Hongo M, Shimizu R, Sakae K, Kohchi T, Tada K, Tani M
Jpn J Antibiot. 1986 May;39(5):1389-400.
A new carbapenem antibiotic, imipenem/cilastatin sodium (MK-0787/MK-0791), was administered by intravenous drip infusion at a dose level of 500 mg/500 mg to 30 patients who underwent total abdominal hysterectomy for uterine myomas with or without benign ovarian tumors. The uterine arteries were clamped bilaterally at 0.25, 0.5, 1, 2, 3, 4, 6 and 8 hours after administration, and plasma samples and uterine tissues were taken for measurements of MK-0787 by bioassay and MK-0791 by HPLC. The measured values were analyzed using a two-compartment open model. Maximum concentrations of MK-0787 at 0.5 hour after the start of intravenous drip infusion were 98.5 micrograms/ml in the antecubital vein, 100.1 micrograms/ml in the uterine artery, 26.5 micrograms/g in the oviduct, 21.2 micrograms/g in the ovary, 19.1 micrograms/g in the endometrium, 19.0 micrograms/g in the myometrium, 22.1 micrograms/g in the cervix uteri and 16.4 micrograms/g in the portio vaginalis. These results suggest that the penetration of MK-0787/MK-0791 into female genital tissues is good, and sufficient concentrations are obtained enough to inhibit organisms which are frequently isolated from patients with pelvic inflammatory disease.
一种新型碳青霉烯类抗生素亚胺培南/西司他丁钠(MK - 0787/MK - 0791),以500毫克/500毫克的剂量水平通过静脉滴注给药于30例因子宫肌瘤伴或不伴有良性卵巢肿瘤而接受全腹子宫切除术的患者。在给药后0.25、0.5、1、2、3、4、6和8小时双侧钳夹子宫动脉,采集血浆样本和子宫组织,通过生物测定法测定MK - 0787,通过高效液相色谱法测定MK - 0791。使用二室开放模型分析测量值。静脉滴注开始后0.5小时,MK - 0787在前臂静脉的最大浓度为98.5微克/毫升,在子宫动脉为100.1微克/毫升,在输卵管为26.5微克/克,在卵巢为21.2微克/克,在内膜为19.1微克/克,在肌层为19.0微克/克,在子宫颈为22.1微克/克,在阴道部为16.4微克/克。这些结果表明MK - 0787/MK - 0791在女性生殖组织中的渗透良好,可获得足以抑制盆腔炎患者中常见分离菌的足够浓度。