Effects of buffered and plain acetylsalicylic acid formulations with and without ascorbic acid on gastric mucosa in healthy subjects.
BACKGROUND
The most frequently reported adverse events associated with acetylsalicylic acid intake are minor gastrointestinal complaints. Galenic modifications, such as buffered formulations with or without ascorbic acid, may improve the benefit-risk ratio by decreasing the local mucosal side-effects of acetylsalicylic acid.


OBJECTIVE
To assess endoscopically-proven gastrointestinal lesions and the amount of gastric microbleeding of four different buffered and plain acetylsalicylic acid formulations, one containing paracetamol.


METHODS
A randomized, four-fold cross-over study was performed in 17 healthy subjects who underwent serial oesophago-gastro-duodenoscopy before and after each course of 4-day dosing. Gastric aspirates were collected for the determination of haemoglobin concentrations to detect microbleeding.


RESULTS
Buffered acetylsalicylic acid plus ascorbic acid yielded the lowest Lanza score, the lowest increase in the number of mucosal petechiae and the lowest increase in the amount of gastric microbleeding. Subjects receiving acetylsalicylic acid plus paracetamol plus caffeine showed the highest Lanza score of all treatments, and a considerably greater sum of petechiae in the oesophagus, stomach and duodenum compared with those receiving buffered acetylsalicylic acid plus ascorbic acid.


CONCLUSIONS
The trial confirms that buffering of acetylsalicylic acid improves local gastric tolerability. Acetylsalicylic acid in combination with ascorbic acid shows significantly fewer gastric lesions and the lowest increase in gastric microbleeding compared with the other tested formulations.
Klinische Forschung Hamburg, Hamburg, Germany. ammann@kfhh.de
H-G
HG
Dammann
M
M
Saleki
M
M
Torz
H-U
HU
Schulz
S
S
Krupp
M
M
Schürer
J
J
Timm
U
U
Gessner
D000328:Adult; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000009:adverse effects*; D000975:Antioxidants / Q000008:administration & dosage*; D001205:Ascorbic Acid / Q000008:administration & dosage*; D001241:Aspirin / Q000008:administration & dosage / Q000009:adverse effects*; D018592:Cross-Over Studies; D005260:Female; D005753:Gastric Mucosa; D006471:Gastrointestinal Hemorrhage / Q000139:chemically induced*; D006801:Humans; D008297:Male; D011446:Prospective Studies; D012307:Risk Factors; D013272:Stomach Diseases / Q000139:chemically induced*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000975:Antioxidants; D001205:Ascorbic Acid; D001241:Aspirin