Romanian Society of Pharmaceutical Sciences
 

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RESEARCH CONCERNING THE DEVELOPMENT OF A STABLE, FIXED COMBINATION OF ASPIRINE, PARACETAMOL, CAFFEINE AND AN ANTIALERGIC COMPONENT

VICTOR VOICU 1, CONSTANTIN MIRCIOIU 2, VALENTINA ANUȚA 3*, LOREDANA ANDREEA VONICA 4, ION MIRCIOIU 4

1.Department of Clinical Pharmacology and Toxicology, Faculty of Medicine, “Carol Davila” University of Medicine and Pharmacy, Bucharest, Romania
2 .Doctoral School, “Carol Davila” University of Medicine and Pharmacy, Bucharest, Romania
3 .Department of Physical Chemistry, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, Bucharest, Romania
4 .Department of Research and Development, Polisano Pharmaceuticals, Sibiu, Romania

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The multitude of analgesic combinations based on the synergic effect of acetylsalicylic acid, paracetamol and caffeine have in common the problem of irritative adverse effects and relative low stability. Addition of chlorpheniramine to this classical combination allowed the reduction of the usual dosage and consequently of the gastrointestinal adverse effects. The present paper aims to evaluate the stability of the quaternary combination, in both powder and tablet form. A preliminary study was performed in order to evaluate the stability of all combinations of components as well as the compatibility of the active pharmaceutical ingredients with different tableting excipients. The results allowed the development at industrial scale of a new formulation containing 125 mg acetylsalicylic acid, 75 mg acetaminophen, 15 mg caffeine and 2 mg chlorpheniramine combination. Further studies concerning the evaluation of the stability of the selected formula under International Conference on Harmonization accelerated, intermediate and real-time storage conditions (over 36 months) put in evidence that acetylsalicylic acid is the only component that presented a significant concentration decrease. Time to decreasing of acetylsalicylic acid content to 90% was found to be 41 months.