Kaniwa N, Ogata H, Aoyagi N, Ejima A, Takahashi T, Uezono Y, Imazato Y
Division of Drugs, National Institute of Hygienic Sciences, Tokyo, Japan.
Clin Pharmacol Ther. 1991 Jun;49(6):641-7. doi: 10.1038/clpt.1991.81.
The bioavailability of five capsules of cyclandelate that are commercially available in Japan was determined in ten healthy volunteers by measuring mandelic acid (a main metabolite of cyclandelate) excreted in the urine. Bioinequivalence among the five capsules was demonstrated. The relative cumulative excretion of mandelic acid of the most poorly bioavailable capsule was 38% of the most highly bioavailable capsule. The effect of food on the bioavailability of these two capsules was investigated by use of two different kinds of food, one containing fat and one containing high carbohydrates but very low fat. The bioavailability of the two capsules was increased when subjects consumed both types of food before drug administration, although there was a greater effect on bioavailability with food containing fat. This suggests that the absorption of cyclandelate was incomplete in fasting subjects, even from the capsule with the highest bioavailability. Bioinequivalence between the two capsules remained after postprandial drug administration.
通过测量尿液中排出的扁桃酸(环扁桃酯的主要代谢物),在10名健康志愿者中测定了日本市售的5种环扁桃酯胶囊的生物利用度。结果表明这5种胶囊之间存在生物不等效性。生物利用度最差的胶囊中扁桃酸的相对累积排泄量为生物利用度最高的胶囊的38%。通过使用两种不同的食物(一种含脂肪,另一种含高碳水化合物但脂肪含量极低),研究了食物对这两种胶囊生物利用度的影响。当受试者在给药前食用这两种食物时,两种胶囊的生物利用度均有所提高,不过含脂肪的食物对生物利用度的影响更大。这表明即使是生物利用度最高的胶囊,在空腹受试者中,环扁桃酯的吸收也是不完全的。餐后给药后,两种胶囊之间的生物不等效性依然存在。