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在人体中静脉输注乳糖酸红霉素12小时后红霉素的血浆浓度/时间曲线。

Plasma concentration/time curve of erythromycin after a 12-hour intravenous infusion of erythromycin lactobionate in man.

作者信息

Parsons R L, David J, Paddock G M, Stamp S T

出版信息

Postgrad Med J. 1978 Feb;54(628):68-71. doi: 10.1136/pgmj.54.628.68.

Abstract

As the pharmacokinetics after a slow infusion had not previously been evaluated in the doses used in this study, it was decided to measure the plasma concentration/time curve after a twelve-hour intravenous infusion of 2·0 g of erythromycin lactobionate in 2 litres of 0·9% normal saline. Six healthy medical students with no past history of cardiovascular, renal, hepatic, metabolic or gastrointestinal disease and no past drug allergy participated. The concentration of erythromycin base in venous blood was measured by small plate microbiological assay. Venous blood was taken at zero, 15, 30, 45, 60 min and at 2, 3, 4, 6, 8, 12, 16, 20 and 24 hr after starting the infusions. Duplicate assays were performed on all plasma samples at Guy's and at the manufacturer's laboratories. A full haematological and biochemical screening profile was performed before and after the study. The mean ± s.e. plasma erythromycin base concentration rose from 0·7 ± 0·2 μg/ml at 15 min to 6·06 ± 1·6 μg/ml at 1 hr. The peak plasma concentration was between 1·48 ± 0·25 μg/ml at 30 min and 7·21 ± 0·93 μg/ml at 4 hr. The plasma concentration at 12 hr was 6·17 ± 0·33 μg/ml, and fell to 0·37 ± 0·05 μg/ml at 24 hr. These findings suggest that therapeutically effective plasma concentrations follow a slow intravenous infusion of erythromycin lactobionate. There was no evidence of adverse haematological or biochemical function in the tests of blood, hepatic or renal function, apart from two volunteers who vomited after the infusions were discontinued.

摘要

由于此前尚未对本研究中使用的剂量进行缓慢输注后的药代动力学评估,因此决定在2升0.9%生理盐水中静脉输注2.0克乳糖酸红霉素12小时后,测量血浆浓度/时间曲线。六名无心血管、肾脏、肝脏、代谢或胃肠道疾病病史且无药物过敏史的健康医学生参与了研究。静脉血中红霉素碱的浓度通过小平板微生物测定法测量。在开始输注后的0、15、30、45、60分钟以及2、3、4、6、8、12、16、20和24小时采集静脉血。所有血浆样本均在盖伊医院和制造商实验室进行了重复检测。在研究前后进行了全面的血液学和生化筛查。血浆红霉素碱平均浓度±标准误从15分钟时的0.7±0.2微克/毫升升至1小时时的6.06±1.6微克/毫升。血浆峰值浓度在30分钟时为1.48±0.25微克/毫升至4小时时为7.21±0.93微克/毫升之间。12小时时血浆浓度为6.17±0.33微克/毫升,24小时时降至0.37±0.05微克/毫升。这些发现表明,缓慢静脉输注乳糖酸红霉素后可达到治疗有效的血浆浓度。除两名志愿者在输注停止后呕吐外,血液、肝脏或肾脏功能测试中没有不良血液学或生化功能的证据。

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