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一种非离子表面活性剂对庆大霉素和阿米卡星肠道吸收的促进作用。

Increase of the intestinal absorption of gentamicin and amikacin by a nonionic surfactant.

作者信息

Rubinstein A, Rubinstein E, Toitou E, Donbrow M

出版信息

Antimicrob Agents Chemother. 1981 May;19(5):696-9. doi: 10.1128/AAC.19.5.696.

Abstract

This study was concerned with the effect of Cetomacrogol (polyethylene glycol 1000 monocetyl ether), a nonionic surfactant, on the absorption of gentamicin and amikacin from the gastrointestinal tract of rats. A 200-mg dose of Cetomacrogol coadministered orally with 10 mg of gentamicin resulted in a mean peak gentamicin blood concentration of 14.1 microgram/ml, compared with 67.8 microgram/mg when the same gentamicin dose was administered intramuscularly. The area under the curve after administration of the oral mixture was 23% of that after the intramuscular dose. The rectal administration of the mixture resulted in a mean peak gentamicin blood level of 8.2 micrograms/ml, compares to 16.5 microgram/ml when the mixture was administered orally. A 50-mg dose of amikacin coadministered orally with 200 mg of Cetomacrogol resulted in a mean peak amikacin blood level of 13.3 microgram/ml, compared to 310 microgram/ml when this amikacin dose was administered intramuscularly. Cetomacrogol augments the intestinal absorption of gentamicin and amikacin in rats. If the toxicity of the combination in humans is limited, the combination may be potentially clinically useful.

摘要

本研究关注非离子表面活性剂鲸蜡醇聚醚(聚乙二醇1000单鲸蜡醚)对庆大霉素和阿米卡星从大鼠胃肠道吸收的影响。口服200毫克鲸蜡醇聚醚与10毫克庆大霉素共同给药后,庆大霉素的平均血药峰浓度为14.1微克/毫升,而肌肉注射相同剂量庆大霉素时为67.8微克/毫克。口服混合剂后曲线下面积为肌肉注射剂量后曲线下面积的23%。直肠给药该混合剂后,庆大霉素的平均血药峰浓度为8.2微克/毫升,而口服该混合剂时为16.5微克/毫升。口服50毫克阿米卡星与200毫克鲸蜡醇聚醚共同给药后,阿米卡星的平均血药峰浓度为13.3微克/毫升,而肌肉注射该剂量阿米卡星时为310微克/毫升。鲸蜡醇聚醚可增强大鼠肠道对庆大霉素和阿米卡星的吸收。如果该组合对人类的毒性有限,则该组合可能具有潜在的临床应用价值。

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引用本文的文献

1
Intranasal administration of gentamicin in human subjects.庆大霉素在人体受试者中的鼻内给药。
Antimicrob Agents Chemother. 1983 May;23(5):778-9. doi: 10.1128/AAC.23.5.778.

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