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目的研究盐酸右美托咪定注射液在36名健康志愿者体内的药动学。方法采用平行设计,36名健康志愿者,男女各半,分3组按0.17,0.33及0.67μg·kg-1·h-1的滴速连续静脉输注右美托咪定10 h,分点采集血样,用LC-MS/MS测定受试者血浆右美托咪定浓度。结果 3个剂量组的t1/2分别为(2.77±1.85),(2.97±1.35)和(2.50±0.87)h;ρmax分别为(104.04±28.19),(289.71±94.50)和(793.57±156.74)ng·L-1;CL分别为(101.96±24.99),(69.58±18.21)和(50.21±14.28)h·L-1;Vss分别为(330.48±182.38),(294.08±136.37)和(177.33±67.94)L;AUC0-24分别为(893.29±256.48),(2 816.31±1 139.61)和(7 932.02±1 515.33)ng·h·L-1。ρmax、AUC0-24与给药剂量呈现线性依赖关系。结论中国人右美托咪定的药动学与非中国人群相比无种族差异,但个体间有差异,临床使用可参照国外用药方案,用药剂量需个体化。
Objective To study the pharmacokinetics of dexmedetomidine hydrochloride injection in 36 healthy volunteers. Methods By parallel design, 36 healthy volunteers were divided into three groups and received intravenous drip of dexmedetomidine at 0.17,0.33 and 0.67μg · kg-1 · h-1 for 10 h Blood samples were taken and plasma dexmedetomidine concentrations were determined by LC-MS / MS. Results The t1 / 2 of the three dose groups were (2.77 ± 1.85), (2.97 ± 1.35) and (2.50 ± 0.87) h, respectively; the ρmax were (104.04 ± 28.19), (289.71 ± 94.50) and (793.57 ± 156.74) ng · L-1; CL were (101.96 ± 24.99), (69.58 ± 18.21) and (50.21 ± 14.28) h · L-1; Vss were (330.48 ± 182.38), (294.08 ± 136.37) and (177.33 ± 67.94) L; AUC0-24 were (893.29 ± 256.48), (2 816.31 ± 1 139.61) and (7 932.02 ± 1 515.33) ng · h · L-1, respectively. ρmax, AUC0-24 and dose dose showed a linear dependence. Conclusion The pharmacokinetics of dexmedetomidine in Chinese has no racial difference compared with that of non-Chinese population, but there are differences among individuals. For clinical use, the dosage may need to be individualized according to the foreign drug regimen.