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本项研究目的是比较头孢土嗪噻肟(ceftriaxone,CTRX)临床常用的几种每日单次给药方案与作者建议的每日2次给药方案进行比较,并在研究比较的基础上提出2种治疗方案供临床参考。多次给药的血药浓度可以在单次给药的药代动力学参数的基础上,用电脑进行计算,并可根据药物在体内的时间过程与血浆浓度、治疗反应及其他因素(消除半衰期、血浆蛋白结合率等)之间的相互关系对适宜的剂量方案进行评价。按照我们先前对CTRX与CTX所进行的单次给药药代动力学比较研究,用其中静脉给药的药代动力学参数。利用IBM PC/AT电脑,估算出10种多次给药的给药方案。所用程序由中国科学院数学研究所提供。从10种方案中选出一种比较合理的方案B-1,在6名中国男性成人志愿者中进行多次给药药代动力学研究。研究结果表明:在为期5天的疗程内,静脉给药10次,所得药代动力学参数与电脑估算结果非常相似。实测与估算的药代动力学参数表明:CTRX多次给药后各次血药浓度均明显高于CTX,与单次给药药代动力学研究结果相符。作者建议的二种治疗方案为: B-1 用于中度感染:最初48h,1g q12h×2d。第3—7天,0.5g q12h×5d。B-2 用于重度感染:最初48h,每12h给药1次,第1次2g,第2次1g。第3—7天,每日2次,每次1g,间隔12h。
The purpose of this study was to compare several daily single-dose regimens commonly used in ceftriaxone (CTRX) with those recommended by the authors twice a day, and to propose on the basis of a comparative study Two kinds of treatment plan for clinical reference. The plasma concentration for multiple administrations can be calculated on a computer based on the pharmacokinetic parameters of a single administration and can be calculated on the basis of the time course of the drug in the body and the plasma concentration, therapeutic response and other factors (elimination half-life , Plasma protein binding rate, etc.) to evaluate the appropriate dosage regimen. According to our previous single-dose pharmacokinetic study of CTRX vs. CTX, pharmacokinetic parameters were used for intravenous administration. Using IBM PC / AT computers, ten multi-dose dosing regimens were estimated. The procedure used is provided by the Institute of Mathematics, Chinese Academy of Sciences. A reasonable protocol, B-1, was selected from 10 protocols and multiple pharmacokinetic studies were conducted among 6 Chinese male adult volunteers. The results show that: in the 5-day course of treatment, intravenous administration of 10 times, the resulting pharmacokinetic parameters and computer estimates are very similar. The measured and estimated pharmacokinetic parameters showed that the plasma concentration of CTRX after repeated administrations was significantly higher than that of CTX, which was consistent with the single-dose pharmacokinetic study. The authors recommend two treatment options: B-1 for moderate infection: first 48h, 1g q12h × 2d. Day 3-7, 0.5g q12h x 5d. B-2 for severe infections: first 48h, once every 12h, first 2g, second 1g. Day 3-7, 2 times a day, each 1g, interval 12h.