HPLC检测人血浆头孢丙烯及其药动学研究

Determination of Cefprozil by HPLC in Human Plasma and Its Pharmacokinetics

关键词:  头孢丙烯  药动学  高效液相色谱法

Key words:  cefprozil  pharmacokinetics  HPLC

摘要:

目的 建立人血浆头孢丙烯检测的高效液相色谱方法，研究头孢丙烯分散片的人体药动学。方法 血浆经高氯酸沉淀，采用ZORBAX Eclipse XDB-C₈色谱柱；流动相为乙腈-0.1%三氟乙酸-水(15∶40∶45)，流速为1.0 mL·min^-1；检测波长282 nm。10名健康志愿者单剂量口服500 mg头孢丙烯分散片后，不同时间点抽取静脉血。用该方法检测血浆中头孢丙烯浓度，用DAS程序计算药动学参数。结果 头孢丙烯浓度在0.10~20.00 mg·L^-1内线性关系良好(r=0.999 9)；高、中、低3个浓度的相对回收率分别为(99.20±4.41)%，(98.07±3.94)%和(100.07±1.69)%；日内RSD分别为5.28%，5.19%和1.97%，日间RSD分别为4.38%，3.95%和1.33%。头孢丙烯在人体内符合一级吸收的一室模型，C_max为(8.79±1.09)mg·L^-1，t_1/2(ke)为(1.06±0.29) h。结论 本方法简便、快速、准确可靠，可满足药动学研究的要求。

Abstract:

OBJECTIVE To develop a high performance liquid chromatography method for the determination of cefprozil in human plasma and to study its pharmacokinetics. METHODS The human plasma samples were precipitated by perchloric acid. The analytical column was ZORBAX Eclipse XDB-C₈. The mobile phase was acetonitrile-0.1% trifluoroacetic acid-water(15∶40∶45) and the flow rate was 1.0 mL·min^-1. The UV detection wavelength was 282 nm. RESULTS Excellent liner relationship was obtained in the range of 0.10-20.00 mg·L^-1(r=0.999 9). The relative recoveries were (99.20±4.41)%, (98.07±3.94)%, and (100.07±1.69)% respectively at three concentrations. The intra-day RSD were 5.28%, 5.19%, and 1.97% and inter-day RSD were 4.38%, 3.95%, and 1.33% respectively. Cefprozil was fit to the one-compartment model with first absorption, C_max was (8.79±1.09)mg·L^-1, t_1/2(ke) was (1.06±0.29) h. CONCLUSION The method was simple, rapid, and accurate. It can be used to determine the cefprozil concentration in human plasma and to study of its pharmacokinetics.