口服威霉素与市售红霉素制剂在健康志愿者中药代动力学研究

PHARMACOKINETIC STUDY IN HEALTHY VOLUNTEERS OF ORAL ERYTHROMYCIN FILMTAB AND THREE ORAL PRODUCTS OF ERYTHROMYCIN OR ITS ESTER AVAILABLE IN THE MARKET

观察了威霉素(新工艺红霉素硷,美国)及3种国产红霉素制剂正常人空腹单次口服1000mg药代动力学特点,结果表明,威霉素体内吸收明显优于传统红霉素硷肠溶衣片。服药后1.06h出现的高峰血药浓度为3.67±1.64u/ml,明显高于肠溶衣片服药后5.55h的1.46±0.69u/ml的高峰浓度,其曲线下面积是红霉素硷肠溶片的1.18倍;2个厂家的国产红霉素琥珀酸乙酚片口服吸收均不如威霉素。服药后1.09及1.49h出现的高峰血药浓度分别为1.42±0.41u/ml及0.92±0.46u/ml,明显低于威霉素(P<0.05),曲线下的面积AUC,2种国产品分别为威霉素的38%及20%(P<0.05);威霉素,单次空腹口服500mg,每6～8h服药1次,稳态血药浓度可达2.26～0.68u/ml及2.01～0.38u/ml。

Four oral products of erythromycin or its ester were used in the study of their pharmacokinetics in 16 healthy fasting volunteers with a single dose of 1.0g.The results of the study are:(A)Erythromycin base filmtab (Abbott of America)has a peak serum level of 3.67±1.64u/ml at 1.06± 0.56h after administration with an AUC of 1.1 times that of the enteric-coated tablet.(B)Enteric-coated erythromycin tablet has a peak serum level of 1.46± 0.69u/ml at 5.5h after administration with an AUC lower than that of(A). (C)Two tablets of erythromycin ethylsuccinate from different manufacturers have a peak serum level of 1.42±0.41u/ml and 0.92±0.46u/ml at 1.09 and 1.49h respectively after administration with an AUC much lower than that of (A).The data of the study showed that erythromycin base filmtab has an ex- cellent bioavailability than that of the other three products.