STABLE PHARMACEUTICAL COMPOSITION OF CLOPIDOGREL FREE BASE FOR ORAL AND PARENTERAL DELIVERY

摘要

The present invention provides a ready-to-use, oil/water emulsion composition having an average droplet size (intensity-average, nm) of 100-500 nm, wherein the oil phase is clopidogrel free base dispersed in a pharmaceutically acceptable oil(s). Includes. Emulsions use as starting material clopidogrel free base or a premix of clopidogrel free base in oil(s) and also one or more excipients such as surfactants and or co-surfactants, osmotic agents, pH adjusters, antioxidants, preservatives, sweeteners, and /Or suspending agents, etc. are contained. Emulsion formulations and their preparation methods significantly improve the stability of clopidogrel in chiral degradation, hydrolysis, and thermal degradation than other aqueous formulations (e.g., cyclotextrin-based formulations and emulsions using clopidogrel salt as starting material). Ready-to-use emulsion compositions administered orally or parenterally as a single high dose with up to 300 mg of clopidogrel are prepared and stored at room temperature for at least 19 weeks or at freezing temperature for at least 1 year. The composition provides a rapid therapeutic action as anti-platelet preparation for emergency and intensive care patients or patients unable to swallow tablet dosage forms.