阿莫西林分散片与阿莫西林片的药代动力学比较研究

Pharmacokinetics comparison between amoxicillin dispersible tablets and amoxicillin tablets in healthy volunteers

目的建立测定人血浆中阿莫西林浓度的RP-HPLC法,比较阿莫西林分散片与阿莫西林普通片在健康人体内药代动力学差异。方法选择12名男性健康志愿者分为2组,分别单剂量口服阿莫西林分散片与阿莫西林普通片各500 mg,采用高效液相色谱法检测阿莫西林的血药浓度。结果阿莫西林分散片与阿莫西林普通片主要药代动力学参数C_（max）分别为（742.8±68.4）μg/L和（676.7±57.2）μg/L,t_（max）分别为（2.7±0.3）h和（3 4±0.6）h,t_（1/2）分别为（4.9±1.5）h和（5.9±1.8）h,AUC_0~∞分别为（6 417.3±167.5）μg/（h·L）和（4 704.8±117.9）μg/（h·L）,AUC_0~1分别为为（4 927.4±119.7）μg/（h·L）和（3436.5±103.5）μg/（h·L）。结论阿莫西林分散片t_（max）、t_（1/2）小于普通片,AUC_0~t、AUC_0~∞、C_（max）高于普通片,说明阿莫西林分散片具有一定的速释优点,明显优于普通片。

Objective To develop a RP - HPLC method for determination of amoxicillin in human plasma and compare the pharmacokinetics of amoxicillin dispersible tablets and amoxicillin tablets in healthy volunteers.Methods Twelve healthy male volunteers were selected and divided into two groups,who received a single oral dose of 500 mg amoxicillin sustained release tablets and amoxicillin tablets respectively.The plasma concentrations of amoxicillin were determined by HPLC.Results The main pharmacokinetic parameters of amoxicillin sustained release tablets and amoxicillin tablets were as follows：C_（max） were（742.8±68.4）μg/L and（676.7±57.2）μg/L,t_（max） were（2.7±0.3） h and（3.4±0.6） h,t_（1/2） were（4.9±1.5） h and（5.9±1.8） h,AUC_0~∞were（6 417.3±167.5）μg/（h·L） and（4 704.8±117.9）μg/（h·L）,AUC_0~t were（4 927.4±119.7）μg/（h·L） and（3 436.5±103.5）μg/（h·L） respectively.Conclusion The t_（max） and t_（1/2） of amoxicillin dispersible tablets were significantly smaller than that of amoxicillin tablets,AUC_0~t,AUC_0~∞and C_（max） were significantly higher than that of the amoxicillin tablets.It suggested that the amoxicillin dispersible tablets had a certain property of swift releasing,and it is obvious better than its ordinary tablets.