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[阿米卡星在耳周淋巴液和血清中的药代动力学。氨基糖苷类抗生素潜在耳毒性比较评估方法]

[Pharmacokinetics of amikacin in the perilymph and blood serum. An approach to the comparative evaluation of the potential ototoxicity of aminoglycoside antibiotics].

作者信息

Dolgova G V, Berezhinskaia V V, Firsov A A

出版信息

Antibiot Med Biotekhnol. 1986 Dec;31(12):909-13.

PMID:3566220
Abstract

The pharmacokinetics of amikacin in serum and perilymph was studied on guinea pigs treated with its single subcutaneous administrations in doses of 100, 200, 400 and 800 mg/kg. Proportional relation between the values of the areas under the concentration against time curves of the antibiotic in serum and perilymph was shown. It suggested that the level of the antibiotic penetration into the internal ear might be predicted by the area under the concentration against time curve of the aminoglycoside. It was demonstrated that in equitherapeutic doses when D/Deq = 1 aminoglycosides had different areas under the concentration against time curve. Thus, the area under the curve of amikacin was 2.2 times higher than that of sisomicin. It was also demonstrated that the angle coefficient characterizing the relationship between the area under the concentration against time curve in perilymph and the dose standardized with respect to the equitherapeutic value was markedly higher for amikacin than for sisomicin.

摘要

在豚鼠上研究了阿米卡星单次皮下注射100、200、400和800mg/kg剂量后在血清和外淋巴中的药代动力学。结果显示抗生素在血清和外淋巴中的浓度-时间曲线下面积值之间存在比例关系。这表明氨基糖苷类抗生素在血清中的浓度-时间曲线下面积可预测其在内耳中的渗透水平。结果表明,在等效治疗剂量(D/Deq = 1)时,氨基糖苷类抗生素的浓度-时间曲线下面积不同。因此,阿米卡星的曲线下面积比西索米星高2.2倍。还表明,表征外淋巴中浓度-时间曲线下面积与相对于等效治疗值标准化剂量之间关系的角系数,阿米卡星明显高于西索米星。

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