摘要
目的：通过建立HPLC-UV法研究三七皂苷R1在正常和心肌缺血模型大鼠的体内药动学。方法：将48只雄性SD大鼠等分成正常对照组和模型组,以垂体后叶素诱导急性心肌缺血模型,两组均分为三七皂苷R1高、中、低（200、100、50 mg/kg）剂量组,单次灌胃给药后于不同时间点采血,以淫羊藿苷为内标,流动相为乙腈-水,经Waters symmetry C18色谱柱（250 mm×4.6 mm,5μm）分离,检测波长203 nm,采用DAS 2.0软件计算药动学变化参数。结果：三七皂苷R1在该方法下线性范围为0.2~125μg/m L,R2=0.9997,以信噪比1∶3计算最低检测限为0.053μg/m L,提取率、日间、日内精密度、专属性、准确度、精密度符合生物样品处理要求。与正常大鼠比较,模型大鼠AUC0-t和AUC0-∞显著增加（P〈0.01）,消除半衰期显著延长（P〈0.01）。结论：该方法专属性强、灵敏度高、准确性好,操作简便,可用于三七皂苷R1的含量测定及药动学研究;模型组大鼠对三七皂苷R1生物利用度显著高于正常对照组,表明三七皂苷R1在模型组大鼠体内更能发挥其药效。
Objective： To establish an HPLC-UV method for determining pharmacokinetic difference of notoginsenoside R1 between normal rats and ischemic rats. Methods： 48 male SD rats were randomly divided into normal group and acute myocardial ischemia（ AMI）model group induced by pituitrin and each group was classified into high,middle and low-dose of groups with notoginsenoside R1（ 200,100 and 50 mg/kg） respectively. Blood samples were collected at different points in time after they were administered once by gavage and separated by Waters symmetry C18column（ 250 mm × 4. 6 mm,5 μm） under the detective wavelength 203 nm,the mobile phase was acetonitrile-water with icariin as the internal standard and the pharmacokinetic parameters were calculated by DAS 2. 0. Results： Notoginsenoside R1 had good linearity in the ranges of 0. 2 ~ 125 μg/m L（ R2= 0. 9997） with SNR 1 ∶ 3 and the lowest detection limit was0. 053 μg/m L,the extraction rate,RSDs of within-day and between-day,specificity,accuracy and precision accorded with the requirement of bio-sample pretreatment. Compared to the normal group,AUC0-tand AUC0-∞was significantly increased（ P〈0. 01） and the terminal half-life was prolonged markedly（ P〈0. 01） in AMI group. Conclusions： The method is simple,accurate and had high specificity and sensitivity,that could be applied in quantitative determination of notoginsenoside R1 and research of pharmacokinetics; the relative bioavailability of notoginsenoside R1 is increased significantly in AMI group,which indicates that notoginsenoside R1 has better effect in model rat.
出处
《中药材》
CAS
CSCD
北大核心
2015年第9期1908-1911,共4页
Journal of Chinese Medicinal Materials
基金
广东省社会发展领域科技计划项目(83100)
广东省中医药管理局基金资助项目(1060060
2008005)
广州市中医药中西医结合科研项目(20112A011011)
广东省医院药学研究基金(2015A11)
