从药物动力学角度对四种大环内酯类抗生素的评价

Pharmacokinetics evaluation of four kinds of macrolides antibiotics

本文报道交沙霉素、乙酰螺旋霉素、美欧卡霉素及麦迪霉素四种大环内酯类抗生素的药物动力学参数。126名健康志愿者分别给予单剂1000mg 的交沙霉素片剂、乙酰螺旋霉素片剂、美欧卡霉素干糖浆及麦迪霉素胶囊日本产或国产制剂后,其血药浓度采用微生物法测定,它们的体内过程符合一室模型。其日本产和国产制剂主要药动学参数如下:(1)交沙霉素:T_(1/2)分别为1.23及1.02h,Tmax 分别为1.04及1.12 h,Cmax 分别为4.64及4.54μg/ml,AUC 分别为10.51及9.62μg/ml.h。(2)乙酰螺旋霉素:T_(1/2)分别为8.05及2.89h,Tmax 分别为2.76及4.25h,Cmax 分别为1.46及1.89μg/ml,AUC 分别为11.39及11.78ug/ml.h。(3)美欧卡霉素:T_(1/2)分别为0.89及0.95h,Tmax 分别为0.77及0.74h,Cmax分别为2.39及1.67μg/ml,AUC 分别为4.73及3.85μg/ml.h。(4)麦迪霉素T_(1/2)分别为0.94及1.43h,Tmax 分别为0.64及0.60h,Cmax 分别为1.41及1.40μg/ml.AUC 分别为2.71及3.41μg/ml.h。

The pharmacokinetical parameters of josamycin(JM),acetylspiramycin(acetyl-SP),miocamycin(MOM)and medicamycin(MD)were reported.Ajter given 1000mg oral dose of JM tablets,acetyl-SP tablets,MOM dry syrups or MD capsules to 126 healthy volunteers,the plasma drug levels were detected by microbioassay,and their physiological processes could be described by an one-compartment model.The main parameters of the 4 kinds of antibiotics produced in Japan or china were as followes:(1)JM tablets:T1/2 were 1.23 and 1.02h,Tmax were 1.04 and 1.12h,Cmax were 4.64 and 4.54μg/ml,AUC were 10.51 and 9.62μg.h/ml,respectively.(2)Acetyl-SP tablets:T1/2 were 3.05 and 2.89h,Tmax were 2.76 and 4.25h,Cmax were 1.46 and 1.89μg/ml,AUC were 11.39 and 11.78μg.h/ml,respectively.(3)MOM dry syrups:T1/2 were 0.89 and 0.95h,Tmax were 0.77 and 0.74h,Cmax were 2.39 and 1.67μg/ml,AUC were 4.73 and 3.85μg.h/ml,respectively.(4)MD capsules:T1/2 were 0.94 and 1.43h,Tmax were 0.64 and 0.60h,Cmax were 1.41 and 1.40μg/ml,AUC were 2.71 and 3.41μg.h/ml,respectively.There was no significant difference of these parameters betweer domestic and Japan prodructs.