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小诺霉素的药物动力学研究

PHARMACOKINETIC STUDIES OF MICRONOMICIN

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【摘要】 报告微生物法测定血清中小诺霉素浓度,并用于家兔静脉和肌内给药及细菌性感染患者肌内给药的药物动力学研究。家兔静脉给药5mg/kg,药物动力学方程为C=-27.36e-13.65(?)+22.07e-0.505t;家兔肌内给药5mg/kg,药物动力学方程为c=15.10(e-0.4(?)7-e-5.143t。吸收迅速完全,30min 可达高峰。在10例感染性疾病患者中,一次肌内给药120mg 小诺霉素,吸收迅速,平均达峰时间为0.76h,平均峰浓度9.61ug/ml,平均消除半衰期为2.63h。个体差异较大。

【Abstract】 The present paper reports the pharmacokinetic studies of mieronomi(?)n(MCR)in rabbits and in patients with bacterial infection.The serum con-centration of MCR were monitored by microbiological assay after admini-stration.After a single i.v.5mg/kg of MCR in rabbits,the drug con-centration-time curve was a two-compartment open model with an equitionC=27.36(?)e-13.(?)58T+22.07e-0.505t.The serum data of a single i.v.5mg/kgof MCR fitted a one-compartment open model with an equition C=15.10(e-0.487t-e-5.143t).The MCR was absorbed rapidly and completely the meanserum peak levels were achieved in about 30 min.Ten patients with bac-terial infection were injected intramuscularly with a dose of 120 mg ofMCR,pharmaeokinetic parameters were calculated by a one-compartmentkinetic analysis.The results showed that the rate of absorption was ra-pid,the mean achieved times were 0.76hr,the mean peak levels9.61mg/1,the mean biological malf-life was 2.63hr,there was large interindivi-dual variation in the pharmacokinetic paraments of MCR.

【关键词】 小诺霉素; 药物动力学; 感染; 人类; 兔;
【Key words】 micronomicin; pharmacokinetics; infection; human; rabbits;
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