THERMAL STABILITY ASSESMENT OF AMIODARONE HYDROCHLORIDE IN POLYMERIC MATRIX TABLETS
ANDREEA CREȚEANU1, LĂCRĂMIOARA OCHIUZ1*, CORNELIA VASILE2, OANA MARIA PĂDURARU2, CRISTINA POPESCU2, MĂDĂLINA VIERU1, ALINA DIANA PANAINTE1, GLADIOLA ȚÂNTARU1
1.Faculty of Pharmacy, “Gr. 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
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Amiodarone, an antiarrhythmic agent with low bioavailability caused by its low water solubility, is currently used in the form of conventional release tablets (200 mg/tablet). In order to develop new solid oral dosage forms with prolonged release, we analysed the stability of pure amiodarone and amiodarone complexed with hydroxypropyl-β-cyclodextrin (HP-β-CD), in association with matrix forming agents (Kollidon®SR and chitosan), during direct compression. The stability assessment and the identification of potential interactions between amiodarone and the auxiliary substances were established by spectrophotometric and thermal analysis. The thermal profile of the tablet formulation containing amiodarone and excipients (abbreviated F1) showed the conservation of the crystalline form of the active substance following direct compression. In the thermogram of the formulation containing complexed amiodarone (abbreviated F10), the melting point of the crystalline form disappeared, which indicated the amorphous nature of the active substance caused by its interactions with the polymers. FTIR spectra for the two tablet formulations revealed characteristic bands of the tertiary amine bond in the amiodarone structure. The band attributed to the aromatic C=C bond stretching is frequently displaced/bent in the presence of excipients, due to the interactions between amiodarone and polymers. The complete disappearance of the absorption bands characteristic of amiodarone (2580 - 2455 cm-1) in the FT-IR spectrum for the formulation with the inclusion complex showed the formation of chemical bonds between the OH groups of HP-β-CD and the tertiary amine of the active substance.