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目的对国产赖脯胰岛素注射液和进口赖脯胰岛素注射液(优泌乐)进行药动学和生物等效性研究。方法 Beagle犬头颈部皮下注射交叉给予1 IU/kg单一剂量受试制剂和参比制剂,于给药后0、2、5、10、20、30、45、60、90、120、180和240 min股静脉取血,全自动免疫分析仪检测血清中药物浓度,绘制药-时曲线。将数据经DAS 2.0软件计算药动学参数并进行生物等效性评价。结果赖脯胰岛素受试制剂和参比制剂的药动学参数分别如下:C max(932.0±358.2)和(1 070.2±335.6)μIU/ml,t max(24.0±5.2)和(21.5±12.7)min,t1/2(51.9±28.4)和(66.6±20.7)min,AUC(0-t)为(84 833.2±10 512.9)和(98506.4±31 324.3)μIU·ml-1·min,AUC(0-∞)为(90 438.3±10 492.9)和(107 900.2±34 465.1)μIU·ml-1·min。以AUC(0-∞)计算,受试制剂对参比制剂的相对生物利用度为(93.4±35.9)%。结论 Beagle犬头颈部皮下注射给予1 IU/kg单一剂量受试制剂和参比制剂的体内药动学行为具有生物等效性。
Objective To study the pharmacokinetics and bioequivalence of domestic insulin lispro and insulin lispro injection. Methods Beagle dogs were injected subcutaneously with head and neck subcutaneously with 1 IU / kg single dose of the test preparation and reference preparation, and after 0,2,5,10,20,30,45,60,90,120,180 and 240 min femoral vein blood, automatic immune analyzer to detect serum drug concentration, draw the drug - time curve. Pharmacokinetic parameters were calculated and bioequivalence assessed using DAS 2.0 software. Results The pharmacokinetic parameters of the insulin lispro test and reference preparations were as follows: C max (932.0 ± 358.2) and (1 070.2 ± 335.6) μIU / ml, t max (24.0 ± 5.2) and (21.5 ± 12.7) AUC (0-t) were (84 833.2 ± 10 512.9) and (98506.4 ± 31 324.3) μIU · ml-1 · min, respectively -∞) were (90 438.3 ± 10 492.9) and (107 900.2 ± 34 465.1) μIU · ml-1 · min. The relative bioavailability of the test formulation to the reference formulation was (93.4 ± 35.9)% based on AUC (0-∞). Conclusions The in vivo pharmacokinetic behavior of Beagle dogs given subcutaneously with 1 IU / kg single dose of test formulation and reference formulation was bioequivalent.