Abstract
Low-dose aspirin represents the best option in the secondary prevention of coronary artery disease, but its extensive use in primary prevention is limited by the occurrence of gastric mucosal lesions and increased risk of bleeding. We investigated the safety profile of a novel sublingual aspirin formulation in 200 healthy volunteers, randomly assigned to ten (n = 20 each) different 7-day once-daily treatment regimens. Gastric mucosal injury based on the modified Lanza score (MLS), the histopathology of gastric mucosa and the serum determination of thromboxane B2 (TXB2) and urinary 11-dehydro-TXB2 levels were evaluated at basal as well as after 7 days of each placebo or aspirin treatment regimen. In Groups A and B (placebo—oral and sublingual, respectively), no changes in MLS and in gastric mucosal micro-vessel diameter were found at day 7. In contrast, in Groups C and D (oral standard aspirin—100 and 50 mg daily, respectively), the median MLS was significantly increased. Very few changes were found in Groups E and F (standard sublingual aspirin—100 and 50 mg, respectively). Groups G and H (oral administration of micronized collagen-cogrinded aspirin) showed gastric protection compared to Groups C and D. Moreover, Groups I and L (sublingual collagen-cogrinded aspirin—100 and 50 mg, respectively) showed a significant reduction (Group I) or total abolition (Group L) of gastric mucosal lesions and no difference compared to the standard one in serum TXB2 and urinary 11-dehydro-TXB2 levels. In conclusion, our data show that the new formulation leads to a better safety profile compared to standard aspirin, representing a better therapeutic option for extended use in primary and secondary prevention of cardiovascular diseases.
Highlights
IntroductionAspirin is the most successful drug in history
We developed and tested a new aspirin formulation based on an original process, which includes micronization and cogrinding with collagen of its crystalline form, thereby achieving a better drug absorption associated with significant protection of gastric mucosa [18]
We found that the severity of the aspirin-induced ulceration of the gastric mucosa was reduced when aspirin was cogrinded with collagen, an effect confirmed by histopathological studies [18]
Summary
Aspirin is the most successful drug in history. It was discovered over a hundred years ago, and, one billion tablets are consumed every year worldwide. Evidence has been collected showing that low-dose aspirin may play a crucial role in the secondary prevention of both cardiovascular and cerebrovascular diseases [1,2,3]. Due to its direct, as well as indirect, damaging effect on gastric mucosa, the occurrence of aspirin-related peptic ulcers is increasing [4,5,6], and upper intestine bleeding still represents a major issue in patients chronically using aspirin. Due to its direct, as well as indirect, damaging effect on gastric mucosa, the occurrence of aspirin-related peptic ulcers is increasing [4,5,6], and upper intestine bleeding still represents a major issue in patients chronically using aspirin. 4.0/).
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