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苏木对羟基红花黄色素A在寒凝血瘀大鼠体内药代动力学的影响
徐宁1,董娟妮1,吴一振1,陈向梅1,夏丽1,彭莉蓉2,于洁1,廖莎1,刘勤社1,3,郑晓晖1,4*
0
(1.西北大学生命科学学院中药学系,西安 710069
2.西安市中心医院药剂科,西安 710086
*通信作者)
摘要:
目的 建立寒凝血瘀大鼠体内羟基红花黄色素A(HSYA)的反相高效液相色谱分析方法,研究苏木对HSYA在寒凝血瘀模型大鼠体内药代动力学(药动学)的影响。 方法 寒凝血瘀模型大鼠12只,随机分为2组,分别灌服红花单煎液和红花-苏木合煎液,于给药后5、10、20、30、45、60、90、120、150、210、270 min眼底静脉丛取血,20%三氯乙酸水溶液沉淀蛋白,采用RP-HPLC法检测给药不同时间后大鼠血浆中HSYA的浓度,DAS 2.0药动学软件计算药动学参数。 结果 与红花单用组相比,红花与苏木配伍后,大鼠血浆中HSYA的药时曲线下面积AUC(0-t)和峰浓度Cmax及分布半衰期t1/2α增大(P<0.01),表观分布容积V1/F和清除率CL/F减小(P<0.01)。 结论 苏木可促进寒凝血瘀模型大鼠对红花中HSYA的吸收,降低HSYA在体内的分布,从而发挥增效作用。
关键词:  红花  苏木  羟基红花黄色素A  寒凝血瘀  药代动力学
DOI:10.3724/SP.J.1008.2013.00458
投稿时间:2012-11-02修订日期:2013-03-11
基金项目:“十一五”国家科技支撑计划课题(2008BAI51B01),陕西省自然科学基金(2011JM4042,2011JM4047),陕西省中医药管理局项目(ZY47,20072506),深圳市科技工贸和信息化委员会项目(CXB201005260069A).
Effects of Sappan lignum on pharmacokinetics of hydroxysafflor yellow A from Carthami flos in rats with cold coagulation and blood stasis
XU Ning1,DONG Juan-ni1,WU Yi-zhen1,CHEN Xiang-mei1,XIA Li1,PENG Li-rong2,YU Jie1,LIAO Sha1,LIU Qin-she1,3,ZHENG Xiao-hui1,4*
(1. Department of Traditional Chinese Medicine, College of Life Sciences, Northwest University, Xi’an 710069, Shaanxi, China
2. Department of Pharmacy, the Central Hospital of Xi’an,Xi’an 710086, Shaanxi, China
*Corresponding author.)
Abstract:
Objective To develop a reversed phase high performance liquid chromatographic (RP-HPLC) analysis system for hydroxysafflor yellow A (HSYA) in rat model of cold coagulation and blood stasis (CCBS), and to investigate the influence of Sappan lignum on the pharmacokinetics of HSYA in CCBS rats. Methods Rat CCBS models were randomly divided into two groups with each containing 6 animals. Rats were orally given Carthami flos extract or Carthami flos extract combined with Sappan lignum (The dosage: 20.0 g/kg crud drug of Carthami flos). Plasma samples were collected in heparinized tubes from the oculi chorioideae vein at 5, 10, 20, 30, 45, 60, 90, 120, 150, 210, and 270 min after drug administration; and the plasma proteins were precipitated with 20% trichloroacetic acid aqueous solution. Plasma concentrations of HSYA were detected by RP-HPLC at different time points after drug administration. The data were processed by DAS 2.0 software to calculate the pharmacokinetic parameters. Results Compared with the Carthami flos group, the pharmacokinetic parameters V1/F and CL/F of HSYA in the Carthami flos combined with Sappan lignum group were significantly decreased (P<0.01), and the AUC0-t, Cmax, and t1/2α of HSYA were significantly increased (P<0.01). Conclusion Sappan lignum can promote the absorption of HSYA in rat model of CCBS and reduce the distribution of HSYA, thus exercise an efficacy-enhancing effect.
Key words:  Carthami flos  Sappan lignum  hydroxysafflor yellow A  cold coagulation and blood stasis  pharmacokinetics