通心络超微粉大鼠药代动力学研究  

Pharmacokinetics of Tongxinluo Supermicro Powder in Rats

作　　者：王海荣[1,2] 王宏涛[2] 刘丽杰[2] 赵韶华[2] 张兰桐[1] 

机构地区：[1]河北医科大学药学院,河北石家庄050017 [2]石家庄以岭药业股份有限公司,河北石家庄050035

出　　处：《时珍国医国药》2014年第6期1328-1331,共4页Lishizhen Medicine and Materia Medica Research

基　　金：国家重点基础研究发展计划(973计划)项目(No.2012CB518606)

摘　　要：目的建立快速、灵敏、简便的大鼠血浆中芍药苷定量分析的HPLC-MS-MS方法;研究大鼠灌胃给予通心络超微粉后的大鼠血浆中芍药苷的药物动力学,为评价其临床疗效提供依据。方法研究大鼠以6g/kg剂量单次和多次灌胃给予通心络超微粉(相当于芍药苷24.52 mg/kg)后芍药苷的药物动力学。测定血浆中芍药苷的浓度,绘制药-时曲线并计算其药代动力学参数。结果单次和多次给予通心络超微粉Cmax分别为77.8,189.6 ng/ml,t1/2分别为(207.9±138.3)min,(224.3±120.4)min,AUC0-∞分别为31662,40493 ng·min/ml。单次给药芍药苷吸收缓慢,而多次给药(3次/d,第10次给药后检测)后吸收迅速,首次达峰为28 min,120 min后再次达峰。结论多次给予通心络超微粉后芍药苷在大鼠体内有累积作用;复方制剂及不同给药剂量可影响中药活性成分的吸收及临床疗效。Objective A rapid, sensitive and specific liquid chromatography - tandem mass spectrometric （ LC - MS - MS） meth- od was developed and validated for determination of paeonifiorin in rat plasma. The pharmacokineties of paeonifiorin was evaluated in rats after intragastric administration of TXLSP and provide a firm basis for evaluating the clinical efficacy of TXLSP. Methods The pharmacokinetics of paeoniflorin was evaluated in rats after a single and multiple dosing of 6 g/kg of TXLSP （ 24.52 mg/kg, paeoniflorin）. The plasma concentration and pharmaeokinetic profiles of paeoniflorin was determined. The main pharmaeokinetic parameters of paeoniflorin were calculated. Results After single and multiple dosing of TXLSP the main pharmacokinetic parame- ters were as follows： Cmax77.8 ng/ml and 189.6 ng/ml; hn（207.9 ± 138.3） rain and （224.3 ± 120.4） rain; AUC0-∞ 31662 ng. min/ml and 40493 ng. min/ml. Paeoniflorin reached a maximum slowly for single administration and reached a maxi- mum firstly at 28 min and 120 min secondly for multiple dosing. Conclusion It was found that the accumulation achieved with multiple doses of TXLSP. It was indicated that the complex prescription and different dosages can influence the absorption of active ingredient and the clinical efficacy.

关 键 词：通心络超微粉 芍药苷 药物动力学 HPLC-MS-MS 

分 类 号：R962[医药卫生—药理学]