Mielants H, Veys E M, Verbruggen G, Schelstraete K
Clin Rheumatol. 1984 Mar;3(1):47-54. doi: 10.1007/BF02715695.
Gastrointestinal fecal blood loss, determined by injecting 51Cr-labelled autologous red blood cells, was measured in 191 orthopaedic patients after oral or parenteral intake of different forms of acetylsalicylates or salicylates. Oral or parenteral administration of non-acetylated salicylates caused nearly no gastrointestinal bleeding, but the anti-inflammatory activity of these products can be questioned since they cannot inhibit prostaglandin synthetase. Buffered, soluble forms of acetylsalicylates caused gastrointestinal bleeding in more than 50% of the patients. However, enteric-coated and intravenous forms resulted in significantly less gastrointestinal bleeding. For both preparations a relationship between serum salicylate level and amount of fecal blood loss was found in the group of "bleeders" (an upper limit of physiological blood loss could definitely be determined by this method). The findings suggested a similar mode of action of enteric-coated and intravenous acetylsalicylates on gastric mucosa through a systemic action. It was concluded that in long-term anti-inflammatory salicylate treatment, enteric-coated forms are probably the galenic form of first choice.
通过注射51Cr标记的自体红细胞来测定胃肠道粪便失血情况,在191名骨科患者口服或肠胃外摄入不同形式的乙酰水杨酸酯或水杨酸酯后进行了测量。口服或肠胃外给予非乙酰化水杨酸酯几乎不会引起胃肠道出血,但这些产品的抗炎活性可能受到质疑,因为它们无法抑制前列腺素合成酶。缓冲的、可溶形式的乙酰水杨酸酯在超过50%的患者中导致胃肠道出血。然而,肠溶包衣和静脉注射形式导致的胃肠道出血明显较少。对于这两种制剂,在“出血者”组中发现血清水杨酸水平与粪便失血量之间存在关联(通过这种方法肯定可以确定生理性失血的上限)。研究结果表明,肠溶包衣和静脉注射的乙酰水杨酸酯通过全身作用对胃黏膜的作用方式相似。得出的结论是,在长期抗炎水杨酸酯治疗中,肠溶包衣形式可能是首选的药剂形式。