头孢克肟在正常人中的药物代谢动力学研究

PHARMACOKINETICS OF CEFIXIME IN HEALTHEALTHY VOLUNTEERS

本文报道头孢克肟在正常人中的药物代谢动力学和测定头孢克肟血浓度的高效液相色谱（ＨＰＬＣ）方法学。８位健康志愿者交叉单次空腹及进食后口胺头孢克厉２００ｍｇ后平均Ｃｍａｘ分别为２．７±０．９和１．７±０．４ｍｇ／Ｌ，平均Ｔ１／２Ｋｅ为３．７±０．４和３．３±０．７ｈ，平均ＡＵＣ为２５．４±８．５和１３．９±４．０ｈ／ｍｇ／Ｌ。２４ｈ内分别排出给药量的２３．７±７．６％和１３，６±４．５％。服药后１２ｈ的平均血药浓度分别为０．８３ｔ０．２６和０．４５±０．１８ｍｇ／Ｌ。经统计学处理（配对Ｔ检验），空腹与进食后口服头孢克肟后的Ｃｍａｘ、ＡＵＣ和２４ｈ内尿排出卒间的差异具极显著意义（Ｐ＜０．０１）。本文建立的高效液相色谱法准确性高、具重复性。以ＨＰＬＣ法测得血药浓度与微生物法测得者相符。

Pharmackjnetics of Cefixime in healthy volunteers and the high performance liquid chromatograhy method for the determination of the concentration of Cefixime in serum were described in this paper.After a single orai dose of 200mg Cefixime in 8 heaIthy volunteers both in fasting state and after meai, the mean Cmax were 2.7± 0.9 and 1.7± 0.4mg/L,the mean T1/2 Ke were 3.7± 0.4 and 3.3± 0.7h,the mean AUC were 25.4 ±8.5 and 13.9± 4.0h·mg/ L and 23.7±7.5%and 13.6± 4.5%of the drug were excreted in urine within 24h,The mean serum concentration at 12 h were 0.83± 0.26 and 0.45 ± 0.18 mg/L respectively. The difference of Cmax,AUC,and urinary excretion rates of Cefixime between volunteers in fasting state and after meal were statistically significant. The HPLC me-thod was accurate and lilghly reproducible. The drug concentratons in se-rum determined by HPLC method were hiawhly corrLnspondent with those obtained by bioassay.