Kisaka Y, Hiraoka H, Matsuoka T, Tanaka S, Kishida H, Aihara M, Urabe T, Fujiwara A
Jpn J Antibiot. 1985 May;38(5):1287-300.
Fundamental and clinical studies on cefminox (CMNX, MT-141), a new cephamycin antibiotic, were carried out and the results were as follows. After the intravenous one shot administration of 1 g CMNX to 17 cases, serum concentrations, tissue concentrations in pelvic organs and protein binding capacities in serum were measured. Blood concentrations ranged between 100-200 micrograms/immediately after the injection and declined gradually. Half-life (T1/2) was 75 minutes. Tissue concentrations were 30-70 micrograms/g (tissue weight) 10 minutes after injection and declined. Half-life was 90 minutes. The average serum protein binding rate was 66.3 +/- 8.4%. Correlation between tissue concentration (Y) and free serum concentration (X) was expressed as Y = 0.42 + 7.14X. Correlation coefficient (r) was 0.80 (r = 0.80). Correlation coefficient in serum concentrations between HPLC and bioassay was 0.83 and that in free concentration was 0.97. In clinical studies, CMNX was administered to 19 cases of obstetric and gynecological infections. The patients were constituted of 3 with puerperal endometritis, 3 with pyometra, 3 with pelvic peritonitis, 3 with parametritis, 3 with adnexitis, 2 with BARTHOLIN's abscess and 1 with retroperitoneal abscess and vulva abscess. Overall clinical efficacy was 89.5% (17/19). Bacteriologically 26 strains were isolated, 6 strains of E. coli, 4 strains of B. fragilis, 2 strains of P. anaerobius and P. asaccharolyticus and each one of E. faecalis, S. epidermidis, N. gonorrhoeae, S. marcescens, P. maltophilia, A. calcoaceticus, K. pneumoniae, P. mirabilis, H. influenzae, S. intermedius, E. lentum and F. varium. Twenty of these 24 strains were eliminated after the administration, K. pneumoniae was decreased, E. faecalis, S. marcescens and P. maltophilia remained unaffected. No side effects were observed but 1 case showed mild elevation of transaminases which normalized 1 week after CMNX was stopped.
对新型头孢霉素抗生素头孢米诺(CMNX,MT - 141)进行了基础和临床研究,结果如下。对17例患者静脉一次性注射1g头孢米诺后,测定了血清浓度、盆腔器官的组织浓度以及血清中的蛋白结合能力。注射后即刻血药浓度在100 - 200微克/毫升之间,并逐渐下降。半衰期(T1/2)为75分钟。注射后10分钟组织浓度为30 - 70微克/克(组织重量),随后下降。半衰期为90分钟。平均血清蛋白结合率为66.3±8.4%。组织浓度(Y)与游离血清浓度(X)之间的相关性表示为Y = 0.42 + 7.14X。相关系数(r)为0.80(r = 0.80)。高效液相色谱法与生物测定法测定的血清浓度之间的相关系数为0.83,游离浓度之间的相关系数为0.97。在临床研究中,对19例妇产科感染患者使用了头孢米诺。患者包括3例产褥期子宫内膜炎、3例积脓、3例盆腔腹膜炎、3例宫旁组织炎、3例附件炎、2例巴氏腺脓肿以及1例腹膜后脓肿和外阴脓肿。总体临床有效率为89.5%(17/19)。细菌学检查分离出26株菌株,其中大肠杆菌6株、脆弱拟杆菌4株、厌氧消化链球菌和不解糖消化链球菌各2株,粪肠球菌、表皮葡萄球菌、淋病奈瑟菌、黏质沙雷氏菌、嗜麦芽窄食单胞菌、醋酸钙不动杆菌、肺炎克雷伯菌、奇异变形杆菌、流感嗜血杆菌、中间葡萄球菌、迟缓埃格特菌和可变梭杆菌各1株。给药后这些24株菌株中有20株被清除,肺炎克雷伯菌数量减少,粪肠球菌、黏质沙雷氏菌和嗜麦芽窄食单胞菌未受影响。未观察到副作用,但有1例患者转氨酶轻度升高,在停用头孢米诺1周后恢复正常。