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单剂量和多剂量给药后豚鼠血清和外淋巴中核糖霉素的药代动力学分析。

Analysis of the phamacokinetics of ribostamycin in serum and perilymph of guinea pigs after single and multiple doses.

作者信息

Harpur E S, Gonda I

出版信息

Br J Audiol. 1982 May;16(2):95-9. doi: 10.3109/03005368209081453.

Abstract

The pharmacokinetics of ribostamycin in serum and perilymph of guinea pigs was studied after a single s.c. injection of 400 mg/kg or 14 daily injections of the same dose. The repetitive administration of ribostamycin did not produce functional impairment of the kidney and ototoxicity was slight. The pharmacokinetic data were analysed by non-linear least mean squares regression. Ribostamycin did not accumulate in either serum or perilymph after multiple dosing. The half-life of the drug in perilymph was 15.8 h after a single injection, but 7.6 h after the last of 14 injections. The area under the ribostamycin concentration in perilymph against time curve was also reduced after multiple dosing. These changes were found to be due to a marked increase in the rate of transfer of the drug from perilymph to serum after multiple dosing.

摘要

在豚鼠单次皮下注射400mg/kg或每日1次、连续14天注射相同剂量的核糖霉素后,研究了其在血清和外淋巴中的药代动力学。重复给予核糖霉素未产生肾功能损害,耳毒性轻微。采用非线性最小二乘回归分析药代动力学数据。多次给药后,核糖霉素在血清和外淋巴中均未蓄积。单次注射后,药物在外淋巴中的半衰期为15.8小时,但在14次注射中的最后一次注射后为7.6小时。多次给药后,核糖霉素在外淋巴中浓度-时间曲线下面积也减小。发现这些变化是由于多次给药后药物从外淋巴向血清的转运速率显著增加所致。

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