Wåhlin-Boll E, Melander A, Sartor G, Scherstén B
Eur J Clin Pharmacol. 1980 Oct;18(3):279-83. doi: 10.1007/BF00563012.
The influence of a standardized breakfast on the single dose (5 mg) kinetics and effects of glipizide was examined in 9 healthy volunteers and in 14 diabetics not previously exposed to a sulfonylurea. In the volunteers, glipizide caused an increase in plasma insulin and a reduction in blood glucose both during continued fasting and when the drug was taken with the breakfast. Food intake did not influence the peak concentration, the elimination half-life or the bioavailability of the drug. However, food intake significantly delayed the absorption of glipizide by about 0.5 h. In the patients. glipizide produced a significant increase in plasma glucose in response to the meal. Starting at breakfast and for 45 min thereafter serum glipizide concentrations were significantly higher when the drug was taken 0.5 h before the meal, than when ingested concurrently with it. With the former treatment, the increase in plasma insulin occurred earlier and the blood glucose reduction was pronouncedly greater than with the latter treatment. As the absorption of glipizide may be delayed by concurrent breakfast, this may help to explain, why the administration of glipizide 0.5 h before breakfast led to a more appropriate relation between the serum concentration of the drug and the metabolic impact of the meal, thereby promoting more appropriate insulin release and better glucose disposition than after concurrent intake of the drug and breakfast.
在9名健康志愿者和14名既往未使用过磺脲类药物的糖尿病患者中，研究了标准化早餐对单剂量（5毫克）格列吡嗪的药代动力学及效应的影响。在志愿者中，无论是持续禁食期间还是药物与早餐同时服用时，格列吡嗪均使血浆胰岛素升高，血糖降低。食物摄入不影响药物的峰浓度、消除半衰期或生物利用度。然而，食物摄入使格列吡嗪的吸收显著延迟约0.5小时。在患者中，格列吡嗪使餐后血浆葡萄糖显著升高。早餐开始时及此后45分钟内，饭前0.5小时服用药物时的血清格列吡嗪浓度显著高于与餐同服时。采用前一种给药方式时，血浆胰岛素升高出现得更早，血糖降低幅度明显大于后一种给药方式。由于同时进食早餐可能会延迟格列吡嗪的吸收，这可能有助于解释为何早餐前0.5小时服用格列吡嗪会使药物血清浓度与餐的代谢影响之间的关系更为合适，从而比药物与早餐同时服用后促进更合适的胰岛素释放和更好的血糖处置。
