Key result
Oral anticoagulants face absorption challenges due to high molecular weight and hydrophilicity, making novel formulation approaches promising for long-term therapy.
Highlights the challenges of oral anticoagulant formulation due to molecular weight and hydrophilicity, and the need for new formulation approaches.
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May limit long-term oral anticoagulant effectiveness; leaves open whether novel formulations will translate to clinical benefit.
Anticoagulation remains the therapy of choice for the prevention and treatment of venous and arterial thromboembolic disorders which can cause major organ damage or death. Heparins represent the antithrombotic drugs of choice in short and medium-term prophylaxis and therapy of thromboembolic diseases. Fondaparinux, a synthetic and structural analog of the antithrombin-binding pentasaccharide domain of heparin, has selective anti-Xa activity and longer half-life. However, anticoagulants are poorly absorbed by oral route because of their high molecular weight, hydrophilicity and negative charges. Long-term anticoagulation therapy is problematic because of side effects and frequent monitoring. Formulation approaches are particularly promising.
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Ralay-Ranaivo et al. (2015) conducted a review in Venous and arterial thromboembolic disorders. Oral Anticoagulants was evaluated. Oral anticoagulants face absorption challenges due to high molecular weight and hydrophilicity, making novel formulation approaches promising for long-term therapy.
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