RELEASE OF KETOPROFEN FROM AQUEOUS SYSTEM S IN THE PRESENCE OF HYDROPHILIC BETA-CYCLODEXTRIN DERIVATIVES

Nonsteroidal antiinflammatory drugs (NSAID) are often characterised by a low water solubility. Possible partners for complexation inducing a n increase of the solubility may be cyclodextrins and their derivative s. By using hydrophilic beta-cyclodextrin derivatives for inclusion of ketoprofen the solubility is increased by 1500 times. The stability o f the drug in these preparations is often higher than in aqueous solut ion. Only preparations which are physical mixtures of ketoprofen and h ydroxypropyl-beta-cyclodextrin show a decrease of the drug stability. In case of mechanical separation of the two compartments, drug liberat ion of cyclodextrin containing systems shows a linear relationship bet ween the amount of liberated drug and the square root of time. If a di alysis membrane is used for separation, a linear relationship exists b etween the quantity of liberated drug and the time. With excised human skin as separating membrane drug release is furthermore reduced. Thus dermal application does not seem promising.