Hongo M, Shimizu R, Hayashi S, Shirakawa N, Yoshinouchi M, Ando M
Jpn J Antibiot. 1983 May;36(5):1033-40.
One gram of T-1982 (cefbuperazone), a new cephamycin antibiotic, was given intravenously to a total of 28 patients prior to abdominal total hysterectomy for uterine myoma or benign ovarian tumor. Bilateral uterine arteries were clamped at 0.25, 0.5, 1, 2, 4 hours or 6 hours after administration, and serum samples and uterine tissues were taken for the measurement of T-1982 concentration by bioassay method. A little difference was found in the serum concentration between cubital venous and uterine arterial serum, the half lives being 1.88 hours and 1.74 hours, respectively. The initial concentrations were estimated to be 99.9 micrograms/ml and 103.2 micrograms/ml, respectively. The peak concentrations were obtained at 30 minutes in the endometrium, myometrium, oviduct and ovary, and at 1 hour in the cervix uteri and portio vaginalis. These were 45.2 micrograms/g, 22.4 micrograms/g, 36.1 micrograms/g, 19.9 micrograms/g, 27.6 micrograms/g and 23.4 micrograms/g, respectively. The tissue concentrations thereafter decreased in the same manner as the serum concentrations. Judging from its favorable transfer into the uterine tissues and MICs against clinical isolates often seen in the field of obstetrics and gynecology, T-1982 was evaluated to be clinically useful in the treatment of obstetrical and gynecological infections.
在28例因子宫肌瘤或良性卵巢肿瘤行腹部全子宫切除术的患者中,于术前静脉注射1克新型头孢霉素类抗生素T - 1982(头孢布宗)。给药后0.25、0.5、1、2、4小时或6小时钳夹双侧子宫动脉,采集血清样本和子宫组织,采用生物测定法测定T - 1982浓度。发现肘静脉血清和子宫动脉血清中的浓度略有差异,半衰期分别为1.88小时和1.74小时。初始浓度估计分别为99.9微克/毫升和103.2微克/毫升。子宫内膜、肌层、输卵管和卵巢在30分钟时达到峰值浓度,子宫颈和阴道部在1小时时达到峰值浓度。这些峰值浓度分别为45.2微克/克、22.4微克/克、36.1微克/克、19.9微克/克、27.6微克/克和23.4微克/克。此后组织浓度与血清浓度以相同方式下降。从其向子宫组织的良好转运以及对妇产科常见临床分离株的最低抑菌浓度来看,T - 1982被评估在治疗妇产科感染方面具有临床实用性。