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  

Determination of Cyperenone and α-Cyperone in Rat Plasma by UPLC-MS/MS and Their Pharmacokinetics

作　　者：封传华 郭慧玲[2] 汤小林[3] 赵晓娟[2] 范新禄 刘德坤 李刚[4] FENG Chuanhua;GUO Huiling;TANG Xiaolin;ZHAO Xiaojuan;FAN Xinlu;LIU Dekun;LI Gang(The First Affiliated Hospital of Nanchang University,Nanchang 330000,China;Jiangxi University of Chinese Medicine,Nanchang 330100,China;Jiangxi Provincial Children’s Hospital,Nanchang 330002,China;The 908th Hospital of PLA Joint Logistic Support Force,Nanchang 330000,China)

机构地区：[1]南昌大学第一附属医院,南昌330000 [2]江西中医药大学,南昌330100 [3]江西省儿童医院,南昌330002 [4]中国人民解放军联勤保障部队第908医院,南昌330000

出　　处：《中国现代应用药学》2023年第23期3197-3201,共5页Chinese Journal of Modern Applied Pharmacy

基　　金：国家自然科学基金项目(82160737);江西省卫生健康委员科技计划项目(20165563,20204814);江西省中医药科研项目(2019A155);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)(KP202203007);南昌大学第一附属医院青年人才科研培育基金项目(YFYPY202263)。

摘　　要：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 C_(18)(150 mm×2.0 mm,3μm)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DAS 2.0软件拟合主要的药动学参数。结果香附烯酮在10~500 ng·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C_(max)、AUC_(0-∞)、MRT_((0-∞))分别为(8 862.59±1 106.81)ng·L^(-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。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 C_(18)(150 mm×2.0 mm,3μm) column with acetonitrile-water as mobile phase.The column temperature was 30℃,injection volume was 1μL,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 ng·mL^(-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 mg·kg^(-1)) from Cyperus rotundus L.in SD rats.The pharmacokinetic parameters of C_(max),AUC_(0-∞)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^(-1)·h,(3.21±0.72)h and (934.69±106.81)ng·L^(-1),(792.26±74.52)ng·L^(-1)·h,(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.

关 键 词：香附 药动学 香附烯酮 Α-香附酮 蛇床子素 

分 类 号：R285.5[医药卫生—中药学]