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[~3H]-异丁基哌嗪力复霉素在小鼠体内的药物代谢动力学研究
A STUDY OF PHARMACOKINETICS OF ~3H-ISOBUTYL PIPERAZINYL RIFAMYCIN SV IN MICE
【摘要】 <正> 异丁基哌嗪力复霉素系四川抗菌素工业研究所于1976年试制成功,经过多年的体内外抗菌作用研究,临床前药理研究和临床试用,均证实它具有抗菌谱广,作用强,毒副反应小的优点,特别是对结核,麻风杆菌具有较强的抗菌作用。临床试用于治疗结核病、麻风病、化脓性皮肤病,以及沙眼、结膜炎等疾病均取得满意的疗效,与甲哌力复霉素相比具有抗菌力强,对肝脏损害小价格便宜的特点,是一种较理想的新抗结核药。 我们在研究该药的体内过程中,发现在人和不同动物体内该药的血药半衰期有很大差别为了进一步证实这个问题,确保临床用药的安全性和研究异丁基哌嗪力复霉素的体内过程,本文通过测量小鼠口服[~3H]
【Abstract】 Isobutyl-piperazinyl Rifamycin SV (Ri-fandin, R76-1) is a new semisynthetic rifa-mycin family antibiotic produced in China. This paper reported the studies of pharma-cokinetics of 3H-isobutylpiperazinylrifamy-cin SV in mice by liquid scintilation and whole body autoradiogram methods.The experimental results showed the absorption of 3H-R-76-1 was slow and incomplete by oral administration. Six hours after administration per os, the plasma drug concentration reached peak level. The elimination of the drug from the body was rather slow. The half-life in plasma was 20 hours approximately.The whole body radioautogram and liq-uid scintilation method demonstrated the antibiotic was distributed widely in the body. The radioactivity level in liver was the highest, and then the spleen, kidney and lung, only trace amount can be detected in the brain. In the early period after drug administration, e. g. 1 to 3 hours, the stomach and intestine accumulated high concentration of radioactive substances, and then it decreased gradually as the time prolonged.From the parameters of the pharmaco-kinetics in mice, suggested that there were racial difference between the pharmacokin-etics of dogs and rats,which had been studied previously in our labotatory.
- 【文献出处】 抗生素 , 编辑部邮箱 ,1983年05期
- 【被引频次】2
- 【下载频次】26