首页|UPLC-MS/MS测定大鼠血浆中香附烯酮和α-香附酮浓度及其药动学研究

UPLC-MS/MS测定大鼠血浆中香附烯酮和α-香附酮浓度及其药动学研究

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目的 建立UPLC-MS/MS测定大鼠血浆中香附烯酮和α-香附酮的方法,并研究其药动学.方法 采用Phenomennex C18(150 mm×2.0 mm,3 μm)色谱柱,以乙腈-水为流动相进行梯度洗脱,柱温30℃,进样量1μL,蛇床子素为内标,采用电喷雾离子源,正离子模式,香附烯酮m/z为219.1/135.1,α-香附酮m/z为219.1/111.0,蛇床子素m/z为245.0/123.0.检测大鼠血浆中香附烯酮、α-香附酮的浓度,应用DAS2.0软件拟合主要的药动学参数.结果 香附烯酮在10~500ng·mL-1内线性关系良好(r=0.991 0),α-香附酮在2.5~300 ng·mL-1内线性关系良好(r=0.994 1),日内精密度RSD<9.45%,日间精密度RSD<9.09%,加样回收率>86.79%.SD大鼠灌胃给予香附挥发油提取物(20 mg·kg-1)后,香附烯酮和α-香附酮Cmax、AUC0-∞、MRT(0-∞)分别为(8 862.59±1 106.81)ngL-1,(7 060.94±774.25)ng·L-1·h,(3.21±0.72)h 和(934.69±106.81)ng·L-1,(792.26±74.52)ng·L-1.h,(4.94±0.82)h.结论 建立的方法能够快速、准确测定血浆中香附烯酮和α-香附酮的浓度,可用于香附烯酮和α-香附酮在大鼠体内的药动学研究.
Determination of Cyperenone and α-Cyperone in Rat Plasma by UPLC-MS/MS and Their Pharmacokinetics
OBJECTIVE To establish an UPLC-MS/MS method for the determination of the concentrations of cyperenone andα-cyperone in rat plasma and to study the pharmacokinetics.METHODS Gradient elution was carried out on a Phenomennex C18(150 mm×2.0 mm,3 μm)column with acetonitrile-water as mobile phase.The column temperature was 30℃,injection volume was l μL,osthenite was used as the internal standard,electrospray ion source and positive ion mode were used.The m/z values of cyperenone,α-cyperone and osthenite were 219.1/135.1,219.1/111.0 and 245.0/123.0,respectively.The plasma concentrations of cyperenone and α-cyperone were measured,and the main pharmacokinetic parameters were calculated using DAS 2.0 software.RESULTS The linear relationship of cyperenone was good in the range of 10-500 ngmL-1(r=0.991 0),and the linear relationship of α-cyperone was good in the range of 2.5-300 ng·mL-1(r=0.994 1),RSDs of intra-day precision were less than 9.45%.RSDs of daytime precision were less than 9.09%.The recoveries were greater than 86.79%.After intragastric administration of essential oil extract(20 mgkg-1)from Cyperus rotundus L.in SD rats.The pharmacokinetic parameters of Cmax,AUC0-∞ and MRT(0-∞)of cyperenone and α-cyperone were(8 862.59±1 106.81)ng·L-1,(7 060.94±774.25)ng·L-1h,(3.21±0.72)h and(934.69±106.81)ng·L-1,(792.26±74.52)ng·L-1h,(4.94±0.82)h,respectively.CONCLUSION The established method can be used for the rapid and accurate determination of the concentration of cyperenone and α-cyperone in plasma,and can be used for the pharmacokinetic study of cyperenone and α-cyperone in rats in vivo.

Cyperus rotundus L.pharmacokineticcyperenoneα-cyperoneosthenite

封传华、郭慧玲、汤小林、赵晓娟、范新禄、刘德坤、李刚

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南昌大学第一附属医院,南昌 330000

江西中医药大学,南昌 330100

江西省儿童医院,南昌 330002

中国人民解放军联勤保障部队第908医院,南昌 330000

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香附 药动学 香附烯酮 α-香附酮 蛇床子素

国家自然科学基金江西省卫生健康委员科技计划项目江西省卫生健康委员科技计划项目江西省中医药科研项目江西省中医药管理局重点研究室临床研究基地建设项目(第三批)南昌大学第一附属医院青年人才科研培育基金

8216073720165563202048142019A155KP202203007YFYPY202263

2023

中国现代应用药学
中国药学会

中国现代应用药学

CSTPCDCSCD北大核心
影响因子:0.877
ISSN:1007-7693
年,卷(期):2023.40(23)
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