Pharmacokinetic And Serum Pharmacochemistry Studies Of Huanglian Shang Qing Pills

Huang lian Shang Qing pills(HLSQP) which been incorporated in the 2010 edition of Chinese Pharmacopoeia is a widely used compound Chinese medicine for the treatment of clearing heat and relieving pain for five hundred years. It is composed of seventeen kinds of herbs, such as Rheum palmatum L, Coptidis rhizome,Scutellaria baicalensis, Cortex Phellodendri Chinensis and so on. However, the action mechanism and process and effective constituents of HLSQP in vivo is not clear and there were no any reports about the pharmacokinetic and serum pharmacochemistry studies of HLSQP. In order to control its quality and clarify pharmacodynamic material basis, a High Performance Liquid Chromatography( HPLC) method was created to simultaneously determinate the content of aloe-emodin and emodin in HLSQP and this is the first report for the study of pharmacokinetic and serum pharmacochemistry of HLSQP.1. A HPLC method was developed to determinate the content of aloe-emodin and emodin in HLSQP from different factories. Chromatographic separation was performed on an Inertsil®ODS-3 column(150mm×4.6mm, 5um) with a mobile phase consisting of methanol-0.2% phosphoric acid(65:35 v/v) at a ?ow rate of 1.0ml/min.Detection wavelength of analyte was set at 254 nm. The temperature of the analytical column was maintained at 25℃. The injection volume was 10 μl. The method was validated in terms of speci?city, precision, linearity and stability. Under this condition,aloe emodin in 14-41.40μg/ml(r=0.9999)and rhein in 6.49-29.70μg/ml(r=0.9998)exhibited good linearity of the calibration graphs. The results showed that content of aloe-emodin and emodin in HLSQP from partly different factories with different batch numbers was obvious different.2. A HPLC method with diode array detection was developed and validated to determinate rhein in rat plasma and its application to a pharmacokinetic study of HLSQP was investigated for the first time in this paper. Chromatographic separation was performed on an Inertsil®ODS-3 column(150mm×4.6mm, 5um) with a mobile phase consisting of methanol-0.2% phosphoric acid(80:20 v/v) at a ?ow rate of1.0ml/min. 1, 8- Dihydroxy anthraquinone was used as an internal standard.Detection wavelength of analyte was set at 254 nm. The temperature of the analytical column was maintained at 25℃. The injection volume was 10 μl. The method was validated in terms of speci?city, intra- and inter-day precision(<14.7%), accuracy,linearity(r=0.9981), extraction recovery(86.5%-106.3%) and stability.Pharmacokinetic results exhibited that rhein fit opened two-compartment model in rats and the Tmax was 0.222 h, Cmax was 0.219μg/ml.3. A liquid chromatography tandem quadrupole time-of-?ightmass spectrometry(LC-Q-TOF/MS)method was established to study serum pharmacochemistry of HLSQP for the first time in this paper. 46 components were observed in extract of HLSQP and 27 components were identified. In vivo, 15 components and 21 metabolites of HLSQP were observed in plasma, 10 components and 8 metabolites were identified. Serum pharmacochemistry results indicated that berberine, rhein,baicalin, emodin and some other components were absorbed in prototype.