Palacios G, Castell O, Colombo M, Roser R, Esteve J
Laboratorios Dr. Esteve, S.A., Barcelona, Spain.
Methods Find Exp Clin Pharmacol. 1987 Jun;9(6):353-70.
In this histological study it has been demonstrated that a single-dose administration of piroxicam, at the same dosage (4 mg/kg) as droxicam, has a greater erosive potential on the gastric mucosa of rats later exposed to cold stress. For this purpose the depth of all lesions found was evaluated by light microscopy and results showed that piroxicam produces lesions deeper and more numerous than those of droxicam. The transmission and scanning electron microscopic studies showed that the lesive mechanism was very similar for both drugs and that both local and general factors induced by these drugs and stress come into play. Absorption or penetration and uptake by the cells of the mucosa have been considered among the most important local factors in the development of erosive gastric lesions caused by non-steroid anti-inflammtaory drugs. As this absorption is in direct relation to the depth of the lesions, it can be considered from the results of this study that the lesser lesive effect of droxicam on the gastric mucosa when compared to that of piroxicam is due to the fact that, owing to its hydrolysis to piroxicam the absorption rate is slower.
在这项组织学研究中,已证实单剂量给予吡罗昔康,剂量与屈昔康相同(4毫克/千克),对随后遭受冷应激的大鼠胃黏膜具有更大的侵蚀潜力。为此,通过光学显微镜评估所发现的所有损伤的深度,结果表明吡罗昔康产生的损伤比屈昔康更深且更多。透射电子显微镜和扫描电子显微镜研究表明,两种药物的损伤机制非常相似,并且这些药物和应激所诱导的局部和全身因素均起作用。黏膜细胞的吸收、渗透和摄取被认为是由非甾体类抗炎药引起的糜烂性胃损伤发展过程中最重要的局部因素之一。由于这种吸收与损伤深度直接相关,从本研究结果可以认为,与吡罗昔康相比,屈昔康对胃黏膜的损伤作用较小是由于其水解为吡罗昔康的过程中吸收速率较慢。