STUDIES ON THE INFLUENCE OF AMIODARONE COMPLEXATION
WITH CYCLODEXTRIN DERIVATIVES ON THE IN VITRO RELEASE
FROM MATRIX TABLETS
ANDREEA CREȚEANU1, LĂCRĂMIOARA OCHIUZ1*, CORNELIA VASILE2, MĂDĂLINA VIERIU1, GLADIOLA ŢÂNTARU1
1Faculty of Pharmacy, “Grigore T. Popa” University of Medicine and Pharmacy, 15 Universității Street, 700115, Iași,
Romania
2“Petru Poni” Institute of Macromolecular Chemistry, 41A Grigore Ghica Vodă Alley, 700487, Iași, Romania
*corresponding author: ochiuzd@yahoo.com
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Abstract:
The release of the active substance from the matrix modified-release tablets based on Kollidon® SR and chitosan is dependent
on its degree of solubility in the dissolution medium as well as on the matrix forming polymers. Through the complexation of
amiodarone hydrochloride with hydroxypropyl-β-cyclodextrin, an inclusion complex was obtained that showed an increase in
solubility by more than 200%. Matrix tablets were obtained through the direct compression method for both free and
complexed amiodarone. The two formulations were comparatively studied in terms of the release kinetics of the active
substance using in vitro release testing and the results were analysed by fitting into four representative mathematical models
for the modified release oral formulations. The release tests were conducted using a paddle apparatus 2 for a 12 hours total in
simulated gastrointestinal fluids: 2 hours at pH 1.2 and then 10 hours at pH 6.8. The released amiodarone from the studied
formulations was quantified using a validated HPLC method. Two factors have been calculated to assess the release profile
of amiodarone: f2 - the similarity factor and f1 - the difference factor. Akaike index and the correlation coefficient were the
criteria used for selecting the model that most faithfully depicted the release profile of each formulation studied.

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