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
1University of Medicine and Pharmacy “Carol Davila” Bucharest, Faculty of Pharmacy, Department of Drug Control, 6 Traian Vuia street, 020956, Bucharest, Romania
2University 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
3University of Medicine and Pharmacy “Carol Davila” Bucharest, Faculty of Pharmacy, Department of Drug Industry and Pharmaceutical Biotechnologies, 6 Traian Vuia street, 020956, Bucharest, Romania
4University of Medicine and Pharmacy “Carol Davila” Bucharest, Faculty of Pharmacy, Department of Pharmaceutical Technology and Biopharmaceutics, 6 Traian Vuia street, 020956, Bucharest, Romania
5University of Medicine and Pharmacy “Carol Davila” Bucharest, Faculty of Pharmacy, Department of Toxicology, 6
Traian Vuia street, 020956, Bucharest, Romania
6University of Medicine and Pharmacy “Carol Davila” Bucharest, Faculty of Pharmacy, Department of Pharmaceutical Physics and Informatics, 6 Traian Vuia street, 020956, Bucharest, Romania
*corresponding author: flavian.radulescu@umf.ro
DownloadDownload Full Article

Abstract:
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.






Top