HPLC测定千里光提取物及千柏鼻炎胶囊中金丝桃苷在大鼠体内的血药浓度及药动学研究
|
摘要
目的:建立RP-HPLC测定大鼠血浆中金丝桃苷浓度的方法,研究千里光提取物及千柏鼻炎胶囊中金丝桃苷的在动物体内药动学特征,评价复方中药物配伍对金丝桃苷药动学的影响。方法 :大鼠分别灌胃给予千里光提取物、千柏鼻炎胶囊内容物,眼眶后静脉丛取血,离心得血浆,加乙腈沉淀蛋白处理后测定金丝桃苷的血药浓度,DAS2.0软件处理数据。结果金丝桃苷血浆浓度在0.341～13.64μg·mL~(-1)之间线性关系良好,检测限为0.079μg·mL~(-1),高,中,低浓度样品回收率分别为96.46%,98.62%,98.99%。大鼠灌胃千里光提取物和千柏鼻炎胶囊后的药-时曲线均符合二房室模型。灌胃千柏鼻炎胶囊后测定的金丝桃苷较千里光提取物的Cmax和AUC_(0→∞)分别比其增加了1.25和1.74倍。结论:本研究建立的RP-HPLC测定法,专属、准确、灵敏,适用于千里光提取物及千柏鼻炎胶囊中金丝桃苷的药动学研究。且研究显示,千柏鼻炎胶囊中的其他药材配伍可以促进金丝桃苷的吸收,提高金丝桃苷的生物利用度。
OBJECTIVE To develop a RP-HPLC method for determination of the concentration of hyperoside in rat plasma and comparative study of the pharmacokinetics of the extract of Senecionis scandens Herba and Qianbai Biyan Capsules,and to assess the effect of other components in medical material in compound on the pharmacokinetics of hyperoside.METHODS The rats received the extract of Senecionis scandens Herba and Qianbai Biyan Capsules by oral.After liquide extraction with acetonitrile,plasma concentration of hyperoside was measured.The pharmacokinetics parameters were calculated with 3 P97 program.RESULTS A good linear relationship of hyperoside was obtained between 0.341～13.64 μg·mL~(-1),the limit of determination was 0.079 μg·mL~(-1).The mean recoveries was96.46%,98.62%,98.99% for high,middle,low concentrations of the samples respectively.The plasma concentration-time curves of hyperoside was best fitted with two-compartments model.The AUC_(0→∞) and Cmax of hyperoside were much greater when Qianbai Biyan Capsules were administrated.CONCLUSION The HPLC method was selective,accurate and sensitive.The results indicated that the other herbs had significant affect on the absorption of hyperoside therefore effecting the bioavailability of hyperoside significantly.
OBJECTIVE To develop a RP-HPLC method for determination of the concentration of hyperoside in rat plasma and comparative study of the pharmacokinetics of the extract of Senecionis scandens Herba and Qianbai Biyan Capsules,and to assess the effect of other components in medical material in compound on the pharmacokinetics of hyperoside.METHODS The rats received the extract of Senecionis scandens Herba and Qianbai Biyan Capsules by oral.After liquide extraction with acetonitrile,plasma concentration of hyperoside was measured.The pharmacokinetics parameters were calculated with 3 P97 program.RESULTS A good linear relationship of hyperoside was obtained between 0.341～13.64 μg·mL~(-1),the limit of determination was 0.079 μg·mL~(-1).The mean recoveries was96.46%,98.62%,98.99% for high,middle,low concentrations of the samples respectively.The plasma concentration-time curves of hyperoside was best fitted with two-compartments model.The AUC_(0→∞) and Cmax of hyperoside were much greater when Qianbai Biyan Capsules were administrated.CONCLUSION The HPLC method was selective,accurate and sensitive.The results indicated that the other herbs had significant affect on the absorption of hyperoside therefore effecting the bioavailability of hyperoside significantly.
引文
[1] 国家药典委员会.中华人民共和国药典·一部[S].北京:中国医药科技出版社,2015:511-512.
[2] 国家药典委员会.中华人民共和国药典·一部[S].北京:中国医药科技出版社,2015:33-34.
[3] 王梦夏,郭方遒,孙琼,等.高效液相色谱法结合化学计量学测定千里光中四种活性成分的含量[J].分析科学学报,2014(2):219-222.
[4] 王秀芹,林彤,顾利红.千柏鼻炎胶囊质量标准研究[J].中成药,2012,34(8):1505-1509.
[5] 史宁,郭宏举,王欢,等.金丝桃苷对急性炎症疼痛模型小鼠的抗炎镇痛作用研究[J].药物评价研究,2016,39(5):771-774.
[6] 王丽敏,卢春凤,白雪,等.金丝桃苷联合长春新碱对人结肠癌HCT8细胞增殖和凋亡的影响[J].时珍国医国药,2016,27(4):792-794.
[7] 黄凯,耿淼,王建华,等.金丝桃苷对免疫性肝损伤小鼠的保护作用[J].中国实验方剂学杂志,2015,21(19): 137-141.
[8] 白鑫宇,杨晓峰,赵叶利,等.金丝桃苷对内毒素(LPS)诱导的小鼠急性肾损伤的保护作用[J].沈阳药科大学学报,2014,31(10):799-803.
[9] 郑梅竹,李杰帅,范亚军,等.金丝桃苷等5个天然黄酮类化合物的抗抑郁活性筛选研究[J].时珍国医国药,2013,24(5): 1043-1045.
[2] 国家药典委员会.中华人民共和国药典·一部[S].北京:中国医药科技出版社,2015:33-34.
[3] 王梦夏,郭方遒,孙琼,等.高效液相色谱法结合化学计量学测定千里光中四种活性成分的含量[J].分析科学学报,2014(2):219-222.
[4] 王秀芹,林彤,顾利红.千柏鼻炎胶囊质量标准研究[J].中成药,2012,34(8):1505-1509.
[5] 史宁,郭宏举,王欢,等.金丝桃苷对急性炎症疼痛模型小鼠的抗炎镇痛作用研究[J].药物评价研究,2016,39(5):771-774.
[6] 王丽敏,卢春凤,白雪,等.金丝桃苷联合长春新碱对人结肠癌HCT8细胞增殖和凋亡的影响[J].时珍国医国药,2016,27(4):792-794.
[7] 黄凯,耿淼,王建华,等.金丝桃苷对免疫性肝损伤小鼠的保护作用[J].中国实验方剂学杂志,2015,21(19): 137-141.
[8] 白鑫宇,杨晓峰,赵叶利,等.金丝桃苷对内毒素(LPS)诱导的小鼠急性肾损伤的保护作用[J].沈阳药科大学学报,2014,31(10):799-803.
[9] 郑梅竹,李杰帅,范亚军,等.金丝桃苷等5个天然黄酮类化合物的抗抑郁活性筛选研究[J].时珍国医国药,2013,24(5): 1043-1045.