Oral composition containing an antiplatelet agent of the thienopyridine family in the form of free base

摘要

The invention relates to non hemolytic compositions containing an antiplatelet agent such as clopidogrel or ticlopidine; these compositions being characterized in that the antiplatelet agent is in the form of free base, and the composition contains at least one hydrophilic non ionic surfactant. The invention relates also a galenic form, a method of preparation of thereof, as well as therapeutic uses of thereof, especially in patients who suffer from undesirable effects related to hemolysis and/or gastrointestinal acidity.

主权项

1. An oral, non-hemolytic, oily liquid, pharmaceutical formulation comprising the oily liquid, free base form of clopidogrel, as an antiplatelet agent, dissolved in at least one hydrophilic non-ionic surfactant selected from the group consisting of macrogolglycerol ricinoleate, macrogolglycerol hydroxystearate, macrogol 15 hydroxystearate, and a mixture of macrogolglycerol hydroxystearate and vitamin E/polyethylene glycol succinate, said formulation having a pH close to neutrality after dilution in water, lacking of food effect and without gastric irritation, and the solubility of the clopidogrel in the formulation is greater than 70 mg/ml in a simulated intestinal fluid according to the pharmacopeia USP XXI at pH 7.5 and at 37° C.