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头孢硫脒的改进制备
头孢硫脒(cefathiamidine,1),化学名为(6R，7R)-3-[(乙酰氧基)甲基]-7-[α-(N,N'-二异丙基脒硫基)乙酰胺基]-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-甲酸内铵盐,是我国首个自主研发的广谱头孢菌素,临床使用其注射制剂,对大部分革兰阳性菌和部分革兰阴性菌有效,特别对肠球菌疗效良好,血药浓度高、临床疗效好.
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苄星头孢匹林的合成
苄星头孢匹林(cefapirin benzathine,1),化学名为(6R,7R)-3-[(乙酰氧基)甲基]-8-氧代-7-[(4-吡啶基硫基)乙酰胺基]-5-硫杂-1-氮杂二环[4.2.0]辛-2-烯-2-羧酸N,N'-二苄基乙二胺(2:1),是头孢匹林的胺盐复合物,主要用作兽药,用于治疗奶牛的乳腺炎和子宫内膜炎等1,2.美国药典(USP)31版有收载.
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Objective:To determine the relationship between the application of antibiotic and the production of extended spectrum β-lactamases (ESBLs).Methods:ESBLs were detected by the double disc diffusion method among 161 gram-negative bacilli isolated from clinical specimens.The use of antibiotic in the patients was investigated before ESBLs were detected. Results:The rate of ESBLs-producing strains was 35.4% (57/161). In the patients with ESBLs-producing strains, the utilization rates of antibiotic and the third-generation cephalosprin were 96.4% (55/57) and 42.1% (24/57) respectively, which were significantly higher than those without ESBLs-producing strains [80.6% (84/104) and 16.3% (17/104), respectively].There were significant differences (P＜0.05 and P＜0.005,respectively) between the two groups of patients.The duration of the third-generation cephalosprins therapy was significantly longer in the patients with ESBLs-producing strains [(7.5 ± 5.4)d] than those without ESBLs-producing strains [(2.7±2.6)d,P＜0.05].Conclusion:The application of antibiotic, especially the third-generation cephalosprins, is the risk factor for the production of ESBLs.
