摘要
目的建立人血浆比阿培南（biapenem）浓度的反相高效液相色谱测定法（HPLC）。研究健康受试者单剂量和多剂量注射国产比阿培南后的人体药动学。方法11名健康志愿者分别接受比阿培南注射液静脉滴注300mg单次和多次，应用反相高效液相色谱法测定血药浓度，计算药动学参数。结果血浆中比阿培南浓度分别在0．5～10μg／ml浓度范围内呈良好的线性关系，日内、日间变异系数及回收率均达到临床药动学研究的要求。受试者静注比阿培南单剂和多剂后体内过程均符合二房室模型，主要药动学参数cmax分别为（16．64±3．32）和（17．01±3．92）mg／L；平均AUC（n-∞）（27．28±8．94）和（26．85±7．46）[mg／（L·h），平均血浆消除半衰期t1／2β分别为（1．17±0．69）和（0．85±0．14）h。结论国产注射用比阿培南在健康人体内的药动学符合二房室模型特征；多次给药体内无蓄积作用。
Objective To establish a HPLC method for determination of biapenem in human plasma and study the pharmaeokinetics of parenteral biapenem in Chinese healthy volunteers. Methods The pharmacokinetics of a parenteral carbapenem antibiotic, biapenem, was studied in 11 healthy volunteers, following single intravenous dose and multiple doses （300mg）. The drug concentrations in serum samples were assayed by high performance chromatography. The pharmacokinetic parameters were calculated by DAS2.0 Software. Results Serum concentrations ranged from 0.5 to 10mg/L were found in well linearity. The precisions of within-days and the recovery rate were all coincided with the study on the clinical pharmacokinetics. The pharmacokinetics of biapenem was fitted in a two-compartment open model, the mean peak concentrations （cmax） in serum was （16. 64±3. 32）, （17. 01±3.92）mg/L; the area under the concentration-timecurve （AUC） was （27. 28±8.94）, （26. 85±7.46） [mg/（L·h）]; and the elimination half-life （t1/2β） being （1. 17±0.69）, （0.85 ± 0. 13） h, respectively. Conclusion The pharmacokinetics of biapenem was fitted in a two-compartment open model and there was no accumulation after a multiple intravenous dose of biapenem in six days.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
2008年第12期717-720,共4页
Chinese Journal of Antibiotics
