麦迪霉素口服制剂人体生物利用度比较研究  

COMPARATIVE BIOAVAILABILITY OF ORAL MYDECAMYCIN PREPERATIONS IN NORMAL VOLUNTEERS

作　　者：陆红[1] 李家泰[1] 金少鸿[2] 吴铨[2] 张朴[1] 徐秀英[1] 

机构地区：[1]北京医科大学临床药理研究所,北京100034 [2]中国药品生物制品检定所,北京100050

出　　处：《中国临床药理学杂志》1993年第2期75-80,共6页The Chinese Journal of Clinical Pharmacology

摘　　要：8例男性健康志愿者分别交叉口服600mg日本产和国产的麦迪霉素胃溶胶囊和肠溶片,用微生物法测定血尿标本进行相对生物利用度研究,结果表明:口服日本产和国产的胃溶胶囊均能较快吸收,达峰时间(Tmax)分别为0.62±0.30和0.70±0.08 h;峰浓度(Cmax)分别为1.06±0.54和0.93±0.57mg/l;二者的药时曲线下面积(AUC)为1.09±0.28和0.99±0.33mg/l·h;消除半衰期分别为0.51±0.12和0.53±0.28h;国产胃溶胶囊对日本产胃溶胶囊的平均相对生物利用度为90.83%。口服日本产和国产的麦迪霉素肠溶片吸收均较差,血药浓度很低,明显低于胃溶胶囊,大多数受试者的最高血药浓度均<0.1mg/l,一般只有胃溶胶囊血药浓度的1/10。12h尿中麦迪霉素回收率:日本产和国产胃溶胶囊分别为给药剂量的0.83%和1.86%;肠溶片分别为给药剂量的0.65%和1.05%。从本组交叉试验结果可见,胃溶胶囊吸收比较规律,而肠溶片吸收不规律,个体差异很大,所以认为肠溶片不宜作为口服剂型上市。The relative bioavailability of Mydecamycin of gastro-dissolved capsule and en-tero-dissolved tablet made in Japan and in China was studied in 8 normal male volunteers. Serum andurine concentrations of Mydecamycin was rapidly absorbed from the gastro-dissolved capsule made inJapan and in China. Peak serum levels reached 1.06±0.54 and 0.93±0.30mg/l at 0.62±0.30 and 0.70±0.08h respectively. The biological half-life (t1/2) were 0.51±0.12 and 0.53±0.28h respectively. Therelative bioavailability of gastro dissolved capsule made in China to that made in Japan was 90.83%. The12 h recoveries of Mydecamycin were 0.83% and 1.86% of the dose, respectively. Mydecamycin was bad absorbing after administration of 600mg entero-dissolved tablet made in Japanand in China, the serum levels of entero-dissolved tablets were lower than that of the gastro-dissolvedtablets. Most volunteers peak levels were lower than 0.1 mg/l, 1/10 of the gastro-dissolved capsuleserum levels. The 12h recoveries of Mydecamycin made in Japan and in China were 0.65% and 1.05% ofthe dose, respectively.

关 键 词：麦迪霉素 胶囊 片剂 生物利用度 

分 类 号：R927.2[医药卫生—药学]