al-Behaisi Samar, Antal István, Morovján György, Drabant Sándor, Plachy János, Marton Sylvia, Klebovich Imre
EGIS Gyógyszergyár Rt., Kutatási Igazgatóság, Budapest, Keresztúri út 30-38.-1106.
Acta Pharm Hung. 2002;72(3):185-90.
Food intake is known to exert numerous effects on drug pharmacokinetics through a variety of mechanisms, and for some medicinal compounds, food-drug interaction could prove of crucial clinical importance. As for acid-labile drugs, bioavailability studies performed in both fasting and fed states are considered essential. A simple and fast in vitro procedure using the USP Dissolution Apparatus II (paddle method) was applied to study acid buffering capacity of food components under simulated in vivo environment. As expected, carbohydrates (starch, sugars) and fat (oil emulsions) failed to show considerable acid buffering capacities, while protein-containing components (milk powder, gelatine) showed significant acid buffering capacity. The results of an in vitro model applying the so-called "standard meal" were in correlation with data obtained from studies performed in healthy volunteers. Nevertheless, in vitro models simulating both the fed and the fasting states in the GIT help explore factors related to food effect on drug dissolution; and consequently, achieve better insight into postprandial drug behaviour.
众所周知，食物摄入通过多种机制对药物药代动力学产生诸多影响，对于某些药物化合物而言，食物与药物的相互作用可能具有至关重要的临床意义。对于酸不稳定药物，在禁食和进食状态下进行生物利用度研究被认为是必不可少的。采用美国药典溶出度测定仪II（桨法）的简单快速体外方法，在模拟体内环境下研究食物成分的酸缓冲能力。不出所料，碳水化合物（淀粉、糖）和脂肪（油乳剂）未显示出可观的酸缓冲能力，而含蛋白质成分（奶粉、明胶）则显示出显著的酸缓冲能力。应用所谓“标准餐”的体外模型结果与健康志愿者研究获得的数据相关。然而，模拟胃肠道进食和禁食状态的体外模型有助于探索与食物对药物溶解影响相关的因素；从而更好地了解餐后药物行为。
