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OPTIMIZATION OF SOLUBILITY OF AMIODARONE HYDROCHLORIDE THROUGH COMPLEXATION WITH HYDROXYPROPYL-?-CYCLODEXTRIN

Andreea Crețeanu

Abstract

Amiodarone (AMD) is an antiarrhythmic agent used for the treatment of ventricular arrhythmias, arterial fibrillation, and severe rhythm disorders. The main therapeutic disadvantage of AMD is its low oral bioavailability and low water solubility. The aim of the study was to obtain the hydroxylpropyl-?-cyclodextrin/AMD inclusion complex and to assess its degree of drug loading using a new HPLC method. The solubilizing effect of cyclodextrin on AMD was evaluated by the phase solubility method. The concentration of AMD was determined by UV-VIS spectroscopy at a wavelength of 254 nm. The assessment of the structural and morphological properties of the inclusion complex was done through various methods: Differential Calorimetry on a NETZSCH DSC200F3 apparatus and FT-IR spectroscopy using the KBr encapsulation technique. The pharmacokinetic characterization of the HP-?-CD/AMD inclusion complex was achieved using in vitro dissolution test on a Dissolution test station SR8 Plus Series apparatus according to the following protocol: 500 mL dissolution medium, pH = 1.2 (HCl 0.1N) 0-2h; pH = 6.8 (phosphate buffer) 2-72h; pH = 5.5 and pH = 7.4; paddle speed: 50 rpm; 37В±0.2В°C. The samples were analyzed using the validated HPLC method. The evaluation of the kinetics of HP-?-CD/AMD inclusion complex was achieved by fitting the data by linear or non-linear progression using the SPSS16 and Matlab 7 software. The Akaike Index (AIC) and the R2 correlation coefficient were the criteria for selecting the model that best described the release profile.

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DOI resolver: doi.org/10.5593/sgem2018/6.1/s24.051

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