1.Study on Pharmacokinetics of Sinapine Thiocyanate ,Quercetin and Kaempferol from Qili Qiangxin Capsule in Rats in vivo
Yu ZHANG ; Fugeng ZHANG ; Shaoqiang ZHANG ; Mingdan ZHU ; Xuefeng XIAO ; Wuxun DU
China Pharmacy 2019;30(15):2042-2046
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.