Romanian Society of Pharmaceutical Sciences
 

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IN VITRO SCREENING OF ALCOHOL-INDUCED DOSE DUMPING PHENOMENA FOR CONTROLLED RELEASE TRAMADOL TABLETS

GEORGE TRAIAN ALEXANDRU BURCEA DRAGOMIROIU1, OCTAV GINGHINĂ2, FLAVIAN ȘTEFAN RĂDULESCU3*, DUMITRU LUPULEASA4, MARIA BÂRCĂ1, DANIELA ELENA POPA1, CAROLINA NEGREI5, DALIA SIMONA MIRON6

1.University of Medicine and Pharmacy “Carol Davila” Bucharest, Faculty of Pharmacy, Department of Drug Control, 6 Traian Vuia street, 020956, Bucharest, Romania
2.University of Medicine and Pharmacy “Carol Davila” Bucharest, Faculty of Dental Medicine, Department of Oncological Surgery, “Sf. Ioan” Hospital, 13 Vitan-Bârzești street, 042122, Bucharest, Romania
3.University of Medicine and Pharmacy “Carol Davila” Bucharest, Faculty of Pharmacy, Department of Drug Industry and Pharmaceutical Biotechnologies, 6 Traian Vuia street, 020956, Bucharest, Romania
4.University of Medicine and Pharmacy “Carol Davila” Bucharest, Faculty of Pharmacy, Department of Pharmaceutical Technology and Biopharmaceutics, 6 Traian Vuia street, 020956, Bucharest, Romania
5.University of Medicine and Pharmacy “Carol Davila” Bucharest, Faculty of Pharmacy, Department of Toxicology, 6 Traian Vuia street, 020956, Bucharest, Romania
6.University of Medicine and Pharmacy “Carol Davila” Bucharest, Faculty of Pharmacy, Department of Pharmaceutical Physics and Informatics, 6 Traian Vuia street, 020956, Bucharest, Romania

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The aim of the study was to evaluate the influence of ethanol content in acidic media on the in vitro release of tramadol hydrochloride from controlled release tablets. The selected products represented both hydrophilic and lipid-based monolithic systems, covering a wide range of dose strengths with various similarity degrees of the qualitative composition. The results confirmed the inhibition of release by gradually increasing the ethanol proportion up to 40% (v/v). The reduced hydration of the macromolecular agents and consequent increased diffusional resistance were suggested as the leading causes of this phenomenon. In vitro release similarity was observed between the different strengths of the same product, as well as between reference listed drug and generics, for the same media. The critical conditions simulated by the upper level of alcohol content minimized the impact of composition and manufacturing variables. Irrespective of media composition, strength and hydrolipophilic nature of the matrix, the kinetic model adequately describing the experimental data was preserved.