本研究的目的是比较葛根芩连汤和葛根提取物口服给药后大鼠体内葛根素和大豆苷元的药代动力学。因此，建立并验证了一种灵敏、选择性的液相色谱/串联质谱（LC-MS/MS）方法，用于同时测定口服葛根芩连汤和葛根提取物后大鼠血浆中葛根素和大豆苷元的含量。
采用岛津CAPCELL PAK C18分析柱（100 mm×2.0 mm内径，5μm）进行色谱分离，以水（0.1%甲酸）-乙腈（0.1%甲酸）为流动相进行线性梯度洗脱。采用电喷雾电离正离子模式下的多反应监测（MRM）模式进行检测。
葛根素的校准曲线在7.80-1560 ng/mL范围内呈线性，大豆苷元的校准曲线在6.30-1260 ng/mL范围内呈线性。日内和日间精密度值均小于13.6%，葛根素的平均回收率在77.8%至88.6%之间，大豆苷元的平均回收率在76.3%至86.8%之间。
该验证方法应用于葛根芩连汤和葛根提取物口服给药后葛根素和大豆苷元的比较药代动力学研究。药代动力学参数表明，与葛根提取物相比，葛根芩连汤中的葛根素和大豆苷元在大鼠血浆中吸收更有效，消除更慢。这些结果表明，就葛根提取物而言，作为葛根芩连汤的临床指导用药具有很高的价值。
