Ryrfeldt A, Norbeck K, Reiland S, Moldéus P
Department of Toxicology, Karolinska Institutet, Stockholm, Sweden.
Acta Physiol Scand Suppl. 1990;592:73-82.
This paper describes an in vitro method of studying the esophago-irritant potential of oral formulations of drugs. Porcine esophagus was used. The method offers the possibility of studying muscle activity and enzyme leakage (e.g. LDH) and of performing histomorphology of the exposed preparations. Examples of drugs which were tested are alprenolol (Aptin), propranolol (Inderal), doxycycline (Idocyklin) and (Vibramycin) and emepronium bromide (Cetiprin). Concerning effects on muscle activity, Aptic caused a marginal contraction while Cetiprin caused a relaxation of the esophagus preparation. Increased LDH-leakage was noted during exposure with the above mentioned pills in comparison with concurrent control preparations. Histopathological examination disclosed morphological changes such as softening and necrosis of the squamous epithelium of the esophageal mucosa after exposure to drugs like Idocyklin and Aptin.
本文描述了一种研究药物口服制剂食管刺激潜力的体外方法。使用了猪食管。该方法提供了研究肌肉活动和酶泄漏（如乳酸脱氢酶）以及对暴露制剂进行组织形态学研究的可能性。所测试药物的例子有阿普洛尔（心得静）、普萘洛尔（心得安）、多西环素（强力霉素）和（威霸霉素）以及溴美喷铵（西替普明）。关于对肌肉活动的影响，心得静引起轻微收缩，而西替普明导致食管制剂松弛。与同时进行的对照制剂相比，在接触上述药丸期间观察到乳酸脱氢酶泄漏增加。组织病理学检查显示，在接触强力霉素和心得静等药物后，食管黏膜鳞状上皮出现软化和坏死等形态学变化。
