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红霉素肠溶颗粒和肠溶片的相对生物利用度
RELATIVE BIOAVAILABILITY OF ENTERIC-COATED ERYTHROMYCIN PELLETS AND TABLETS
【摘要】 红霉素碱肠溶片不便于小儿分剂量服用,我们研制了一种肠溶颗粒新剂型。本文采用微生物法(琼脂打孔法)测定了12名健康志愿者单剂量交叉口服三种不同工艺和辅料制成的红霉素肠溶颗粒(EI、EII、EIII)及一种市售红霉素肠溶片(EIV)各500mg后的血药浓度,经计算机处理:EI、EII和EIII之间各药代动力学参数都较接近(P>0.5),体内吸收(tlag、tmax和Ka)均比EIV快(P<0.05),且个体差异小,血峰浓度(Cmax)分别是EIV的1.15、1.30和1.34倍,相对生物利用度(颗粒AUC/片剂AUC)分别为126.3、136.1和133.3%。
【Abstract】 Enteric-coated erythromycin tablets are not convenient for pediatrio use in sraall divided doges. So we prepared three new formulations of enteric-coated erythromyoin pellets (EⅠ, EⅡ, and EⅢ). In this bioavailability study, 500 mg of three new formulations and 600 mg of another commercially available tablet (EⅣ) were administered by crossover raethod to 12 volunteers. Serum erythromyoin concentration data determined by miorobial assay showed that there were no statistical differences in the pharmacokinetio parameters between EⅠ and EⅡ, or EⅢ. EⅠ, EⅡ and EⅢ appeared in the blood stream more rapidly than EⅣ, as indicated by differences in tlag, tmax and Ka (P<0.05). Their individual variances were less than with EIV. The Cmax of EⅠ, EⅡ, and EⅢ were 1.15, 1.30, and 1.34 times of EⅣ, respectively. The relative bioavailability (AUC of pellet/AUC of tablet) of the three dosage forms of pellets were 123.6, 136.1, and 133.3%, respectively.
【Key words】 erythromycin; enteric-coated pellots; bioavailability; pharmao-okinetics;
- 【文献出处】 上海医科大学学报 , 编辑部邮箱 ,1990年01期
- 【被引频次】3
- 【下载频次】173