氯唑西林钠一水合物

氯唑西林钠一水合物化学性质

安全信息

氯唑西林钠一水合物化学药品说明书

体外研究

Cloxacillin is an antibiotic useful for the study of a number of bacterial infections.

Cell Viability Assay

Cell Line:	Strains M12 and M60.
Concentration:	0.5 μg/mL.
Incubation Time:	4-24 h.
Result:	Significantly reduced the bacterial numbers.

体内研究

Cloxacillin sodium (50 mg/kg, Subcutaneously) results a significant antibiotic efficacy against S. aureus .

Animal Model:	Mice.
Dosage:	10 mg/kg ( Pharmacological Analysis ).
Administration:	Given subcutaneously.
Result:	Reached a maximal concentration in plasma of 8.4 μg/mL at 10 min and had a half-life of approximately 15 min.

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.
Dosage:	0–500 mg/kg.
Administration:	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。

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