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Complexation of ursodeoxycholic acid with beta-cyclodextrin-choline dichloride coprecipitate.
Int J Pharm. 1999 Nov 15; 190(2):139-53.IJ

Abstract

The inclusion complexes of ursodeoxycholic acid (UDCA) with beta-cyclodextrin (betaCD) coprecipitated with choline dichloride (CDC) or beta-cyclodextrin were investigated to evaluate the effect of the presence of choline for UDCA inclusion in betaCD. The inclusion complexes were investigated in solution by phase solubility diagrams and 1H NMR spectrometry and in solid state (kneading, freeze-drying, sealed heating and spray-drying) by DSC, SEM, HSM, XRD and IR spectroscopy. Stability constants were determined at pH 5.5 and 7.0 to simulate the environmental pH of the first intestinal tract and at different temperatures (25, 30 and 37 degrees C) to obtain the thermodynamic parameters of inclusion. Both betaCD-CDC and betaCD increased the water solubility of UDCA particularly betaCD-CDC. All complexes showed a high dissolution rate particularly the spray-dried complexes obtained in the presence of betaCD-CDC.

Authors+Show Affiliations

Department of Pharmaceutical Sciences, University of Bologna, Via S. Donato 19/2, 40127, Bologna, Italy. orienti@biocfarm.unibo.itNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

10547454

Citation

Orienti, I, et al. "Complexation of Ursodeoxycholic Acid With Beta-cyclodextrin-choline Dichloride Coprecipitate." International Journal of Pharmaceutics, vol. 190, no. 2, 1999, pp. 139-53.
Orienti I, Cerchiara T, Zecchi V, et al. Complexation of ursodeoxycholic acid with beta-cyclodextrin-choline dichloride coprecipitate. Int J Pharm. 1999;190(2):139-53.
Orienti, I., Cerchiara, T., Zecchi, V., Arias Blanco, M. J., Gines, J. M., Moyano, J. R., & Rabasco Alvarez, A. M. (1999). Complexation of ursodeoxycholic acid with beta-cyclodextrin-choline dichloride coprecipitate. International Journal of Pharmaceutics, 190(2), 139-53.
Orienti I, et al. Complexation of Ursodeoxycholic Acid With Beta-cyclodextrin-choline Dichloride Coprecipitate. Int J Pharm. 1999 Nov 15;190(2):139-53. PubMed PMID: 10547454.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Complexation of ursodeoxycholic acid with beta-cyclodextrin-choline dichloride coprecipitate. AU - Orienti,I, AU - Cerchiara,T, AU - Zecchi,V, AU - Arias Blanco,M J, AU - Gines,J M, AU - Moyano,J R, AU - Rabasco Alvarez,A M, PY - 1999/11/5/pubmed PY - 1999/11/5/medline PY - 1999/11/5/entrez SP - 139 EP - 53 JF - International journal of pharmaceutics JO - Int J Pharm VL - 190 IS - 2 N2 - The inclusion complexes of ursodeoxycholic acid (UDCA) with beta-cyclodextrin (betaCD) coprecipitated with choline dichloride (CDC) or beta-cyclodextrin were investigated to evaluate the effect of the presence of choline for UDCA inclusion in betaCD. The inclusion complexes were investigated in solution by phase solubility diagrams and 1H NMR spectrometry and in solid state (kneading, freeze-drying, sealed heating and spray-drying) by DSC, SEM, HSM, XRD and IR spectroscopy. Stability constants were determined at pH 5.5 and 7.0 to simulate the environmental pH of the first intestinal tract and at different temperatures (25, 30 and 37 degrees C) to obtain the thermodynamic parameters of inclusion. Both betaCD-CDC and betaCD increased the water solubility of UDCA particularly betaCD-CDC. All complexes showed a high dissolution rate particularly the spray-dried complexes obtained in the presence of betaCD-CDC. SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/10547454/Complexation_of_ursodeoxycholic_acid_with_beta_cyclodextrin_choline_dichloride_coprecipitate_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378517399002057 DB - PRIME DP - Unbound Medicine ER -