Cyclodextrins are torus-shaped molecules with a hydrophilic outer surface and a lipophilic central cavity. Due to their unique spatial configuration, they can form inclusion complexes with a variety of lipophilic drugs, thus favourably affecting many physicochemical properties, such as their solubility and stability. Therefore the importance of cyclodextrins as excipients in pharmaceutical formulations is always increasing [1]. However, due to their relatively low complexation efficiency, it often happens that larger amounts of carrier should be used than those actually employable in many drug formulations. Therefore it is important to find methods for enhancing the cyclodextrin complexation efficiency, by making possible less carrier can be used to achieve the same favourable effect. Recent works reported the positive effect of the addition of a suitable third component on the complexation efficiency of cyclodextrins [1]. We previously showed that the solubility of naproxen (NAP), non-steroidal anti-inflammatory drug very poorly water-soluble (25 mg/L at 25 °C), can be improved by complexation with ß-cyclodextrin and even more with chemically-modified ß-cyclodextrins [2]. Furthermore the favourable effect of macromolecules such as PVP on the NAP solubility and dissolution properties was also demonstrated [3]. The aim of the present work was to investigate the combined effect of hydroxypropyl-ß-cyclodextrin (HPßCd) and polyvynilpyrrolidone (PVP) on the enhancement of NAP dissolution properties
THE EFFECT OF POLYVINYLPYRROLIDONE ON HYDROXYPROPYL-ß-CYCLODEXTRIN COMPLEXATION WITH NAPROXEN / Mura, P.; Faucci, M.T.; Bettinetti, G.P.. - STAMPA. - (2000), pp. 953-954. (Intervento presentato al convegno 3rd world meeting on pharmaceutics, biopharmaceutics, pharmaceutical technology tenutosi a Berlin nel April 03-06, 2000).
THE EFFECT OF POLYVINYLPYRROLIDONE ON HYDROXYPROPYL-ß-CYCLODEXTRIN COMPLEXATION WITH NAPROXEN
MURA, PAOLA ANGELA;FAUCCI, MARIA TERESA;BETTINETTI, GIAMPIERO
2000
Abstract
Cyclodextrins are torus-shaped molecules with a hydrophilic outer surface and a lipophilic central cavity. Due to their unique spatial configuration, they can form inclusion complexes with a variety of lipophilic drugs, thus favourably affecting many physicochemical properties, such as their solubility and stability. Therefore the importance of cyclodextrins as excipients in pharmaceutical formulations is always increasing [1]. However, due to their relatively low complexation efficiency, it often happens that larger amounts of carrier should be used than those actually employable in many drug formulations. Therefore it is important to find methods for enhancing the cyclodextrin complexation efficiency, by making possible less carrier can be used to achieve the same favourable effect. Recent works reported the positive effect of the addition of a suitable third component on the complexation efficiency of cyclodextrins [1]. We previously showed that the solubility of naproxen (NAP), non-steroidal anti-inflammatory drug very poorly water-soluble (25 mg/L at 25 °C), can be improved by complexation with ß-cyclodextrin and even more with chemically-modified ß-cyclodextrins [2]. Furthermore the favourable effect of macromolecules such as PVP on the NAP solubility and dissolution properties was also demonstrated [3]. The aim of the present work was to investigate the combined effect of hydroxypropyl-ß-cyclodextrin (HPßCd) and polyvynilpyrrolidone (PVP) on the enhancement of NAP dissolution properties
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