摘要
目的:建立马鞭草提取物中马鞭草苷、戟叶马鞭草苷在大鼠血浆中的反相高效液相色谱(RP-HPLC)法,对其在大鼠体内药动学进行研究。方法:大鼠静脉注射低、中、高剂量马鞭草提取物后,分别于5、10、20、30、40、50、60、80、100、120、140 min取血样,以RP-HPLC法测定血浆中马鞭草苷、戟叶马鞭草苷的血药浓度。色谱柱为Shimadzu Shim-pack VP-ODS C18(150 mm×4.6mm,5μm),流动相为甲醇-水(30∶70,V/V),流速为1.0 ml/min,柱温为35℃,检测波长为238 nm,进样量为10μl。以DAS2.0版药动学程序软件计算药动学参数。结果:马鞭草苷与戟叶马鞭草苷的质量浓度分别在0.269~65.500、0.288~70.000 mg/L范围内与其峰面积和内标峰面积比值呈良好线性关系(r均>0.999 0)。马鞭草苷与戟叶马鞭草苷精密度试验的RSD均≤6.2%,准确度在(93.3±3.4)%^(107.8±2.2)%之间,提取回收率在(93.8±1.5)%^(97.3±1.7)%之间,稳定性试验的RSD均<5%。马鞭草苷和戟叶马鞭草苷在大鼠体内代谢均符合二室模型;马鞭草提取物高、中、低剂量组马鞭草苷的主要药动学参数t1/2β分别为(63.2±49.0)、(28.2±3.4)、(30.8±8.5)min;AUC(0-t)分别为(2 005.2±726.6)、(598.8±349.1)、(220.4±105.4)mg(/min·L)。马鞭草提取物高、中、低剂量组戟叶马鞭草苷主要药动学参数t1/2β分别为(50.2±30.2)、(23.3±3.8)、(21.2±6.9)min;AUC(0-t)分别为(2 736.2±971.4)、(842.6±469.3)、(314.5±136.0)mg(/min·L)。结论:该方法准确、灵敏、稳定性好、回收率高,适用于大鼠体内马鞭草苷、戟叶马鞭草苷的药动学研究。
OBJECTIVE： To develop an RP-HPLC method for the determination of plasma concentration of verbenalin and has- tatoside in Verbena officinalis extract, and to study pharmacokinetics of verbenalin and hastatoside in rats. METHODS： The blood samples were collected at 5, 10, 20, 30, 40, 50, 60, 80, 100, 120 and 140 min after rats were given low-dose, medium-dose and high-dose V. officinalis extract. The plasma concentrations of verbenalin and hastatoside were determined by RP-HPLC. The de- termination was performed on Shimadzu Shim-pack VP-ODS C18 （150 mm×4.6 mm, 5 μm） column with mobile phase consisted of methanol-water （30 ： 70, V/V） at the flow rate of 1.0 ml/min. The column temperature was 35 ℃ and UV detection wavelength was set at 238 nm. The sample size was 10 μl. The pharmacokinetic parameters of verbenalin and hastatoside were calculated by DAS2.0 software. RESULTS： The linear range of verbenalin and hastatoside were 0.269-65.500 mg/L and 0.288-70.000 mg/L, re- spectively （r〉0.999 0）. Verbenalin and hastatoside glucoside precision test of RSD is lower than 6.2%, the accuracy in （93.3 ±3.4）% to （107.8 ± 2.2）% ,the extraction recovery in （93.8± 1.5）% to （97.3 ± 1.7）%, stability test of RSD〈5%. Verbenalin and hastatoside showed two-compartment open model in rats. The main pharmacokinetic parameters of high-dose, medium-dose and low-dose verbenalin： t1/2β were（63.2 ± 49.0）, （28.2 ± 3.4） and （30.8 ± 8.5） min, respectively; AUC（0 , were （2 005.2 ±726.6）, （598.8± 349.1） and （220.4 ± 105.4） mg/（min.L）, respectively. The main pharmacokinetic parameters of high-dose, medium-dose and low-dose hastatoside： t1/2β were（50.2 ± 30.2）, （23.3 ± 3.8） and （21.2 ± 6.9） min, respectively; AUC（0 t） were （2 736.2 ± 971.4）, （842.6 ± 469.3） and （314.5 ± 136.0） mg/（min. L）, respectively. CONCLUSIONS： The method is accurate, sensitive, stable and re- producible. It is suitable for the pharmacokinetic study o
出处
《中国药房》
CAS
CSCD
2013年第39期3663-3666,共4页
China Pharmacy
基金
贵州省科学技术基金资助项目(No.黔科合J字〔2010〕2224号)
贵阳市科学技术计划项目(No.〔2010〕筑科农合同字第1-中-08号)
