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目的:对单剂量美罗培南静脉制剂在健康受试者体内的药代动力学过程进行分析与研究。方法:选取健康受试者15名,对受试者随机分组交叉注射美罗培南静脉制剂,静滴给药100、300、500mg。在受试者静脉给药后每隔0.5小时取患者血样,每隔2、4、6、12小时取患者尿液。利用高效液相色谱仪对患者血液中以及尿液中的药物浓度进行测定。用药代学公式对实验测定的血药浓度和尿药浓度进行药物代谢分析。对于美罗培南静脉制剂在体内的药代动力学过程进行研究。结果:15例健康受试者在接受药物注射后的血药浓度分别为(7.14±1.76)mg/L、(19.45±3.02)mg/L、(40.37±3.17)mg/L。半衰期分别为(1.71±0.46)h、(1.53±0.32)mg/L、(1.29±0.05)mg/L。AUC分别是(15.68±5.48)mg·h/L、(35.65±4.78)mg·h/L、(67.84±9.58)mg·h/L。记录每个时间段的尿药排泄率分别为31.8%、30.4%、33.6%。结论:美罗培南注射后再人体内由肾脏排泄,不随着给药量的增多而增加血药浓度,不存在体内累积的现象,会随着时间逐渐被肾脏代谢。
OBJECTIVE: To analyze and study the pharmacokinetics of single-dose meropenem intravenous preparations in healthy volunteers. Methods: Fifteen healthy subjects were selected. Subjects were randomized to receive intravenous injection of meropenem intravenously at 100, 300 and 500 mg. Patient blood samples were taken every 0.5 hours after intravenous administration of the subject and patient urine was taken every 2, 4, 6, 12 hours. The concentration of the drug in the blood and in the urine of the patient was measured using a high-performance liquid chromatograph. Pharmacokinetic formula on the experimental determination of plasma concentration and urinary drug concentration for drug metabolism analysis. In vivo pharmacokinetic studies of meropenem intravenous formulations were performed. Results: The plasma concentrations of 15 healthy subjects after receiving drug injection were (7.14 ± 1.76) mg / L, (19.45 ± 3.02) mg / L and (40.37 ± 3.17) mg / L, respectively. The half-lives were (1.71 ± 0.46) h, (1.53 ± 0.32) mg / L and (1.29 ± 0.05) mg / L, respectively. AUC were (15.68 ± 5.48) mg · h / L, (35.65 ± 4.78) mg · h / L and (67.84 ± 9.58) mg · h / L, respectively. Record urinary excretion rate of each time period were 31.8%, 30.4%, 33.6%. CONCLUSION: Meropenem is excreted by the kidneys after injection, and does not increase the plasma concentration with the increase of the dose. There is no phenomenon of accumulation in the body, which is gradually metabolized by the kidneys over time.