泰宁中亚胺培南在呼吸系统感染患者体内的药物动力学

PHARMACOKINETICS OF IMIPENEM IN PATIENTS WITH RESPIRATORY TRACT INFECTIONS

对泰宁中亚胺培南在８ 例呼吸系统感染患者体内的药物动力学特征进行了研究，其血浆浓度采用ＨＰＬＣ 测定。泰宁１ ０００ ｍ ｇ 溶于 １００ ｍ ｌ生理盐水静滴后，即刻平均血药浓度为（３８．４±１０．６）ｍ ｇ／Ｌ，５．５ ｈ 血中浓度仍达（０．４８５±０．１１３） ｍ ｇ／Ｌ，ｔ１／２β为（０．９７０±０．０４６４） ｈ，Ｃｌｓ 为（１２．９±３．０２） Ｌ／ｈ，Ｖｃ 为（６．４９±１．８５） Ｌ，ＡＵＣ为（４４．９±１０．９） ｍ ｇ·ｈ／Ｌ。

Imipenem, a stable derivative of thienamycin, is a carbapenem antibiotic with a broad antibacterial spectrum. The pharmacokinetics of imipenem was studied in eight patients with respiratory tract infections. Hepatic and renal functions were normal in these patients. The concentration of imipenem in human plasma was detected by HPLC. The drug containing 500 mg of imipenem and 500 mg of cilastatin, which was dissolved in 100 ml of normal saline, was given to each patient by iv infusion at 30 min. The kinetics of this drug fit a two compartment model. The mean peak plasma level was (38.4±10.6) mg/L. The plasma level at 5.5 h after infusion was (0.485±0.113) mg/L. Pharmacokinetic parameters of imipenem in patients, plasma half life of elimination (t 1/2β ),volume of appearance distribution ( V c ), serum clearance (Cls) and area under curve AUC o→∞ were (0.970±0.0464) h, (6.49±1.85) h, (12.9±3.02) L/h and (44.9±10.9) mg·h/L, respectively.