Cloxacillin Sodium是Cloxacillin的钠盐形式,是一种耐青霉素酶,耐酸,半合成的青霉素。
Cloxacillin is an antibiotic useful for the study of a number of bacterial infections.
Cell Viability Assay
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Cell Line:
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Strains M12 and M60.
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Concentration:
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0.5 μg/mL.
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Incubation Time:
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4-24 h.
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Result:
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Significantly reduced the bacterial numbers.
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Cloxacillin sodium (50 mg/kg, Subcutaneously) results a significant antibiotic efficacy against
S. aureus
.
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Animal Model:
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Mice.
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Dosage:
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10 mg/kg (
Pharmacological Analysis
).
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Administration:
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Given subcutaneously.
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Result:
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Reached a maximal concentration in plasma of 8.4 μg/mL at 10 min and had a half-life of approximately 15 min.
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|
Animal Model:
|
Mice injected with approximately 2 × 10
6
CFU of bacteria in 0.1 mL saline were aseptically injected into the right thigh muscle.
|
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Dosage:
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0–500 mg/kg.
|
|
Administration:
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Subcutaneously in the nuchal region at 1 h after infection.
|
|
Result:
|
Resulted in a significant decrease in the number of viable
S. aureus
measured 18 h thereafter.
|
化学性质
白色粉末或结晶性粉末。熔点170℃(分解)。易溶于水,溶于乙醇,微溶于氯仿,有引湿性,微臭,味苦。
用途
该品为半合成抗菌素,与苯唑西林的作用特点和用途均极相似,对耐药金葡菌该品有杀菌作用。口服或肌注吸收较好,血浓度比苯唑西林高2倍,主要用于耐药金葡菌所致感染,如败血症、骨髓炎、皮肤软组织感染、心内膜炎、泌尿系统感染及脑膜炎等疗效较好。
生产方法
邻甲苯胺经重氮化、置换、氯化、水解、肟化等操作。得到邻氯苯甲肟氯,然后与乙酰乙酸乙酯环合、用五氯化磷氯化,得到3-邻氯苯基-5-甲基-4异噁酰氯,最后与6-APA缩合得到邻氯青霉素碱、加异辛酸钠成盐、即为邻氯青霉素钠。