Influence of Food on the Bioavailability of Drugs
Influence of Food on the Bioavailability of Drugs
复制标题
食物对药物生物利用度的影响
DOI：
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发表时间：
1978
影响因子：
4.5
通讯作者：
A. Melander
中科院分区：
文献类型：
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作者：
A. Melander
食物摄入对药物的生物利用度有着复杂的影响。它不仅可能干扰片剂崩解、药物溶出和药物通过胃肠道的转运，还可能影响药物在胃肠道壁和肝脏中的代谢转化。不同的食物成分可能会产生不同的效果，食物可能会以相反的方式相互作用，甚至与化学相关的药物也是如此。因此，食物对药物生物利用度的净影响只能通过直接的临床研究来预测。主要从单餐、单剂量研究判断，食物摄入可提高几种不同药物的生物利用度，如普萘洛尔、美托洛尔、肼屈嗪、氢氯噻嗪、坎利酮（来自螺内酯）、呋喃妥因、红霉素（硬脂酸盐）、双香豆素、苯妥英和卡马西平，但降低了诸如异烟肼、利福平、四环素、青霉素和氨苄青霉素的药物的含量，而对甲硝唑、奥沙西泮、美哌隆、丙基硫氧嘧啶、磺胺嘧啶和磺脲类药物的生物利用度没有一致的影响。对于某些药物，如地高辛和扑热息痛，吸收速率降低，但吸收程度不降低;食物可以提高生物利用度，即使胃排空速率降低，或者更确切地说，因为胃排空速率降低;这显然是氢氯噻嗪和呋喃妥因的情况。食物诱导的普萘洛尔、美托洛尔和肼屈嗪的生物利用度增加可能是由于这些药物的首过代谢减少，而食物诱导的药物溶出度增加可能解释了卡马西平、坎利酮、双香豆素和苯妥英的生物利用度增加。胃肠道pH值升高可能是食物引起的药物生物利用度降低的部分原因，如异烟肼和四环素。除了单餐效应外，重复摄入富含蛋白质的膳食增强了安替比林和茶碱的氧化速率，而富含碳水化合物的膳食降低了安替比林和茶碱的氧化速率。此外，木炭烤肉的摄入显著加速非那西丁的氧化，而茶碱的摄入加速茶碱的消除。因此，食物及其成分和污染物可能对影响药物全身利用度的吸收和生物转化过程产生短期和长期影响。
Food intake exerts a complex influence on the bioavailability of drugs. It may interfere not only with tablet disintegration, drug dissolution and drug transit through the gastrointestinal tract, but may also affect the metabolic transformation of drugs in the gastrointestinal wall and in the liver. Different food components can have different effects, and food may interact in opposite ways, even with drugs that are chemically related. Therefore, the net effect of food on drug bioavailability can be predicted only by direct clinical studies of the drug in question.As judged mainly from single meal, single dose studies, food intake enhances the bioavailability of several different drugs, such as propranolol, metoprolol, hydrallazine, hydrochlorothiazide, canrenone (from spironolactone), nitrofurantoin, erythromycin (stearate), dicoumarol, phenytoin and carbamazepine, but reduces that of drugs such as isoniazid, rifampicin, tetracycline, penicillin and ampicillin, while having no consistent effect on the bioavailability of metronidazole, oxazepam, melperone, propylthiouracil, sulphasomidine and sulphonylureas. For some drugs such as digoxin and paracetamol, the rate but not the extent of absorption is reduced.Food may enhance bioavailability even though, or rather because, the rate of gastric emptying is reduced; this is apparently the case with hydrochlorolhiazide and nitrofurantoin. The food induced enhancement of bioavailability of propranolol, metoprolol and hydrallazine is probably due to reduced first pass metabolism of these drugs, while food induced improvement of drug dissolution may explain the enhanced bioavailability of carbamazepine, canrenone, dicoumarol and phenytoin. An increased gastrointestinal pH may be in part the cause of the food induced reduction of the bioavailability of drugs such as isoniazid and tetracycline.In addition to single meal effects, repeated intake of protein-rich meals enhance, while carbohydrate-rich meals reduce, the rate of oxidation of antipyrine and theophylline. Moreover, intake of charcoal broiled meat markedly accelerates the oxidation of phenacetin and variably accelerates elimination of theophylline. Thus, food and its components and contaminants may have both short and long term effects on both the absorptive and biotransformation processes influencing systemic availability of drugs.