Stability studies on steroidal drug/β-cyclodextrin kneaded systems

Abstract 6-Methylenandrosta-1,4-diene-3,17-dione (FCE24304), an aromatase inhibitor, is characterised not only by poor solubility in aqueous media and slow dissolution rate, but also by low chemical stability due to possessing conjugate double bonds. Several approaches have already been evaluated for improving both the biopharmaceutical properties and chemical stability of drugs in a particular way by the use of β-cyclodextrin. An accelerated short-term stability study on FCE24304β-cyclodextrin kneaded systems, prepared using two different molar ratios, was carried out and the systems evaluated by HPLC, DSC and X-ray difiractometry techniques and correlated with dissolution rate behaviour. A tablet formulation with a 1:2 molar ratio of the FCE24304/β-cyclodextrin complex is now under development.