Hongo M, Shimizu R, Sakae K, Hayashi S, Yoshinouchi M, Mitsui Y
Jpn J Antibiot. 1984 Dec;37(12):2391-6.
One gram of ceftriaxone (Ro 13-9904, CTRX), a new cephalosporin antibiotic, was given intravenously to a total of 25 patients prior to abdominal total hysterectomy for uterine myoma with or without small benign ovarian tumor. Bilateral uterine arteries were clamped at 0.5, 1, 2, 6, 12 and 24 hours after administration, and serum samples and uterine tissues were taken for the measurement of CTRX concentration by bioassay method. A little difference was found in the serum concentration between cubital venous and uterine arterial serum, the half-lives being 8.0 and 7.9 hours, respectively. The initial concentrations were estimated to be 153 micrograms/ml and 160 micrograms/ml, respectively. The tissue peak concentrations were obtained at 30 minutes in the myometrium, portio vaginalis, oviduct and ovary, and at 1 hour in the endometrium and cervix uteri. These were 41, 51, 51, 39, 42 and 47 micrograms/g, respectively. The tissue concentrations after peak decreased in the same manner as the serum concentrations. Judging from its favorable transfer into the uterine tissues, CTRX was evaluated to be clinically useful in the treatment of obstetrical and gynecological infections.
在25例因子宫肌瘤合并或不合并小的良性卵巢肿瘤而接受腹式全子宫切除术的患者中，于手术前静脉注射了1克头孢曲松（Ro 13-9904，CTRX），这是一种新型头孢菌素抗生素。给药后0.5、1、2、6、12和24小时钳夹双侧子宫动脉，并采集血清样本和子宫组织，采用生物测定法测定CTRX浓度。发现肘静脉血清和子宫动脉血清中的血清浓度存在微小差异，半衰期分别为8.0小时和7.9小时。初始浓度估计分别为153微克/毫升和160微克/毫升。子宫肌层、阴道部、输卵管和卵巢在30分钟时达到组织峰值浓度，子宫内膜和子宫颈在1小时时达到组织峰值浓度。这些浓度分别为41、51、51、39、42和47微克/克。峰值后的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来看，CTRX被评估为在治疗妇产科感染方面具有临床实用性。
