Ma. Vandelli et al., A solution and solid state study on 2-hydroxypropyl-beta-cyclodextrin complexation with hyodeoxycholic acid, J INCL P MA, 37(1-4), 2000, pp. 237-251
Citations number
29
Categorie Soggetti
Chemistry
Journal title
JOURNAL OF INCLUSION PHENOMENA AND MACROCYCLIC CHEMISTRY
Hyodeoxycholic acid (HDCA) is a 6-alpha dihydroxylated natural bile acid ca
pable of preventing gallstone formation by reducing the bile cholesterol sa
turation. However, any attempt to enrich the bile acid pool with HDCA have
failed owing to the poor solubility of the molecule. To resolve the bioavai
lability problems, the complexation of HDCA into the HP beta CD cavity was
studied in solution (solubility methods, C-13- and H-1-NMR spectroscopy and
circular dichroism) and in the solid state (IR spectroscopy, X-ray diffrac
tometry and thermal analysis). According to the results, the HDCA inclusion
took place with 1 : 1 stoichiometry. The influence of different preparatio
n methods of the solid complex was evaluated for its potential use in appro
priate pharmaceutical formulations to improve the bioavailability of HDCA.