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目的:研究注射用奥美拉唑在大鼠失血模型体内的药动学变化。方法:32只大鼠随机分为4组,分别为空白对照组(A组)、失血10%组(B组)、失血20%组(C组)和失血30%组(D组),每组8只。大鼠失血模型建立后,对照组和失血组分别尾静脉注射奥美拉唑(10 mg·kg-1),采用高效液相色谱法分析测定奥美拉唑的血浆浓度,利用DAS ver 2.0程序计算其药动学参数。结果:B组与对照组相比,药时曲线下面积(AUC0-t,AUC0-∞)、平均滞留时间(MRT0-t,MRT0-∞)、半衰期(t1/2)、清除率(CL)、表观分布容积(V)各药动学参数差异均无显著性(P>0.05);C组与对照组相比,MRT0-t、MRT0-∞、t1/2均延长(P<0.01),其余参数差异无显著性(P>0.05);D组与对照组相比,MRT0-t、MRT0-∞、t1/2均延长(P<0.01),且V增大(P<0.01),其余参数差异无显著性(P>0.05)。结论:当机体失血20%以上时,可能需要调整注射用奥美拉唑的给药方案,以确保用药的安全性和有效性。
Objective: To study the pharmacokinetics of omeprazole for injection in rat model of blood loss. Methods: Thirty-two rats were randomly divided into 4 groups: control group (A), blood loss 10% (B), blood loss 20% (C) and blood loss 30% Group of eight. After establishment of the model of blood loss in rats, omeprazole (10 mg · kg -1) was injected into the caudal vein of the control group and the blood loss group respectively. The plasma concentration of omeprazole was determined by high performance liquid chromatography (HPLC) Calculate its pharmacokinetic parameters. Results: The area under the curve (AUC0-t, AUC0-∞), mean retention time (MRT0-t, MRT0-∞), half-life (t1 / 2), clearance (CL) (P> 0.05). Compared with the control group, the MRT0-t, MRT0-∞ and t1 / 2 in group C were longer than those in control group (P <0.01) (P <0.05). The MRT0-t, MRT0-∞ and t1 / 2 in group D were longer than those in control group (P <0.01) There was no significant difference in other parameters (P> 0.05). Conclusion: When the body blood loss more than 20%, may need to adjust the injection of omeprazole dosing regimen to ensure the safety and effectiveness of medication.