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两性霉素B在人体内的分布与活性。

Distribution and activity of amphotericin B in humans.

作者信息

Christiansen K J, Bernard E M, Gold J W, Armstrong D

出版信息

J Infect Dis. 1985 Nov;152(5):1037-43. doi: 10.1093/infdis/152.5.1037.

DOI:10.1093/infdis/152.5.1037
PMID:4045244
Abstract

Concentrations of amphotericin B (AmB) in tissues obtained at autopsy from eight patients were measured by high-performance liquid chromatography (HPLC). The patients had received doses of 101-2,688 mg of antibiotic. Highest concentrations of the drug were found in the liver; in one patient the amount of AmB in the liver was 41% of the total dose. No evidence of metabolism of the drug was observed, and bioassay of ethanol extracts of tissue showed that the drug retained activity. Three of the patients had histologic evidence of aspergillar or candidal infection in tissues with concentrations of AmB ranging from 2.5 to 166 micrograms/g. With two patients, the concentrations of the drug in the tissues exceeded by greater than or equal to 10-fold the minimum inhibitory concentrations of the drug in isolates that had been obtained from the same tissues. Unknown factors present in tissues appear to limit the in vivo activity of AmB.

摘要

通过高效液相色谱法(HPLC)测定了8例患者尸检时获取的组织中两性霉素B(AmB)的浓度。这些患者接受的抗生素剂量为101 - 2688毫克。药物在肝脏中的浓度最高;在1例患者中,肝脏中AmB的量占总剂量的41%。未观察到该药物代谢的证据,并且组织乙醇提取物的生物测定表明该药物仍具有活性。3例患者的组织中有曲霉或念珠菌感染的组织学证据,AmB浓度范围为2.5至166微克/克。对于2例患者,组织中该药物的浓度比从相同组织分离出的菌株中该药物的最低抑菌浓度高出10倍或更多。组织中存在的未知因素似乎限制了AmB的体内活性。

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