Replacing the acetyl linkage in aspirin with choline and magnesium moieties reduces the occurrence of gastric mucosal injury.
Aliment Pharmacol Ther
; 1(1): 51-6, 1987 Feb.
Article
in En
| MEDLINE
| ID: mdl-2979212
ABSTRACT
The acetyl moiety in aspirin (acetyl salicylic acid ASA) is considered to play a major part in the pathogenesis of ASA-induced mucosal injury. At equivalent salicylate doses and pH values, the induction of acute gastric mucosal haemorrhagic erosions in rats by ASA and choline magnesium trisalicylate (CMT), a new non-acetylated salicylate, with and without the potentiating damaging effect of taurodeoxycholic acid (TDCA) were compared. Test solutions were administered by per oral intubation to five groups of fasting Sprague-Dawley rats (n = 24). Gastric mucosa were examined after 4 hours and mucosal injury assessed by a lesion-scoring system. The incidence and severity (median lesion scores with quartiles) of the lesions were 83% and 13 (720) respectively for ASA (128 mg kg-1) compared with 17% and 0 (00) for CMT (128 mg kg-1) (P less than 0.001 and P less than 0.001). TDCA increased mucosal damage to 100% and 29 (2034) for ASA compared with 30% and 0 (04) for CMT (P less than 0.001) and P less than 0.001). Serum salicylate levels (median values of 1.4 for ASA and 1.5 mmol litre-1 for CMT) were not significantly different. It is concluded that replacing the acetyl moiety in ASA with choline and magnesium moieties reduces the ASA-induced mucosal injury, without affecting blood salicylate concentrations.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Stomach Ulcer
/
Salicylates
/
Anti-Inflammatory Agents, Non-Steroidal
/
Choline
/
Gastric Mucosa
Limits:
Animals
Language:
En
Journal:
Aliment Pharmacol Ther
Journal subject:
FARMACOLOGIA
/
GASTROENTEROLOGIA
/
TERAPIA POR MEDICAMENTOS
Year:
1987
Type:
Article