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阿莫西林联合羧甲司坦与单用阿莫西林在病理性支气管分泌物及肺组织中的穿透性比较。

Comparison between penetration of amoxicillin combined with carbocysteine and amoxicillin alone in pathological bronchial secretions and pulmonary tissue.

作者信息

Braga P C, Scaglione F, Scarpazza G, Fraticelli G, Roviaro G, Varoli F, Mariani C, Falchi M, Fraschini F

出版信息

Int J Clin Pharmacol Res. 1985;5(5):331-40.

PMID:4066083
Abstract

Patients with chronic bronchitis were treated orally with either amoxicillin (500 mg) alone or in combination with carbocysteine (150 mg), thrice daily for five days, in order to assess whether the combination allows higher antibiotic levels to be obtained in bronchial mucus than those obtained from amoxicillin alone. Serum and mucus levels were determined for each patient at first and fifth day of the two drug regimens. The levels of amoxicillin in the lung tissue collected in patients undergoing pulmonary surgery were also determined after a single oral dose of amoxicillin (1 g) or of amoxicillin (1 g) plus carbocysteine (300 mg). In the bronchial secretions, at the same plasma concentrations, amoxicillin levels were statistically higher after administration of combined substances. These findings indicate the presence of a pharmacokinetic synergism between these compounds, which allows amoxicillin to penetrate more easily through the hemato-bronchial barrier. The association of amoxicillin and carbocysteine, determining an increase of the quantitative levels of antibiotic in the bronchial secretion (also if it is purulent), performs a sterilizing action in a short time with significant therapeutic advantages.

摘要

为了评估阿莫西林(500毫克)单独使用或与羧甲司坦(150毫克)联合使用(均每日口服三次,持续五天)治疗慢性支气管炎患者时,联合用药是否能使支气管黏液中的抗生素水平高于单独使用阿莫西林时的水平,对每位患者在两种药物治疗方案的第一天和第五天测定血清和黏液水平。在接受肺部手术的患者单次口服阿莫西林(1克)或阿莫西林(1克)加羧甲司坦(300毫克)后,也测定了肺组织中阿莫西林的水平。在支气管分泌物中,在相同血浆浓度下,联合用药后阿莫西林水平在统计学上更高。这些发现表明这些化合物之间存在药代动力学协同作用,这使得阿莫西林更容易穿透血-支气管屏障。阿莫西林与羧甲司坦联合使用,可使支气管分泌物中抗生素的定量水平升高(即使是脓性分泌物),能在短时间内发挥杀菌作用,具有显著的治疗优势。

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