A simple, sensitive and accurate method based on high performance liquid chromato- graphy （HPLC） with diode array detector （DAD） was developed and validated for systematic quality evaluation of one type of traditi...A simple, sensitive and accurate method based on high performance liquid chromato- graphy （HPLC） with diode array detector （DAD） was developed and validated for systematic quality evaluation of one type of traditional Chinese medicine preparations named Xinkeshu （XKS） tablet. In this study, the chromatographic fingerprints of XKS tablet were developed first, 23 peaks were selected as the common peaks to evaluate the similarities among different batches of XKS samples, which were manufactured in a long time span of three years. Additionally, simultaneous quantification of six markers in XKS tablet, including Danshensu, Protocatechuic aldehyde, Puerarin, Daidzin, Salvianolic acid B and Daidzein, was performed. The validation results showed that the developed method was specific, accurate, precise and robust. The preliminary explanation on why a close similarity between fingerprints did not exactly mean similar contents of chemical components in samples was given. The contribution of each chromatographic peak to similarity was also evaluated. The developed method offers an efficient, reliable and practical approach for systematic quality evaluation of XKS tablet.展开更多
目的采用"Cocktail"探针药物法考察丹参注射液和心可舒片对家兔CYP酶5种亚型CYP1A2、CYP2C9、CYP2C19、CYP2D6和CYP3A4代谢的影响。方法将16只雄性家兔同时空腹给予混合探针药咖啡因、甲苯磺丁脲、奥美拉唑、右美沙芬和咪达唑...目的采用"Cocktail"探针药物法考察丹参注射液和心可舒片对家兔CYP酶5种亚型CYP1A2、CYP2C9、CYP2C19、CYP2D6和CYP3A4代谢的影响。方法将16只雄性家兔同时空腹给予混合探针药咖啡因、甲苯磺丁脲、奥美拉唑、右美沙芬和咪达唑仑,采用LC-MS/MS检测特定时间点的探针药物代谢率(代谢产物浓度与探针原型药物浓度的比值)。家兔随机分为丹参注射液组和心可舒片组,设计为自身对照实验,分3个周期,按顺序分别给药丹参低剂量组(0.5 m L·kg-1)、中剂量组(1 m L·kg-1)、高剂量组(2 m L·kg-1)和心可舒低剂量组(90 mg·kg-1)、中剂量组(180 mg·kg-1)和高剂量组(360 mg·kg-1)。每个周期经7 d洗净期后,连续给药7 d,第15天再给予探针药物后测代谢率。采用ANOVA方差分析比较各剂量组家兔和用药前探针药物的代谢率的变化。结果与用药前相比,各剂量组的混合探针药物代谢率均有下降趋势。结论丹参注射液、心可舒片使用7 d后可能抑制家兔体内CYP450酶代谢,与体外实验结果一致。这些药物与经过CYP450酶代谢的药物联合应用时,可能会引起药物相互作用,临床联合使用应提高警惕。展开更多
基金supported by the Major Projects of Independent Innovation Achievements of Shandong Province(No. 2010ZDZX1A0406)partly by the Scientific and Technological Projects of Shandong Province (No. 2009GG10002081)+1 种基金Independent Innovation Foundation of Shandong University(No. 2010TS054)Shandong Province Natural Science Foundation, China (No. ZR2011HM080)
文摘A simple, sensitive and accurate method based on high performance liquid chromato- graphy （HPLC） with diode array detector （DAD） was developed and validated for systematic quality evaluation of one type of traditional Chinese medicine preparations named Xinkeshu （XKS） tablet. In this study, the chromatographic fingerprints of XKS tablet were developed first, 23 peaks were selected as the common peaks to evaluate the similarities among different batches of XKS samples, which were manufactured in a long time span of three years. Additionally, simultaneous quantification of six markers in XKS tablet, including Danshensu, Protocatechuic aldehyde, Puerarin, Daidzin, Salvianolic acid B and Daidzein, was performed. The validation results showed that the developed method was specific, accurate, precise and robust. The preliminary explanation on why a close similarity between fingerprints did not exactly mean similar contents of chemical components in samples was given. The contribution of each chromatographic peak to similarity was also evaluated. The developed method offers an efficient, reliable and practical approach for systematic quality evaluation of XKS tablet.
文摘目的采用"Cocktail"探针药物法考察丹参注射液和心可舒片对家兔CYP酶5种亚型CYP1A2、CYP2C9、CYP2C19、CYP2D6和CYP3A4代谢的影响。方法将16只雄性家兔同时空腹给予混合探针药咖啡因、甲苯磺丁脲、奥美拉唑、右美沙芬和咪达唑仑,采用LC-MS/MS检测特定时间点的探针药物代谢率(代谢产物浓度与探针原型药物浓度的比值)。家兔随机分为丹参注射液组和心可舒片组,设计为自身对照实验,分3个周期,按顺序分别给药丹参低剂量组(0.5 m L·kg-1)、中剂量组(1 m L·kg-1)、高剂量组(2 m L·kg-1)和心可舒低剂量组(90 mg·kg-1)、中剂量组(180 mg·kg-1)和高剂量组(360 mg·kg-1)。每个周期经7 d洗净期后,连续给药7 d,第15天再给予探针药物后测代谢率。采用ANOVA方差分析比较各剂量组家兔和用药前探针药物的代谢率的变化。结果与用药前相比,各剂量组的混合探针药物代谢率均有下降趋势。结论丹参注射液、心可舒片使用7 d后可能抑制家兔体内CYP450酶代谢,与体外实验结果一致。这些药物与经过CYP450酶代谢的药物联合应用时,可能会引起药物相互作用,临床联合使用应提高警惕。
