芪苈强心胶囊中芥子碱硫氰酸盐、槲皮素和山柰酚在大鼠体内的药动学研究
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篇名: 芪苈强心胶囊中芥子碱硫氰酸盐、槲皮素和山柰酚在大鼠体内的药动学研究
TITLE:
摘要: 目的:建立测定大鼠血浆中芥子碱硫氰酸盐、槲皮素和山柰酚含量的方法,并研究大鼠体内芪苈强心胶囊的药动学。方法:采用高效液相色谱-串联质谱(HPLC-MS/MS)法。色谱柱为ZOBRAX XDB-C18,流动相为0.1%甲酸水溶液-含0.1%甲酸的乙腈溶液(梯度洗脱),流速为0.45 mL/min,进样量为10 μL,定量离子为芥子碱硫氰酸盐质荷比(m/z)310.2→251.2,槲皮素m/z 301.1→150.7,山柰酚m/z 286.2→242.0,内标氯霉素m/z 320.9→151.9。6只大鼠灌胃给予芪苈强心胶囊1.3 g/kg后0.083、0.167、0.333、0.667、1、1.5、2、3、4、6、8、12、24 h经目内眦静脉丛取血,并测定芥子碱硫氰酸盐、槲皮素和山柰酚的血药浓度。采用DAS 3.0软件拟合计算各药动学参数。结果:芥子碱硫氰酸盐、槲皮素和山柰酚的检测质量浓度线性范围分别为0.05~100、0.1~200、0.1~200 ng/mL(r=0.999 4、0.999 7、0.999 9),精密度试验及基质效应RSD均≤11.55%(n=6),稳定性试验RE≤14.69%(n=3)。芥子碱硫氰酸盐、槲皮素和山柰酚在大鼠体内的cmax分别为(1.35±0.62)、(3.23±1.26)、(5.27±1.66) ng/mL,tmax分别为(1.50±0.00)、(0.67±0.00)、(0.67±0.00) h,t1/2分别为(3.98±0.99)、(3.33±0.41)、(4.54±0.85) h,CL分别为(3 683.82±987.96)、          (2 852.33±695.88)和(1 611.85±129.59) mL/(h·kg),AUC0-24 h分别为(3.98±1.21)、(10.96±3.42)和(13.59±5.35) h·ng/mL。结论:该检测方法灵敏度高、专属性强、重复性好,适用于芪苈强心胶囊中芥子碱硫氰酸盐、槲皮素和山柰酚在大鼠体内的药动学研究。
ABSTRACT: OBJECTIVE: To establish a method for the content determination of sinapine thiocyanate, quercetin and kaempferol in rat plasma, and to study pharmacokinetics of Qili qiangxin capsule in rats in vivo. METHODS: HPLC-MS/MS method was adopted. The determination was performed on ZOBRAX XDB-C18 column with mobile phase consisted of 0.1% formic acid solution and acetonitrile containing 0.1% formic acid (gradient elution) at the flow rate of 0.45 mL/min. The sample size was 10 μL. Quantitative ions were sinapine thiocyanate with m/z 310.2→251.2, quercetin with m/z 301.1→150.7, kaempferol with m/z 286.2→242.0, internal standard chloramphenicol with m/z 320.9→ 151.9. 0.083, 0.167, 0.333, 0.667, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 h after intragastric administration of Qili qiangxin capsule 1.3 g/kg, blood samples were collected via intraocular canthal venous plexus of 6 rats. The blood concentrations of sinapine thiocyanate, quercetin and kaempferol were determined. The pharmacokinetic parameters were calculated and fitted by using DAS 3.0 software. RESULTS: The linear range of sinapine thiocyanate, quercetin and kaempferol 0.05-100, 0.1-200, 0.1-200 ng/mL(r=0.999 4, 0.999 7, 0.999 9); RSDs of precision test and matrix effect were all less than or equal to 11.55% (n=6), RE of stability test is less than or equal to 14.69% (n=3). The pharmacokinetic parameter of sinapine thiocyanate, quercetin and kaempferol included that cmax were(1.35±0.62),(3.23±1.26),(5.27±1.66)      ng/mL; tmax were (1.50±0.00), (0.67±0.00), (0.67±0.00) h; t1/2 were (3.98±0.99),(3.33±0.41),(4.54±0.85) h; CL were (3 683.82±987.96), (2 852.33±695.88),(1 611.85±129.59) mL/(h·kg); AUC0-24 h were (3.98±1.21), (10.96±3.42), (13.59±5.35) h·ng/mL. CONCLUSIONS: Established method is highly sensitive, specific and reproducible, and suitable for the pharmacokinetic study of sinapine thiocyanate, quercetin and kaempferol in rat.
期刊: 2019年第30卷第15期
作者: 张瑜,张富赓,张少强,朱明丹,肖学凤,杜武勋
AUTHORS: ZHANG Yu,ZHANG Fugeng,ZHANG Shaoqiang,ZHU Mingdan,XIAO Xuefeng,DU Wuxun
关键字: 芪苈强心胶囊;芥子碱硫氰酸盐;槲皮素;山柰酚;药动学;高效液相色谱-串联质谱法;大鼠
KEYWORDS: Qili qiangxin capsule; Sinapine thiocyanate; Quercetin; Kaempferol; Pharmacokinetics; HPLC-MS/MS; Rat
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