Murray F E, Hudson N, Atherton J C, Cole A T, Scheck F, Hawkey C J
Department of Therapeutics, University Hospital, Nottingham.
Gut. 1996 Jan;38(1):11-4. doi: 10.1136/gut.38.1.11.
Calcium carbasalate is a therapeutically active salicylate which seems to cause less gastroduodenal mucosal damage than aspirin in laboratory animals. This endoscopist-blinded, randomised, cross over trial aimed to compare acute gastric mucosal damage in 20 healthy volunteers treated with acetyl salicylic acid (ASA) (650 mg three times daily) and effervescent calcium carbasalate (ECC) (826.8 mg three times daily) bioequivalent to 650 mg ASA over a five day period. Endoscopy was performed immediately before treatment and on day 5 of each treatment. Serum salicylate, thromboxane B2, and gastric mucosal prostaglandin E2 (PGE2) concentrations were measured after endoscopy. ECC caused fewer gastric mucosal erosions than ASA. The total number of gastric erosions was 23.8 (16.1) in the ASA treated subjects compared with 9.1 (8.7) in ECC treated subjects (p = 0.004). Differences between ASA and ECC were significant for both the gastric antrum and body, and for both haemorrhagic and non-haemorrhagic erosions. The mean gastric body Lanza score for mucosal damage was lower after ECC than ASA (p = 0.003). The visual analogue score for gastric body damage was lower for ECC (16.9 mm (15.9)) than for ASA (32.7 mm (20.8)), p = 0.008. Serum salicylate concentrations were similar after both preparations (ASA: 66 (23) mg/l, versus ECC: 58 (17) mg/l, NS). Serum thromboxane B2 was similarly reduced using both preparations-97.2 (3.5)% inhibition with ASA, 95.2 (5.5)% inhibition with calcium carbasalate (NS). Suppression of gastric mucosal PGE2 synthesis was similar with both preparations (ASA: 83.4 (17.1)%; ECC 84.3 (12.9)%; NS). It is concluded that ECC causes significantly less gastroduodenal mucosal damage than ASA administered at bioequivalent doses as judged by serum salicylate, serum thromboxane, and mucosal PGE2 values. ECC may therefore be a less harmful alternative treatment to plain ASA.
卡巴匹林钙是一种具有治疗活性的水杨酸盐，在实验动物中，它对胃十二指肠黏膜的损伤似乎比阿司匹林要小。这项由内镜检查人员盲法操作的随机交叉试验旨在比较20名健康志愿者在5天内服用乙酰水杨酸（ASA）（650毫克，每日三次）和泡腾卡巴匹林钙（ECC）（826.8毫克，每日三次，生物等效于650毫克ASA）后急性胃黏膜损伤的情况。在每次治疗前及治疗第5天进行内镜检查。内镜检查后测量血清水杨酸、血栓素B2和胃黏膜前列腺素E2（PGE2）的浓度。ECC导致的胃黏膜糜烂比ASA少。ASA治疗组的胃糜烂总数为23.8（16.1）处，而ECC治疗组为9.1（8.7）处（p = 0.004）。ASA和ECC之间在胃窦和胃体、出血性和非出血性糜烂方面的差异均具有显著性。ECC治疗后胃体黏膜损伤的平均兰扎评分低于ASA（p = 0.003）。ECC的胃体损伤视觉模拟评分为16.9毫米（15.9），低于ASA的32.7毫米（20.8），p = 0.008。两种制剂后的血清水杨酸浓度相似（ASA：66（23）毫克/升，ECC：58（17）毫克/升，无显著性差异）。两种制剂对血清血栓素B2的降低程度相似——ASA抑制97.2（3.5）%，卡巴匹林钙抑制95.2（5.5）%（无显著性差异）。两种制剂对胃黏膜PGE2合成的抑制作用相似（ASA：83.4（17.1）%；ECC：84.3（12.9）%；无显著性差异）。结论是，根据血清水杨酸、血清血栓素和黏膜PGE2值判断，ECC导致的胃十二指肠黏膜损伤明显少于生物等效剂量的ASA。因此，ECC可能是比普通ASA危害更小的替代治疗药物。
