Preparation, Characterization and Dissolution Test of an Inclusion Complex of Atorvastatin in β-Cyclodextrin

Radia      Ouarezki; Moulay-Hassane      Guermouche

Abstract

Inclusion complex of Atorvastatin (ATR) in β-cyclodextrin (β-CD) was prepared using co-evaporating technique. Characterization of the complex was carried out by the solubility method, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), 1H, 13C and fluorine nuclear resonance spectrometry (NMR). It was testified that the inclusion complex was formed between βCD and ATR. The stability constant K1:1 and the 1:1 steochiometry of complexation were determined. 1H, 13C and fluorine NMR analysis confirmed the inclusion and to provide information on the behavior of ATR inside the cavity of βCD. The dissolution rate of ATR/β-CD complex prepared by the co-evaporating technique was investigated and compared with this of the pure drug. Analysis of the dissolution samples was made by reversed phase liquid chromatographic method. The overall results showed that the dissolution rate of ATR/β-CD was significantly higher compared to the free ATR.

Keywords: Atorvastatin, β-cyclodextrin, Inclusion complex, Solubility, Characterization dissolution test