不同模型下清脑宣窍方有效组分药代动力学研究  被引量:11

Pharmacokinetics of effective fractions of Qingnaoxuanqiao Formula in different rat models

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作  者:周威[1] 石任兵[1] 孙建宁[1] 王永炎[2] 

机构地区:[1]北京中医药大学中药学院,北京100102 [2]中国中医科学院

出  处:《北京中医药大学学报》2008年第4期265-268,共4页Journal of Beijing University of Traditional Chinese Medicine

基  金:高等学校科技创新工程重大项目培育资金项目(No.v200611)

摘  要:目的研究清脑宣窍方有效组分栀子苷、人参皂苷Rg1、人参皂苷Rb1、三七皂苷R1在正常、脑中风急性期和恢复期状态下大鼠体内的药代动力学变化。方法按双侧颈动脉结扎并喂养2周制备中风恢复期模型,采用MCAO法制备中风急性期模型。灌服给予清脑宣窍方有效组分,血浆样品用C18固相柱萃取,以亥茅酚苷为内标,选用Agilent Eclipse XDB-C18色谱柱(4.6mm×250mm,5μm),流动相为乙腈-水二元梯度洗脱,柱温为30℃;流速为1.0mL/min;检测波长为203nm。采用DAS1.0软件对各血浆药物浓度进行拟和分析。结果栀子苷、人参皂苷Rg1、三七皂苷R1在大鼠体内药动学过程均属于二室模型,人参皂苷Rb1属于一室模型。各组分最高血药浓度(Cmax)、血药浓度时间曲线下面积(AUC)值均表现为急性模型组>恢复模型组>正常组。结论不同模型下动物对清脑宣窍方有效组分吸收不同,同等剂量下生物利用度顺序为急性模型组>恢复模型组>正常组。Objective To study the changes of pharmacokinetics of the effective fractions of Qingnaoxuanqiao Formula, including geniposide, ginsenoside Rgl, ginsenoside Rbl and notoginsenoside Rl in rats of normal, acute phase and convalescent phase of apoplexy. Methods The model of convalescent phase of apoplexy was established by ligating bilateral carotids of SD rats and feeding for 2 weeks, and the model of acute phase of apoplexy was established by MCAO method. The models were given orally the effective fractions of Qingnaoxuanqiao Formula and the blood samples were extracted by Cls solid phase column. Sec-o-glucosyl-hamaudol was taken as internal index. Agilent Eclipse XDB-Cls chromatography column (4.6 mm × 250 mm, 5μm ) was applied. The gradient mobile phase was HCN- H2O system with column temperature of 30 ℃ and flow rate was 1.0 mL/min. The detecting wavelength was 203 nm. The plasma concentrations of different effective infractions were analyzed by DAS 1.0 software.compartment model, and that of ginsenoside Rbl was fitted with one-compartment model in rats. The values of Cmax. and AUC of above 4 infractions showed as follows : the value of acute phase group 〉 that of convalescent phase group 〉 that of normal group. Conclusion The absorptions of effective fractions of Qingnaoxuanqiao formula in different rat models are different. The value of bioavailability in the same dose is as follow order: the value of acute phase group 〉 that of convalescent phase group 〉 that of normal group.

关 键 词:清脑宣窍方 有效组分 中风 药代动力学 大鼠 

分 类 号:R969.1[医药卫生—药理学]

 

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