鹿衔草中异高熊果苷、高熊果苷血药浓度测定及大鼠灌胃给药后药动学研究  

Plasma Concentration Determination of Isohomoarbutin and Homoarbutin from Pyrola decorata and Pharmacokinetics Study in Rats with Intragastric Administration

作　　者：张园园[1] 张玉杰[1] 王秀丽[1] 李磊[1] 李曼曼[1] 李颖[1] 杨洁[1] 

机构地区：[1]北京中医药大学中药学院,北京100102

出　　处：《中国药房》2015年第1期40-42,共3页China Pharmacy

摘　　要：目的：建立大鼠血浆中异高熊果苷和高熊果苷浓度测定的方法,并用于大鼠灌胃鹿衔草提取液后的药动学研究。方法：采用反相高效液相色谱法。色谱柱为Zobax Extend C18,流动相为甲醇-水（6∶94,V/V）,流速为0.8 ml/min,检测波长为280 nm,柱温为30℃,进样量为20μl。6只Wistar大鼠灌胃鹿衔草提取液（10 ml/kg,异高熊果苷、高雄果苷质量浓度分别为2.02、2.10 mg/ml）0、10、15、20、25、30、40 min,1、1.5、2、3、4、6 h后眼眶采血并测定血药浓度,计算药动学参数。结果：异高熊果苷、高熊果苷质量浓度在0.6-60μg/ml范围内与峰面积积分值呈良好线性关系;精密度的RSD均小于10%,准确度为91.9%-111.4%,稳定性的RSD均小于10%,提取回收率为90.1%-98.3%。大鼠灌胃给予鹿衔草药液后,异高熊果苷、高熊果苷在大鼠体内的药动学过程均符合二室模型,cmax分别为（18.5±3.4）、（35.1±6.4）μg/ml,tmax分别为（0.6±0.1）、（0.5±0.1）h,AUC0-∞分别为（37.7±4.5）、（52.7±10.0）μg·h/ml,CL分别为（0.54±0.06）、（0.41±0.10）L/h。结论：本方法可靠、灵敏、简便。鹿蹄草素可能不是鹿衔草的抗菌有效成分。OBJECTIVE： To establish a method for the determination of isohomoarbutin and homoarbutin in rat plasma and to study its pharmacokinetics in rats after intragastric administration of Pyrola decorata extract. METHODS： RP-HPLC method was adopted. The analysis was performed on a Zobax Extend C18 column with mobile phase consisted of methanol-water （6：94, V/V） at the flow rate of 0.8 ml/min. The detective wavelength was set at 280 nm, and column temperature was 30 ℃. The sample size was 20 pl. 6 Wistar rats were given P. decorata extract （10 ml/kg） intragastrically, and the concentrations of isohomoarbutin and ho- moarbutin were 2.02 and 2.10 mg/ml, respectively. The blood samples were collected from eye socket at 0, 10, 15, 20, 25, 30 and 40 min, 1, 1.5, 2, 3, 4 and 6 h after medication to detect plasma concentration and then calculate pharmacokinetic parame- ters. RESULTS： The linear range of isohomoarbutin and homoarbutin were 0.6-60 ~tg/ml, and RSD of precision was lower than 10% and accuracy were 91.9%-111.4%. RSD of stability was lower than 10%, and extraction recoveries were 90.1%-98.3%. The pharmacokinetic behavior of isohomoarbutin and homoarbutin in rats were both fitted to two-compartment open model. The pharmacokinetic parameters of isohomoarbutin and homoarbutin were as follows： Cmax were （18.5 ± 3.4） μg/ml and （35.1±6.4） μg/ml; tm were （0.6 ± 0.1） h and （0.5 ± 0.1） h; AUC were （37.7 ± 4.5） μg-h/ml and （52.7 ± 10.0） μg-h/ml; CL were （0.54 ±0.06） L/h and （0.41 ± 0.10） L/（h. kg）. CONCLUSIONS： The method is reliable, sensitive and convenient. Pryrolin could not be antibacterial effective components in P. decorata.

关 键 词：鹿衔草 大鼠 异高熊果苷 高熊果苷 药动学 反相高效液相色谱法 

分 类 号：R969[医药卫生—药理学]