マクロライド系抗生物質製剤の溶出特性とバイオアベイラビリティの関係

概要

論文の詳細を見る
An evaluation of three commercial macrolide antibiotic tablets on factors concerning absorption characteristics was conducted. Macrolide tablets selected in this study were erythromycin stearate (EM), midecamycin acetate (MOM) and rokitamycin (RKM), and the factors studied were dissolution characteristics, stability and bioavailability of respective tablets in man. Dissolution characteristics were examined in three test solutions with normal, hypoand anacidity. Although all tablets dissolved rapidly and in a similar manner in normal acidic solution, differences were observed in hypo- and anacidic solutions. RKM still showed rapid and complete dissolution, while EM and MOM showed less than 50% in the same period examined. In the stability test, EM degradated to 41% within 60 min in acidic solution, but MOM and RKM showed satisfactory stability and 79 and 90% of respective drugs remained under the same condition. Bioavailability was evaluated with six healthy volunteers. The test was conducted with MOM and RKM in a crossover manner and gastric acidity test was performed between each test. MOM showed a great difference in subjects having hypo- and normal gastric acidity while RKM showed little difference between subjects. These results suggest that in vitro dissolution characteristics and stability are reflected in bioavailability of these tablets in man.
社団法人日本薬学会の論文
1987-09-25