共查询到18条相似文献,搜索用时 115 毫秒
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通过正交实验,确定反应时间、反应温度、碱量和促进剂的量,并选择适宜条件进行验证实验.改进后提高了头孢克肟侧链活性酯的质量和收率,达到了正交优化实验目的. 相似文献
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头孢克肟 总被引:4,自引:0,他引:4
于守凡 《国外医药(抗生素分册)》1995,16(5):339-343,351
头孢克肟(cefixime,FR 17027,FK 027,CL 284635)是口服半合成第三代头孢菌素。化学名为[6R-[6α,7β(Z)]]-7-[[(2-氨基-4-噻唑基)[(羧甲氧基)亚氨基]乙酰]氨基]-3-乙烯-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸。化学结构见图1。 相似文献
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头孢泊肟酯与头孢克肟治疗急性细菌性感染随机对照研究 总被引:3,自引:0,他引:3
目的比较头孢泊肟酯与头孢克肟治疗急性细菌性感染的安全性、有效性。方法采用随机对照研究方法,以头孢克肟为对照,入选细菌感染性疾病115例,其中头孢泊肟酯试验组60例,头孢克肟对照组55例,2组的用量,用法试验组为100 m g,po,b id,对照组为200m g,po,b id,疗程均为7~12d。结果2组临床总痊愈率分别为73%和69%,总有效率分别为92%和91%,细菌清除率分别为98%和94%,不良反应率分别为7%和6%,经统计学处理均无显著差异(P>0.05)。结论头孢泊肟酯治疗急性细菌性感染临床安全,有效。 相似文献
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头孢克肟临床疗效观察李萍,王世祥,刘皋林,朱彩娟上海长海医院200433上海长征医院200003头孢克肟(cefixime,CFIX)又称世福素(Cefspan),是第三代口服头孢菌素。由日本藤泽制药有限公司研制开发。其抗菌谱广,杀菌作用强。消除半衰... 相似文献
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目的 研究头孢克肟及其关键中间体7-AVCA的合成工艺,以酶解法替代传统化学裂解法.方法 经工艺考察及改进,最终确定以GCLE为起始原料,经关键中间体7-AVCA制备头孢克肟适合于生产的工艺.结果 所制得的头孢克肟质量好,总收率为64%.其中采用的酶解法工艺不仅解决了环保治理的瓶颈问题,同时改进工艺获得的中间体7-AVCA的质最明显优于其他方法,优质的7-AVCA从源头上起到提高下游原料药头孢克肟产品的含量及稳定性,降低杂质的作用.头孢克肟的结构经1H-NMR、IR和UV分析确证,色谱纯度经HPLC检测大于99%.结论 本文工艺与文献相比,操作简化,收率提高,产品质量优异,节能环保,适合于产业化. 相似文献
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目的建立头孢克肟颗粒中主药溶出度的测定方法。方法采用紫外分光光度法.在288nm波长处测定头抱克肟颗粒中主药的吸收度。并计算回收率和溶出度。结果头抱克肟检测浓度线性范围为2.67~21.36μg·mL^-1(r=0.9990);平均回收率为99.9%(RSD=0.70%,n=9);3批样品在45min溶出量均在75%以上。结论本方法准确、可靠。可用于该制剂的溶出度测定。 相似文献
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目的:比较头孢克肟片和头孢克肟胶囊(世福素)的生物利用度和生物等效性。方法:20名健康志愿受试者随机交叉单剂口服头孢克肟片和胶囊各200mg,采用以头孢拉定作内标的高效液相色谱法测定头孢克肟血药浓度,以3p97程序计算两制剂的药物动力学参数和生物利用度。结果:建立的高效液相色谱法,以头孢拉定作内标,测定头孢克肟血浆药物浓度,检测限为1ng(S/N>3),线性范围为0.1-5.0μg·mL-1(r=0.9993,n=5)。0.25、1.0及2.5μg·mL-1三种浓度的回收率分别为(96.0±5.7)、(94.0±2.8)及(100.0±3.4)%,其平均回收率为(96.67±3.06)%,RSD为3.17%;日内误差分别为4.2、3.2及3.6%;日间误差分别为7.4、2.2及3.7%。头孢克肟片和胶囊的人体内血药浓度-时间曲线符合口服一室模型,主要动力学参数:T1/2Ke分别为(4.98±0.58)和(5.28±0.77)h;Tmax分别为(4.7±0.6)和(4.6±0.9)h;Cmax分别为(3.38±0.9)和(3.29±0.87)μg·mL-1;AUC0-24分别为(30.72±7.56)和(30.60±7.92)h·(μg·mL)-1。相对生物利用度为(102.8±19.7)%。结论:头孢克肟片与胶囊(世福素)具有生物等效性。 相似文献
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H Mikawa M Mayumi Y Akiyama S Ito Y Watanabe H Kanaoka S Takeshita Y Takahashi F Akiyama T Yoshimura 《The Japanese journal of antibiotics》1989,42(12):2527-2539
Clinical usefulness of cefixime (CFIX), a new oral cephalosporin antibiotic, in pediatric field was investigated. The results obtained were summarized as follows. 1. The clinical efficacy of CFIX was investigated in a total of 138 children including 49 with upper respiratory tract infections (RTI), 22 with acute bronchitis, 18 with pneumonia, 19 with scarlet fever and 21 with urinary tract infections (UTI). 2. Clinical effectiveness was excellent in 58, good in 60, fair in 14 and poor in 3, with an overall efficacy rate of 87.4%. The efficacy rate classified according to types of infection were 85.7% in upper RTI, 89.5% in acute bronchitis, 94.4% in pneumonia, 78.9% in scarlet fever, and 90.5% in UTI. 3. Out of the suspected causative organisms, 43 strains of a total of 50 strains isolated were eradicated. The bacteriological eradication rate was 86.0%. (Haemophilus influenzae 100%, Haemophilus parainfluenzae 100%, Streptococcus pyogenes 88.5%, Escherichia coli 85.7%). 4. One hundred forty four children were analyzed for side effect. Side effects were observed in 2 children (1.4%) with diarrhea in 1 and anorexia in another. Abnormal laboratory test results were recorded in 4 children (3.3%). The above results suggest that CFIX is a very useful new oral cephalosporin for the treatment of bacterial infections in children. 相似文献
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T Hosoda M Masuda M Miyao H Mimoto S Endo Y Yuasa H Tanaka 《The Japanese journal of antibiotics》1986,39(4):1149-1156
