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[埃瑞莫霉素在实验中的药代动力学研究]

[Pharmacokinetic study of eremomycin in an experiment].

作者信息

Filippos'iants S T, Malkova I V

出版信息

Antibiot Med Biotekhnol. 1987 Jul;32(7):511-6.

PMID:3118795
Abstract

Pharmacokinetics of eremomycin, a novel original glycopeptide antibiotic was studied. It was shown that after a single intravenous or subcutaneous administration to mice, rabbits and dogs eremomycin concentrations in blood and duration of the antibiotic circulation depended on the dose level and administration route. After subcutaneous or intramuscular administration eremomycin was rapidly absorbed and detected in serum even in 15-30 min. The maximum levels were observed in 2 hours. Absolute bioavailability after subcutaneous administration averaged to 85 per cent. Eremomycin penetrated into organs. The antibiotic concentrations in cerebrospinal fluid were low. The highest concentrations of eremomycin were detected in the kidneys, lungs and spleen. The antibiotic mainly excreted with urine. The renal clearance amounted to 85 per cent of the total clearance. 2-3-month exposure of dogs and rats to eremomycin in doses 4-10 times higher than the approximate single therapeutic doses for humans (250 mg) resulted in cumulation of the antibiotic.

摘要

对新型原创糖肽抗生素埃瑞霉素的药代动力学进行了研究。结果表明,对小鼠、兔子和狗单次静脉注射或皮下注射后,血液中的埃瑞霉素浓度以及抗生素的循环持续时间取决于剂量水平和给药途径。皮下或肌肉注射后,埃瑞霉素迅速吸收,甚至在15 - 30分钟内就能在血清中检测到。2小时后观察到最高水平。皮下给药后的绝对生物利用度平均为85%。埃瑞霉素可渗透到器官中。脑脊液中的抗生素浓度较低。在肾脏、肺和脾脏中检测到的埃瑞霉素浓度最高。抗生素主要通过尿液排泄。肾脏清除率占总清除率的85%。给狗和大鼠以高于人类近似单次治疗剂量(250毫克)4 - 10倍的剂量接触埃瑞霉素2 - 3个月,会导致抗生素蓄积。

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