Ogata H, Aoyagi N, Kaniwa N, Ejima A
J Pharmacobiodyn. 1984 Oct;7(10):760-7. doi: 10.1248/bpb1978.7.760.
The effect of food on the bioavailability of two single lots of commercial tablets and one trial tablet of nalidixic acid, varying widely in drug dissolution characteristics, was determined in healthy male subjects after oral administration. Four subjects received, in a crossover fashion, a single 250 mg dose in an uncoated tablet during periods of fasting and non-fasting. Significant differences in Cmax, Tmax and AUC0-8 were observed between the tablet having the fastest dissolution rate and the other tablets tested, when administered postprandially. Both Cmax and AUC0-8 were significantly increased after administration of the two tablets exhibiting the poorer dissolution characteristics to the non-fasting subjects. However, food was not observed to affect any of the bioavailability parameters after postprandial administration of the tablet exhibiting the fastest dissolution rate. The improvement of bioavailability of the two tablets exhibiting the poorer dissolution by food intake was ascribable to enhanced dissolution of nalidixic acid resulting from vigorous mixing and agitation in the digestive tract. It was concluded that the effect of food on the bioavailability of nalidixic acid from uncoated tablets varies with formulation factors, especially with dissolution characteristics.
在健康男性受试者口服给药后，测定了食物对两种不同批次的市售萘啶酸片剂以及一种试验片剂生物利用度的影响，这三种片剂的药物溶出特性差异很大。四名受试者采用交叉方式，在禁食和非禁食期间分别单次服用一片250毫克的未包衣片剂。餐后给药时，溶出速率最快的片剂与其他受试片剂相比，在Cmax、Tmax和AUC0-8方面观察到显著差异。向非禁食受试者给药两种溶出特性较差的片剂后，Cmax和AUC0-8均显著增加。然而，餐后服用溶出速率最快的片剂后，未观察到食物对任何生物利用度参数有影响。摄入食物使两种溶出特性较差的片剂的生物利用度提高，这归因于萘啶酸在消化道中剧烈混合和搅动导致溶出增强。得出的结论是，食物对未包衣片剂中萘啶酸生物利用度的影响因制剂因素而异，尤其是溶出特性。