A clinical study of cefixime (CFIX), a new oral cephalosporin, was carried out to evaluate its therapeutic effectiveness on bacterial infections in children. CFIX was orally administered to 13 patients including 6 with upper respiratory tract infection (RTI), 3 with pneumonia, and 1 each with bronchitis, otitis media, skin abscess, and urinary tract infection (UTI). The daily dosage per kg bodyweight ranged from 5.1 to 17.4 mg (average: 8.7 mg), and was given in 2 or 3 divided doses per day for 3 to 10 days (average: 5.8 days). The clinical response was excellent in 4 (30.8%), good in 7 (53.8%) and poor in 2 (15.4%), with an overall efficacy rate of 84.6%. Bacteriological efficacy was good, and 6 of the 8 identified causative organisms were eradicated. Side effects were observed in 3 children, i.e., loose stool in 1 and transient elevations of GOT and GPT in 2. The above results suggest that CFIX is a useful new oral cephalosporin for the treatment of bacterial infections in children. 相似文献
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The absorption and excretion and clinical effectiveness of cefixime (CFIX) granules, a new oral cephalosporin, were studied with pediatric patients with tonsillitis and urinary tract infection (UTI). Peak serum concentrations in 3 children given orally a single dose of 3 mg/kg on fasting were 0.545 micrograms/ml at 2 hours in 1 patient, and 1.56 and 1.26 micrograms/ml at 4 hours in the other 2. The half-lives in the 3 patients were 3.21-3.42 hours, with an average of 3.29 hours. The urinary concentration during the first 6 hours was 36.5 micrograms/ml in 1 patient showing the low serum level, and the first 6-hour urinary recovery rate was 7.3%. In the other 2 patients, urinary concentrations and recovery rates up to 6 hours were 87 and 62 micrograms/ml, and 17.0 and 15.1%, respectively. The second 6-hour urinary concentrations and recovery rates were 35.5 and 20.8 micrograms/ml, and 12.7 and 8.8%, respectively. The urinary recovery rates up to 12 hours were 29.7 and 23.9%, respectively. CFIX was given orally to 19 children with 20 diseases in daily doses of 6.4-12.9 mg/kg in 2 or 3 divided portions for 3 to 12 days. Clinical evaluations were made on 18 diseases. Clinical effects of CFIX were excellent in 4, good in 7 and poor in 1 of the 12 patients with tonsillitis, and excellent in 5 and good in 1 of the 6 patients with UTI. The overall clinical effectiveness rate was 94.4%. No side effects were observed in any of the 19 patients. Hematological tests, showed slight elevation of blood platelet counts in 2 patients.(ABSTRACT TRUNCATED AT 250 WORDS) 相似文献
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S Nakashima F Hayakawa T Nakashima Y Miyachi S Hakamada K Kuno 《The Japanese journal of antibiotics》1986,39(4):1076-1086
Fundamental and clinical studies on cefixime (CFIX), a new oral cephem antibiotic, were carried out in the pediatric field. The results were as follows: Serum concentrations and urinary recovery rates were determined after oral administration of CFIX at doses of 3 mg/kg and 6 mg/kg in 2 cases each (4 cases in total). The mean serum concentrations of CFIX were 0.52 and 0.58 micrograms/ml at 2 hours, 0.80 and 1.42 micrograms/ml at 4 hours, 0.73 and 1.36 micrograms/ml at 6 hours, 0.54 and 1.12 micrograms/ml at 8 hours, respectively. The mean peak serum concentration of CFIX was obtained at 4 hours after administration, with serum half-lives (T1/2) of 3.77 and 5.30 hours, respectively. The mean cumulative urinary recovery rates within 12 hours after administration of CFIX at doses of 3 mg/kg and 6 mg/kg were 8.4% and 6.8%, respectively. Antibacterial activities of CFIX against clinically isolated strains of S. pyogenes, S. pneumoniae. E. faecalis, S. aureus, E. coli, H. influenzae, H. parainfluenzae were compared with those of amoxicillin (AMPC), cefaclor (CCL), and cephalexin (CEX). It was observed that CFIX was a little less active than AMPC against S. pyogenes and S. pneumoniae, but CFIX was more active than CCL and CEX. CFIX was the most active against E. coli, H. influenzae and H. parainfluenzae. Twenty-one pediatric patients with bacterial infections (10, tonsillitis; 4, pharyngitis; and 7, urinary tract infections) were treated with CFIX at doses of 1.5-6.0 mg/kg in 2 or 3 times daily for 4-10 days. The efficacy rate was 95.2% clinically and 91.3% bacteriologically. No adverse reactions were observed. An abnormal laboratory finding (slight elevation of S-GOT and S-GPT) was observed in 1 case. 相似文献