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ENHANCING THE DISSOLUTION RATE OF TICAGRELOR THROUGH PREPARATION WITH CYCLODEXTRINS – TABLET FORMULATION AND EVALUATION

LOREDANA-MARIA MARIN 1*, EMMA-ADRIANA OZON 2, VALENTINA ANUȚA 3, IULIAN SÂRBU 4, SÎNZIANA OPRIȚESCU 5, MARCIN SKOTNICKI 6, JANINA LULEK 6, DOINA DRĂGĂNESCU 1

1 “Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Physics, 020956, Bucharest, Romania
2 “Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Technology and Biopharmacy, 020956, Bucharest, Romania
3 “Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Physical and Colloidal Chemistry, 020956, Bucharest, Romania
4 “Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, 020956, Bucharest, Romania
5 “Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Clinical Laboratory and Food Safety, 020956, Bucharest, Romania
6 Poznan University of Medical Sciences, Faculty of Pharmacy, Industrial Pharmacy Division, Chair and Department of Pharmaceutical Technology, 60-806, Poznan, Poland

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This research investigates the effect of solid-state modification of ticagrelor (TICA) by combination with selected cyclodextrins (CDs) on the release of the active pharmaceutical ingredient from formulated tablets. Particle size distribution, flowability tests, and volumetric studies were conducted on the powders intended for compression. Based on the obtained results, new oral dosage forms utilising TICA-CD formulations were designed and evaluated. The use of TICA–CD binary systems enabled the preparation of direct compression tablets with reduced drug dosage (45 mg). It was demonstrated that the type of beta-cyclodextrin used did not significantly influence the dissolution rate. The release of the active substance from the tablets exceeded 90% after 75 minutes under conditions of varying pH. Thus, the complexation of ticagrelor with cyclodextrins resulted in significantly higher rates of active substance release. The results of the current study suggested that TICA–CD inclusion complexes can be incorporated into oral dosage forms that can subsequently be used in therapeutic practice.