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引用本文:封传华,郭慧玲,汤小林,赵晓娟,范新禄,刘德坤,李刚.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[J].中国现代应用药学,2023,40(23):3197-3201.
FENG Chuanhua,GUO Huiling,TANG Xiaolin,ZHAO Xiaojuan,FAN Xinlu,LIU Dekun,LI Gang.Determination of Cyperenone and α-Cyperone in Rat Plasma by UPLC-MS/MS and Their Pharmacokinetics[J].Chin J Mod Appl Pharm(中国现代应用药学),2023,40(23):3197-3201.
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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
封传华1, 郭慧玲2, 汤小林3, 赵晓娟2, 范新禄2, 刘德坤2, 李刚4
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
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 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1 μL,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Cmax、AUC0-∞、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。
关键词:  香附  药动学  香附烯酮  α-香附酮  蛇床子素
DOI:10.13748/j.cnki.issn1007-7693.20230631
分类号:R285.5
基金项目: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)
Determination of Cyperenone and α-Cyperone in Rat Plasma by UPLC-MS/MS and Their Pharmacokinetics
FENG Chuanhua1, GUO Huiling2, TANG Xiaolin3, ZHAO Xiaojuan2, FAN Xinlu2, LIU Dekun2, LI Gang4
1.The First Affiliated Hospital of Nanchang University, Nanchang 330000, China;2.Jiangxi University of Chinese Medicine, Nanchang 330100, China;3.Jiangxi Provincial Children's Hospital, Nanchang 330002, China;4.The 908th Hospital of PLA Joint Logistic Support Force, Nanchang 330000, China
Abstract:
OBJECTIVE To establish an UPLC-MS/MS method for the determination of the concentrations of cyperenone and α-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 1 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 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 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-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.
Key words:  Cyperus rotundus L.  pharmacokinetic  cyperenone  α-cyperone  osthenite
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