Davis S S, Hardy J G, Fara J W
Gut. 1986 Aug;27(8):886-92. doi: 10.1136/gut.27.8.886.
The gastrointestinal transit of pharmaceutical dosage forms has been measured in 201 studies in normal subjects using gamma scintigraphy. Solutions, small pellets, and single units (matrix tablets and osmotic pumps) were administered with different amounts of food in the stomach, ranging from fasted state to heavy breakfast. Gastric emptying was affected by the nature of the dosage form and the presence of food in the stomach. Solutions and pellets were emptied even when the stomach was in the digestive mode, while single units were retained for long periods of time, depending on the size of the meal. In contrast, measured intestinal transit times were independent of the dosage form and fed state. The small intestinal transit time of about three hours (mean +/- 1 h SEM) has implications for the design of dosage forms for the sustained release of drugs in specific positions in the gastrointestinal tract.
在201项针对正常受试者的研究中,采用γ闪烁扫描法测定了药物剂型的胃肠道转运情况。溶液剂、小丸剂和单一单元制剂(骨架片和渗透泵)在胃中与不同量的食物一起给药,范围从禁食状态到丰盛早餐。胃排空受剂型性质和胃中食物存在情况的影响。即使胃处于消化模式,溶液剂和小丸剂也会排空,而单一单元制剂会根据餐量大小长时间滞留。相比之下,测得的肠道转运时间与剂型和进食状态无关。约三小时(平均值±1小时标准误)的小肠转运时间对胃肠道特定部位药物缓释剂型的设计具有启示意义。