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目的建立测定人血浆中丁咯地尔质量浓度的HPLC法,并应用该法研究盐酸丁咯地尔片在健康人体内的药动学。方法色谱柱为Kromasil C18柱(250 mm×4.6 mm,5μm),流动相为乙腈-50mmol.L-1磷酸二氢铵缓冲液-三乙胺(体积比25∶75∶0.05),检测波长为275 nm,内标为乌拉地尔。结果丁咯地尔质量浓度线性范围为20μg.L-1～6.000 mg.L-1,回归方程为Y=0.260 5ρ-0.904×10-3,r=0.999 5,提取回收率大于87%,日内和日间RSD均小于7%。18例健康志愿者分别经口给予盐酸丁咯地尔的受试制剂和参比制剂300 mg后,血浆中丁咯地尔的tmax分别为(1.56±1.26)和(1.19±0.84)h,ρmax分别为(2.458±0.887)和(2.595±0.725)mg.L-1,t1/2分别为(4.88±1.25)和(4.96±1.42)h,AUC0-24分别为(16.275±5.931)和(16.040±5.831)mg.h.L-1,AUC0-∞分别为(17.110±6.521)和(17.008±6.782)mg.h.L-1。结论此法简便、快速,适用于盐酸丁咯地尔药动学研究以及临床上血浆药物浓度监测。
OBJECTIVE To establish a HPLC method for the determination of buflomil in human plasma and to study the pharmacokinetics of buflomedil hydrochloride tablets in healthy volunteers. Methods The column was Kromasil C18 (250 mm × 4.6 mm, 5 μm). The mobile phase was acetonitrile-50 mmol·L-1 ammonium dihydrogen phosphate buffer-triethylamine (25:75:0.05) 275 nm, the internal standard is urapidil. Results The linear range of buflomedil was 20μg.L-1 ~ 6.000 mg.L-1. The regression equation was Y = 0.260 5ρ-0.904 × 10-3, r = 0.999 5. The extraction recovery was more than 87% And daytime RSDs were less than 7%. Tmax of buflomedil in plasma was (1.56 ± 1.26) and (1.19 ± 0.84) h, respectively, in 18 healthy volunteers after oral administration of buflomedil hydrochloride and 300 mg of reference preparation, respectively (2.458 ± 0.887) and (2.595 ± 0.725) mg.L-1 respectively, with t1 / 2 being (4.88 ± 1.25) and (4.96 ± 1.42) h, respectively, and AUC0-24 were (16.275 ± 5.931) and ± 5.831) mg.hL-1 and AUC0-∞ (17.110 ± 6.521) and (17.008 ± 6.782) mg.hL-1, respectively. Conclusion This method is simple and rapid, suitable for buflomedil hydrochloride pharmacokinetic studies and clinical plasma drug concentration monitoring.