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Influence of storage and susceptibility test conditions on stability and activity of LY163892 and four other cephalosporins.

机译:贮藏和药敏试验条件对LY163892和其他四种头孢菌素的稳定性和活性的影响。

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摘要

A new carbacephem analog of cefaclor, LY163892, was examined along with four other cephalosporins for chemical stability and for antibacterial activity under a variety of susceptibility test conditions. LY163892 was found to be markedly more stable than cefaclor during storage at 4 and 35 degrees C in human serum, human urine, and various bacteriological media. Under these conditions, LY163892 demonstrated stability equal or superior to the stabilities of cephalexin, cephalothin, and cefuroxime. Broth and agar dilution susceptibility tests did not reveal significant differences in LY163892 activity in a variety of test media, although LY163892 MICs were somewhat higher in Mueller-Hinton chocolate agar or Trypticase soy broth (BBL Microbiology Systems, Cockeysville, Md.) than in other media. The activity of LY163892 against selected pathogens was only slightly influenced by the increased or decreased pH of the test medium, in a manner similar to that of the other cephalosporins tested. Thus, the carbacephem structure of LY163892 appears to represent a more stable cephalosporin than cefaclor, while retaining a similar antimicrobial spectrum.
机译:在各种药敏试验条件下,检查了头孢克洛的一种新的头孢克洛姆类似物LY163892和其他四种头孢菌素的化学稳定性和抗菌活性。发现LY163892在人血清,人尿和各种细菌培养基中于4和35摄氏度下储存期间比头孢克洛更加稳定。在这些条件下,LY163892表现出的稳定性等于或优于头孢氨苄,头孢氨苄和头孢呋辛的稳定性。尽管在Mueller-Hinton巧克力琼脂或Trypticase大豆肉汤(BBL Microbiology Systems,Cockeysville,MD)中,LY163892 MICs较高,但肉汤和琼脂稀释敏感性测试并未显示在各种测试培养基中LY163892活性的显着差异。媒体。 LY163892对所选病原体的活性仅受测试培养基pH值升高或降低的影响很小,其作用方式与所测试的其他头孢菌素相似。因此,LY163892的羧苄基乙酰胺结构似乎代表了比头孢克洛更稳定的头孢菌素,同时保留了相似的抗菌谱。

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