阿奇霉素临床药代动力学研究

CLINICAL PHARMACOKINETIS STUDY ON AZITHROMYCIN

为了研究国产阿奇霉素在健康志愿者体内过程及其胶囊的相对生物利用度，我们在８位健康男性志愿者中单剂空腹口服国产或进口阿奇霉素５００ｍｇ，采用微生物法测定其血、尿药物浓度。结果为健康志愿者单剂空腹口服国产阿奇霉素胶囊５００ｍｇ后，其血药Ｃｍａｘ为０．４１±０．１５ｍｇ／Ｌ，消除半衰期为４６．６±８．５ｈ，ＡＵＣ为６．９４±１．２８ｍｇ·ｈ－１·Ｌ－１，与进口阿奇霉素胶囊的主要药代动力学参数进行比较，其差别均无统计学意义（Ｐ＞０．０５）。与进口阿奇霉素比较，国产阿奇霉素胶囊的相对生物利用度为９７．７９％，口服该药１４４ｈ尿排出率为给药量的１１．２９％。结果表明：国产阿奇霉素体内过程与进口阿奇霉素相仿。

In order to evaluate the pharmacokinetic profiles of domestic azithromycin and the relative bioavailbility of the capsule,five hundred mg of domestic and imported azithromycin capsule were given by oral administration to 8 healthy fasting volunteers.The drug concentration in serum and urine was measured by bioassay,Mean peak Serum concentration was 0.41±0.15 mg/L after a single oral dose of 500 mg of domestic capsule.Mean elimination half-life was 46.6±8.5 h and mean serum area under curve was 6.94±1.28 mg·h-1·L-1.Compared with imported capsule,the differences of the Cmax,T1/2β,AUC and other main pharmacokinetic parameters were not statistically significant.The relative bioavailability of domestic azithromycin capsule was 97.79%,compared with the imported one.The urinary recovery rate of the azithromycin was 11.29% during the period of 144 h after oral adminstration of domestic capsule.In conclusion the pharmacokinetic profile of domestic azithromycin was similar to that of imported azithromycin.