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Dipyridamole Bioavailability in Subjects With Reduced Gastric Acidity

From the Department of Pharmaceutics, University of Florida, Gainesville (Dr Derendorf); Boehringer Ingelheim Pharmaceuticals, Inc, Cardiovascular & Neurology Clinical Research, Ridgefield, Connecticut (Dr VanderMaelen); Boehringer Ingelheim Pharmaceuticals, Inc, Drug Metabolism and Pharmacokinetics, Ridgefield, Connecticut (Dr MacGregor); Boehringer Ingelheim GmbH Pharmaceutical Development, Biberach, Germany (Dr Brickl); and Boehringer Ingelheim GmbH, Department of Medical Affairs, Ingelheim, Germany (Dr Eisert).

Dipyridamole (DP) is an antiplatelet agent that shows decreased oral bioavailability with increased gastric pH that occurs with commonly prescribed antacids. An extended-release (ER) formulation of DP that employs tartaric acid to improve bioavailability of DP in the presence of elevated gastric pH was developed as a combination antiplatelet product with immediate-release aspirin. This crossover-designed study examined the relative bioavailability of DP from the composite product compared to conventional DP tablets during reduced gastric acidity. Gastric pH was increased (pH > 4.0) in 20 healthy subjects with lansoprazole (30 mg/d for 5 days). Dipyridamole systemic exposure over 12 hours was compared after oral administration of a single composite ER capsule (200 mg DP + 25 mg aspirin) versus two 100-mg conventional DP tablets given 6 hours apart combined with 81 mg aspirin. DP relative bioavailability was reduced 53% with conventional tablets compared to the composite buffered ER capsule in reduced gastric acid conditions. Peak DP plasma concentrations were 57% lower with immediate-release tablets compared to the composite formulation with high stomach pH. Substituting generic DP plus low-dose aspirin may be less effective than the buffered DP composite product in patients with concomitant antacid therapies.

Key Words: Dipyridamole • elderly • gastric pH • stroke prevention • antiplatelet agents

Address for reprints: Wolfgang Eisert, MD, PhD, Boehringer Ingelheim GmbH, Department of Medical Affairs, Binger Straße 173, 55216 Ingelheim, Germany.

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