Fraschini F, Scaglione F, Bichisao E, Marchi E, Scarpazza G, Scarpazza P, Gaffuri Riva V
Institute of Pharmacology and Chemotherapy, Milan, Italy.
Int J Clin Pharmacol Ther Toxicol. 1987 Nov;25(11):638-42.
In order to assess pharmacokinetic differences between sulbenicillin (S) and piperacillin (P), two penicillin derivatives, 24 in-patients, 12 males and 12 females mean age 59.4 years, suffering from recurrent bronchial infections were enrolled. Patients were randomly allocated to S (12 patients) and to P (12 patients) and were given 2 g i.m. every 12 h of the awarded antibiotic, for a 7-day period. At the first and 7th day blood samples (0.25, 0.5, 1, 2, 4, 6, 8 and 12 h after dosing) as well as sputum samples (1, 2, 4, 8, 12 h after dosing) and urine samples (3, 6, 9 and 12 h after dosing) were collected, and the levels of S or P were determined by bacillus subtilis test. The pharmacokinetic analysis was performed by a standard program. On day 1 and 7 the mean peak serum concentration occurred at the first hour for S (39.9 +/- 5.2; 40.9 +/- 5.1 mcg/ml, respectively) and for P (32.2 +/- 5.4; 33.1 +/- 5.4 mcg/ml, respectively). Serum AUC0-12 and AUC0-00 (mg/l.h) levels of S were significantly higher (p less than 0.01 or less) than those of P on day 1 and 7. Similarly MRT (8 h) and Cmax (mg/l) where higher but only on day 7. Sputum AUC0-12 (mg/l.h) level of S was significantly higher (p less than 0.05) than that of P on day 1 and 7. In conclusion serum and sputum S appear to have a different pharmacokinetic profile in respect to P. However, when compared to the AUC, both drugs reach antibacterial levels.
为了评估两种青霉素衍生物磺苄西林（S）和哌拉西林（P）之间的药代动力学差异，招募了24名患有复发性支气管感染的住院患者，其中男性12名，女性12名，平均年龄59.4岁。患者被随机分为S组（12例患者）和P组（12例患者），并给予指定抗生素2g，每12小时肌肉注射一次，持续7天。在第1天和第7天，采集血样（给药后0.25、0.5、1、2、4、6、8和12小时）、痰样（给药后1、2、4、8、12小时）和尿样（给药后3、6、9和12小时），并通过枯草芽孢杆菌试验测定S或P的水平。药代动力学分析通过标准程序进行。在第1天和第7天，S的平均血清峰浓度在第1小时出现（分别为39.9±5.2；40.9±5.1μg/ml），P的平均血清峰浓度在第1小时出现（分别为32.2±5.4；33.1±5.4μg/ml）。在第1天和第7天，S的血清AUC0-12和AUC0-∞（mg/l·h）水平显著高于P（p<0.01或更低）。同样，MRT（8小时）和Cmax（mg/l）更高，但仅在第7天。在第1天和第7天，S的痰AUC0-12（mg/l·h）水平显著高于P（p<0.05）。总之，与P相比，血清和痰液中的S似乎具有不同的药代动力学特征。然而，与AUC相比，两种药物均达到抗菌水平。
