Gómez-Lado Noemí, Seoane-Viaño Iria, Matiz Silvia, Madla Christine M, Yadav Vipul, Aguiar Pablo, Basit Abdul W, Goyanes Alvaro
Nuclear Medicine Department and Molecular Imaging Group, University Clinical Hospital (CHUS) and Health Research Institute of Santiago de Compostela (IDIS), 15706 A Coruña, Spain.
Department of Pharmacology, Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Santiago de Compostela (USC), Campus Vida, 15782 Santiago de Compostela, Spain.
Pharmaceutics. 2020 Jan 19;12(1):81. doi: 10.3390/pharmaceutics12010081.
Following oral administration, gastric emptying is often a rate-limiting step in the absorption of drugs and is dependent on both physiological and pharmaceutical factors. To guide translation into humans, small animal imaging during pre-clinical studies has been increasingly used to localise the gastrointestinal transit of solid dosage forms. In contrast to humans, however, anaesthesia is usually required for effective imaging in animals which may have unintended effects on intestinal physiology. This study evaluated the effect of anaesthesia and capsule size on the gastric emptying rate of coated capsules in rats. Computed tomography (CT) imaging was used to track and locate the capsules through the gastrointestinal tract. Two commercial gelatine mini-capsules (size 9 and 9h) were filled with barium sulphate (contrast agent) and coated using Eudragit L. Under the effect of anaesthesia, none of the capsules emptied from the stomach. In non-anaesthetised rats, most of the size 9 capsules did not empty from the stomach, whereas the majority of the smaller size 9h capsules successfully emptied from the stomach and moved into the intestine. This study demonstrates that even with capsules designed to empty from the stomach in rats, the gastric emptying of such solid oral dosage forms is not guaranteed. In addition, the use of anaesthesia was found to abolish gastric emptying of both capsule sizes. The work herein further highlights the utility of CT imaging for the effective visualisation and location of solid dosage forms in the intestinal tract of rats without the use of anaesthesia.
口服给药后,胃排空通常是药物吸收的限速步骤,并且取决于生理和药物因素。为了指导向人体的转化,临床前研究期间的小动物成像已越来越多地用于定位固体剂型在胃肠道中的转运。然而,与人类不同,动物有效成像通常需要麻醉,这可能对肠道生理产生意想不到的影响。本研究评估了麻醉和胶囊大小对大鼠包衣胶囊胃排空率的影响。计算机断层扫描(CT)成像用于跟踪和定位胃肠道中的胶囊。两种市售明胶微胶囊(9号和9h号)填充硫酸钡(造影剂)并用Eudragit L包衣。在麻醉作用下,没有胶囊从胃中排空。在未麻醉的大鼠中,大多数9号胶囊没有从胃中排空,而大多数较小的9h号胶囊成功从胃中排空并进入肠道。本研究表明,即使是设计用于在大鼠胃中排空的胶囊,这种固体口服剂型的胃排空也不能保证。此外,发现使用麻醉会消除两种胶囊大小的胃排空。本文的工作进一步突出了CT成像在不使用麻醉的情况下有效可视化和定位大鼠肠道中固体剂型的实用性。