国产头孢三嗪在急性感染病人中的药代动力学

PHARMACOKINETICS OF HOME-MADE CEFTRIAXONE IN PATIENTS WITH ACUTE INFECTIONS

静脉滴注国产头孢三嗪0.5～1克,治疗8例急性感染病人的药代动力学。静注后半小时用HPLC测得的平均血药浓度为100.75μg/ml,24小时的血药浓度为11.4μg/ml,国产头孢三嗪的药代动力学特点与国外同类产品基本一致。半衰期长,清除半衰期为8.8小时,可在血液和感染部位中保持较长时间的杀菌和抑菌浓度,总表观分布容积为13.0L/kg,表明药物在组织中的浓度高。本品用量小,每日1克1～2次即可达到疗效。5例慢性胆囊炎伴胆石症患者静滴头孢三嗪1克后,2小时胆汁的平均药物浓度为1022.8μg/ml,可作为治疗胆道感染的有效药物。

Pharmacokinetics of home-made ceftriaxone was studied in eight patients with acute infections. After 0.5-1g intravenous infusion in 30 minutes, the blood levels were determined by HPLC method with YWG C18 column and using CH3 OH 0.015 MTBA as mobile phase, the mean blood concentrations of home-made ceftriaxone at 0.5, 1, 2, 4, 8, 12 and 24 hr were 100.75, 94.75,, 77.2, 56.25, 43.28, 29.75 and 11.4 μg/ml, respectively. The pharmacokinetics parameters were Calculated with MCPKP pharmacokinetic PC program in a IMB PC/XT computer and the results are as follows: Kα 0.64992 h-1 T1/2α 1.06744 Vd 0.8855 L/kg Kβ 0.07854 h-1 T1/2β 8.82344 AUC270.66 mg·h·L-1 Results of this study indicated that home-made ceftriarone has the same excellent phar-mcokinetic properties similar to those of imported ceftriaxone, in terms of ligh blood levels and long t1/2. 5 patients with chronic cholecystitis and choleystolithiasis after 1 g introvenous infusion, the drug levels in the bile were determined by HPLC method. The mean bile concentration of the antibiotic at two hour were 1022.6 μg/ml.