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新型广谱头孢菌素SCE - 963在小鼠、大鼠、兔子和狗体内的吸收、分布及排泄情况。

Absorption, distribution and excretion of SCE-963, a new broad-spectrum cephalosporin, in mice, rats, rabbits and dogs.

作者信息

Tsuchiya K, Kondo M, Kita Y, Noji Y, Takeuchi M, Fugono T

出版信息

J Antibiot (Tokyo). 1978 Dec;31(12):1272-82. doi: 10.7164/antibiotics.31.1272.

DOI:10.7164/antibiotics.31.1272
PMID:738967
Abstract

A single dose of 20 mg/kg of SCE-963 [7beta-]2-(aminothiazol-4-yl)acetamido]-3-[[[1-(2-dimethylaminoethyl)-1H-tetrazol-5-yl]thio]methyl]ceph-3-em-4-carboxylic acid] was administered subcutaneously to mice, intramuscularly to rats, rabbits and dogs. Plasma and tissue levels of SCE-963 reached a peak in 15 approximately 30 minutes after administration. In mice, rats and dogs, SCE-963 was distributed at high concentration in the descending order in the kidney, liver, plasma, lung and spleen, and in rabbits, in the kidney, plasma, lung, liver and spleen. The SCE-963 levels in the liver of mice, rats and dogs were higher than those of cefazolin, cephaloridine and cephalothin. The plasma and tissue levels of SCE-963 in mice and rats diminished rapidly, but those in rabbits and dogs declined gradually. SCE-963 was mainly excreted in the urine. The rate of excretion of SCE-963 in the bile was two to three times higher than that of cefazolin.

摘要

以20毫克/千克的剂量给小鼠皮下注射SCE - 963[7β - [2 -(氨基噻唑 - 4 - 基)乙酰胺基]-3 - [[[1 -(2 - 二甲基氨基乙基)-1H - 四氮唑 - 5 - 基]硫代]甲基]头孢 - 3 - 烯 - 4 - 羧酸],给大鼠、兔子和狗肌肉注射。给药后约15至30分钟,SCE - 963的血浆和组织水平达到峰值。在小鼠、大鼠和狗中,SCE - 963在肾脏、肝脏、血浆、肺和脾脏中的分布浓度由高到低,在兔子中,分布顺序为肾脏、血浆、肺、肝脏和脾脏。小鼠、大鼠和狗肝脏中的SCE - 963水平高于头孢唑林、头孢噻啶和头孢噻吩。小鼠和大鼠体内SCE - 963的血浆和组织水平迅速下降,但兔子和狗体内的水平则逐渐下降。SCE - 963主要经尿液排泄。SCE - 963在胆汁中的排泄率比头孢唑林高两到三倍。

相似文献

1
Absorption, distribution and excretion of SCE-963, a new broad-spectrum cephalosporin, in mice, rats, rabbits and dogs.新型广谱头孢菌素SCE - 963在小鼠、大鼠、兔子和狗体内的吸收、分布及排泄情况。
J Antibiot (Tokyo). 1978 Dec;31(12):1272-82. doi: 10.7164/antibiotics.31.1272.
2
Absorption, distribution and excretion of cefmenoxime (SCE-1365), a novel broad-spectrum cephalosporin, in mice, rats, rabbits and dogs.
J Antibiot (Tokyo). 1980 Dec;33(12):1532-44. doi: 10.7164/antibiotics.33.1532.
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Ceftezole, a new cephalosporin C derivative II. Distribution and excretion in parenteral administration.头孢替唑,一种新型头孢菌素C衍生物II。静脉注射给药后的分布与排泄。
J Antibiot (Tokyo). 1976 Oct;29(10):1071-82. doi: 10.7164/antibiotics.29.1071.
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Absorption, distribution and excretion of cefsulodin, an antipseudomonal cephalosporin, in mice, rats and dogs.
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A new cephalosporin. SCE-963: 7-[2-(2-aminothiazol-4-yl)-acetamido]-3-[[[1-(2-dimethylaminoethyl)-1h-tetrazol-5-yl]-thio]methyl]ceph-3-em-4-carboxylic acid. Chemistry and structure-activity relationships.一种新型头孢菌素。SCE - 963:7 - [2 -(2 - 氨基噻唑 - 4 - 基)- 乙酰胺基] - 3 - [[[1 -(2 - 二甲基氨基乙基)- 1H - 四氮唑 - 5 - 基] - 硫代]甲基]头孢 - 3 - 烯 - 4 - 羧酸。化学与构效关系
J Antibiot (Tokyo). 1978 Dec;31(12):1262-71. doi: 10.7164/antibiotics.31.1262.
6
Metabolic fate of SCE-1365, a new broad-spectrum cephalosporin, after parenteral administration to rats and dogs.新型广谱头孢菌素SCE - 1365经肠胃外给药于大鼠和犬后的代谢转归
Antimicrob Agents Chemother. 1980 Oct;18(4):511-8. doi: 10.1128/AAC.18.4.511.
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Cefazolin, a new semisynthetic cephalosporin antibiotic. 3. Absorption, excretion and tissue distribution in parenteral administration.头孢唑林,一种新型半合成头孢菌素抗生素。3. 胃肠外给药的吸收、排泄及组织分布。
J Antibiot (Tokyo). 1970 Apr;23(4):184-94.
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SCE-963, a new broad-spectrum cephalosporin: in vitro and in vivo antibacterial activities.SCE - 963,一种新型广谱头孢菌素:体外及体内抗菌活性
Antimicrob Agents Chemother. 1978 Oct;14(4):557-68. doi: 10.1128/AAC.14.4.557.
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3-Deacetoxy-7-(alpha-amino-1-cyclohexenylacetamido) cephalosporanic acid (SCE-100), a new semisynthetic cephalosporin. III. Comparative studies on absorption, distribution and excretion of SCE-100 and cephalexin (CEX) in laboratory animals.
J Antibiot (Tokyo). 1976 May;29(5):571-8. doi: 10.7164/antibiotics.29.571.
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Comparative pharmacokinetics of SCE-2787 and related antibiotics in experimental animals.SCE - 2787及相关抗生素在实验动物中的比较药代动力学
Antimicrob Agents Chemother. 1992 Nov;36(11):2481-6. doi: 10.1128/AAC.36.11.2481.

引用本文的文献

1
Therapeutic effects of cefotiam and cefazolin on experimental pneumonia caused by Klebsiella pneumoniae DT-S in mice.头孢替安和头孢唑林对小鼠肺炎克雷伯菌DT-S所致实验性肺炎的治疗作用。
Antimicrob Agents Chemother. 1980 Oct;18(4):549-56. doi: 10.1128/AAC.18.4.549.
2
Comparative activities of cefotiam and cefazolin against urinary tract infections with Proteus mirabilis in mice.头孢替安和头孢唑林对小鼠奇异变形杆菌所致尿路感染的比较活性
Antimicrob Agents Chemother. 1980 Aug;18(2):257-63. doi: 10.1128/AAC.18.2.257.
3
Cefotiam therapy of lower respiratory tract infections.
头孢替安治疗下呼吸道感染
Antimicrob Agents Chemother. 1985 Oct;28(4):576-7. doi: 10.1128/AAC.28.4.576.