Tomatsu K, Ando S, Masuyoshi S, Kondo S, Hirano M, Miyaki T, Kawaguchi H
Bristol-Myers Research Institute, Ltd., Tokyo Research Center, Japan.
J Antibiot (Tokyo). 1987 Aug;40(8):1175-83. doi: 10.7164/antibiotics.40.1175.
A new semisynthetic oral cephalosporin, BMY-28100, was evaluated for in vitro and in vivo antibacterial activities in comparison with cefaclor and cephalexin. BMY-28100 showed in vitro activity 3- and 10-fold more potent than that of cefaclor against Staphylococcus aureus and Streptococcus pneumoniae, respectively. BMY-28100 was slightly better than cefaclor and about 4 times more active than cephalexin against Haemophilus influenzae and Neisseria gonorrhoeae. Escherichia coli, Klebsiella pneumoniae and Proteus mirabilis were comparably susceptible to BMY-28100 and cefaclor. The bactericidal activity of BMY-28100 against S. aureus, E. coli and P. mirabilis was equal to or twice as high as MIC value, which was similar to that of cefaclor. The stability of BMY-28100 against penicillinases was nearly comparable to that of cefaclor, whereas cefaclor was somewhat unstable to cephalosporinases. BMY-28100 was about twice as active as cefaclor against three Gram-positive bacterial infections. BMY-28100 was also more potent against infections of H. influenzae and P. mirabilis, but slightly less active against E. coli Juhl than cefaclor. Blood level parameters of BMY-28100 were significantly superior to those of cefaclor and slightly better than cephalexin in mice and rats. The urinary recovery of BMY-28100 was somewhat higher and comparable to that of cefaclor and cephalexin, respectively. BMY-28100 was more stable than cefaclor in human and calf sera at 37 degrees C.
一种新型半合成口服头孢菌素BMY - 28100，与头孢克洛和头孢氨苄相比，对其体外和体内抗菌活性进行了评估。BMY - 28100对金黄色葡萄球菌和肺炎链球菌的体外活性分别比头孢克洛强3倍和10倍。在针对流感嗜血杆菌和淋病奈瑟菌方面，BMY - 28100略优于头孢克洛，活性约为头孢氨苄的4倍。大肠杆菌、肺炎克雷伯菌和奇异变形杆菌对BMY - 28100和头孢克洛的敏感性相当。BMY - 28100对金黄色葡萄球菌、大肠杆菌和奇异变形杆菌的杀菌活性等于或高于最低抑菌浓度值的两倍，这与头孢克洛相似。BMY - 28100对青霉素酶的稳定性与头孢克洛几乎相当，而头孢克洛对头孢菌素酶有些不稳定。在针对三种革兰氏阳性菌感染方面，BMY - 28100的活性约为头孢克洛的两倍。BMY - 28100对流感嗜血杆菌和奇异变形杆菌感染也更有效，但对大肠杆菌Juhl的活性略低于头孢克洛。在小鼠和大鼠中，BMY - 28100的血药浓度参数明显优于头孢克洛，略优于头孢氨苄。BMY - 28100的尿回收率略高，分别与头孢克洛和头孢氨苄相当。在37℃下，BMY - 28100在人血清和小牛血清中比头孢克洛更稳定。
