The complexation in aqueous medium and in the solid phase of ursodeoxycholic acid (UDCA) with a highly soluble cyclodextrin, 2-hydroxypropyl-beta-cyclodextrin, was studied by means of solubility methods, IR and C-13-NMR spectroscopy, X-ray diffractometry and thermal analysis. UDCA inclusion took place with 1:1 stoichiometry. C-13-NMR analysis suggested that the side chain was introduced into the cyclodextrin cavity. The UDCA/cyclodextrin complex showed better dissolution properties than plain drug crystals. Therefore, the complex may be used to improve the delivery and bioavailability of ursodeoxycholic acid.
2-HYDROXYPROPYL-BETA-CYCLODEXTRIN COMPLEXATION WITH URSODEOXYCHOLIC ACID / Vandelli, M.A., Salvioli, G., Mucci, A., Panini, R., Malmusi, L., Forni, F.. - In: INTERNATIONAL JOURNAL OF PHARMACEUTICS. - ISSN 0378-5173. - STAMPA. - 118:(1995), pp. 77-83. [10.1016/0378-5173(94)00342-1]
2-HYDROXYPROPYL-BETA-CYCLODEXTRIN COMPLEXATION WITH URSODEOXYCHOLIC ACID
VANDELLI, Maria Angela;SALVIOLI, Gianfranco;MUCCI, Adele;FORNI, Flavio
1995
Abstract
The complexation in aqueous medium and in the solid phase of ursodeoxycholic acid (UDCA) with a highly soluble cyclodextrin, 2-hydroxypropyl-beta-cyclodextrin, was studied by means of solubility methods, IR and C-13-NMR spectroscopy, X-ray diffractometry and thermal analysis. UDCA inclusion took place with 1:1 stoichiometry. C-13-NMR analysis suggested that the side chain was introduced into the cyclodextrin cavity. The UDCA/cyclodextrin complex showed better dissolution properties than plain drug crystals. Therefore, the complex may be used to improve the delivery and bioavailability of ursodeoxycholic acid.
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