国产硫酸奈替米星注射液的药动学研究  

Pharmacokinetic study on the domestic netilmicin sulphate injection

作　　者：汪冰[1] 张慧琳[1] 冯萍[1] 吕晓菊[1] 卢毅[1] 俞汝佳[1] 朱淑媛[1] 周志强[1] 

机构地区：[1]华西医科大学附属第一医院

出　　处：《中国抗生素杂志》1997年第2期118-123,共6页Chinese Journal of Antibiotics

摘　　要：采用微生物法对８名健康受试者单剂静脉滴注和肌注１００ｍｇ硫酸奈替米星注射液进行药动学研究，测定了给药后不同时间的血、尿药浓度，并经计算机程序计算药动学参数。结果显示：单剂静滴和肌注后的药动学符合二室开放模型，静滴药动学方程式为：Ｃ＝１０．８１２２ｅ－３．６７１４ｔ＋４．８８３１ｅ－０．２２０５ｔ；肌注药动学方程式为：Ｃ＝９．６８６８ｅ－１．４９１８ｔ＋５．４７５４ｅ－０．２０８６ｔ－１０．９７７０ｅ－３．７２５９ｔ。Ｔ１／２α分别为０．７４７８和０．４１２１ｈ，Ｔ１／２β分别为３．２３０８和２．８７４０ｈ，峰浓度分别为１３．１１和７．６０μｇ／ｍｌ，肌注后达峰时间为０．４８ｈ，总清除率分别为３．２２和３．２６（Ｌ／ｈ），２４ｈ肾排出率分别为５９．０６％和６８．５７％。给药后６ｈ内血药浓度及２４ｈ内尿药浓度＞１μｇ／ｍｌ，尿药浓度明显高于血药浓度。本研究结果与进口硫酸奈替米星注射液药动学过程基本一致。根据其药动学特征，建议一般给药方案为１００ｍｇ每日２次，可达到和维持有效血药浓度。In this study, 8 healthy volunteers received 100mg of netilmicin each one, first intravenously and two weeks later intramuscularly, the concentration of netilmicin in serum and urine were tested with microbiological methods. Pharmacokinetic parameters were calculated by the computer program MCPKP. The pharmacokinetic progress of single dose fitted to two compartments open model. The pharmacokinetic equations for intravenous and intramuscular are C =10.8122e -3.6714t +4.8831e -0.2205t and C =9.6868e -1.4918t + 5.4754e -0.2086t -10.9770e -3.7259t . T 1/2α are 0.7478 and 0.4121h; T 1/2β are 3.2308 and 2.8740h respectively. Peak drug concentration in serum are 13.11 and 7.60μg/ml of intravenous and intramuscular administration. After intramuscular administration, the T max was 0.48h, the availability ( F ) is 89.63%. The total clearance rates are 3.22 and 3.26L/h. The renal excreting rate in 24h are 59.06% and 68.57%. The concentration in serum in 6h and the concentration in urine in 24h after administration of single dose are higher than 1μg/ml; the concentration of netilmicin in urine is obviously higher than that in serum. Results are compatible to that of the imported netilmicin sulphate. According to the feature of the pharmacokinetics, it was suggested that the general prescription of netilmicin is 100mg for intravenous or intramu scular q12h, which may produce the effective serum concentration.

关 键 词：奈替米星 药物动力学 

分 类 号：R978.12[医药卫生—药品]