前列安颗粒中芍药苷和连翘苷在大鼠体内的药动学研究  

Study on Pharmacokinetics of Paeoniflorin and Phillyrin from Qianliean Granules in Rats in vivo

作　　者：田溪[1] 梁振江[2] 郭安然[2] 杨秀岭[1] 

机构地区：[1]河北医科大学第二医院药学部,石家庄050000 [2]河北医科大学第二医院制剂科,石家庄050000

出　　处：《中国药房》2016年第10期1363-1366,共4页China Pharmacy

摘　　要：目的：建立大鼠血浆中芍药苷和连翘苷浓度测定的方法,并用于大鼠ig前列安颗粒后的药动学研究。方法：采取液相色谱-质谱联用（LC-MS/MS）法。色谱柱为Waters C18;流动相为乙腈（A）-2 mmol/L乙酸铵溶液（含0.05%甲酸）（B）（0~9 min：15%A→50%A;9~11 min：50%A→90%A;11~17 min：90%A;17~19 min：90%A→15%A;19~20 min：15%A）;流速为0.6 ml/min;柱温为35℃;进样量为20μl;定量离子对为芍药苷m/z 525.2→m/z 449.0,连翘苷m/z 552.3→m/z 355.3。7只雄性SD大鼠ig前列安颗粒药液1 g（生药）/kg后0.25、0.5、0.75、1、1.5、2、3、4、6、8、10、12、24 h眼内眦取血0.5 ml测定血药浓度,采用DAS 2.1.1药动学软件计算药动学参数。结果：芍药苷、连翘苷检测质量浓度线性范围分别为5.0~2 500.0μg/L（r=0.997 9）、2.0~2 000.0μg/L（r=0.998 2）;精密度试验的RSD均小于5.5%（n=5）;方法回收率分别为96.0%~104.0%、92.0%~107.0%,提取回收率分别为71.4%~83.5%、81.5%~92.3%;稳定性试验的RSD均小于5.0%（n=3）。芍药苷、连翘苷在大鼠体内的t1/2分别为（2.206±0.631）、（1.355±0.317）h,cmax分别为（1 504.069±620.885）、（79.043±15.568）μg/L,tmax分别为（1.000±0.250）、（1.214±0.267）h,AUC0-24 h分别为（4 897.645±2 207.577）、（263.475±54.795）μg·h/L,CL分别为（5.025±2.773）、（76.253±13.986）L/（h·kg）。结论：该方法灵敏度高、专属性强、操作简便、准确可靠,可应用于芍药苷、连翘苷在大鼠体内的药动学特征研究。OBJECTIVE：To establish a method for determining the plasma concentration of paeoniflorin and phillyrin and pharmacokinetic study before and after intragastric administration of Qianliean granules. METHODS：LC-MS/MS method was adopted.The column was Waters C18 with mobile phase consisted of acetonitrile（A）-2 mmol/L ammonium acetate（containing 0.05% formic acid）（B）（0-9 min：15% A→50% A;9-11 min：50% A→90% A;11-17 min：90% A;17-19 min：90% A→15% A;19-20 min：15%A）,at the flow rate of 0.6 ml/min;column temperature was 35 ℃ and the volume was 20 μl;quantitative ions were paeoniflorin m/z 525.2 → m/z 449.0,phillyrin m/z 552.3 → m/z 355.3. 7 SD male rats were docked to collect blood 0.5 ml from angular vein0.25,0.5,0.75,1,1.5,2,3,4,6,8,10,12,24 h after administration Qianliean granule solution 1 g（medicinal materials）/kg to determine the blood concentration of drugs. DAS 2.1.1 software was employed to calculate pharmacokinetic parameters. RESULTS：The linear range of paeoniflorin and phillyri were 5.0-2 500.0 μg/L（r=0.997 9）and 2.0-2 000.0 μg/L（r=0.998 2）,respectively;RSD of precision test was less than 5.5%（n=5）;the method recovery were 96.0%-104.0% and 92.0%-107.0%,the extration recovery were 71.4%-83.5% and 81.5%-92.3% and RSD of stability test was less than 5.0%（n=3）. The pharmacokinetic parameters of paeoniflorin and phillyrin were as follows as t1/2of（2.206±0.631）and（1.355±0.317）h;cmaxof（1 504.069±620.885）and（79.043±15.568）μg/L;tmaxof（1.000 ± 0.250）and（1.214 ± 0.267）h;AUC0-24 hof（4 897.645 ± 2 207.577）and（263.475±54.795）μg·h/L;CL of（5.025±2.773）and（76.253±13.986）L/（h·kg）. CONCLUSIONS：The method is highly sensitive,exclusive,simple,accurate and reliable,and can be applied to study the pharmacokinetic characteristics of paeoniflorin and phillyrin in rats in vivo.

关 键 词：液相色谱-质谱联用 前列安颗粒 连翘苷 芍药苷 药动学 大鼠 

分 类 号：R285[医药卫生—中药学]