Improvement of ursodeoxycholic acid bioavailability by 2-hydroxypropyl-beta-cyclodextrin complexation in healthy volunteers. 1995

R Panini, and M A Vandelli, and F Forni, and J M Pradelli, and G Salvioli
Department of Pharmaceutical Sciences, University of Modena, Italy.

Tablets containing the inclusion complex of ursodeoxycholic acid (UDCA) with 2-hydroxypropyl-beta-cyclodextrin were prepared by direct compression. Plasma concentrations of UDCA were determined in six healthy volunteers after oral administration of tablets containing the inclusion complex or UDCA alone (Ursacol). Following the administration of the complex tablets, the mean area under the plasma concentration curve (AUC) and the maximum UDCA plasma concentration (Cmax) were significantly higher than those obtained after the administration of the commercial ones. Moreover, the time of maximum plasma concentration (tmax) appeared at a shorter time. These results may be explained by the increase of the UDCA dissolution rate via complex formation.

UI MeSH Term Description Entries
D008297 Male Males
D008875 Middle Aged An adult aged 45 - 64 years. Middle Age
D003505 Cyclodextrins A homologous group of cyclic GLUCANS consisting of alpha-1,4 bound glucose units obtained by the action of cyclodextrin glucanotransferase on starch or similar substrates. The enzyme is produced by certain species of Bacillus. Cyclodextrins form inclusion complexes with a wide variety of substances. Cycloamylose,Cyclodextrin,Cyclodextrin Derivatives,Cyclomaltooligosaccharides,Derivatives, Cyclodextrin
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000073738 2-Hydroxypropyl-beta-cyclodextrin Derivative of beta-cyclodextrin that is used as an excipient for steroid drugs and as a lipid chelator. 2 Hydroxypropyl-beta-cyclodextrin,HP-beta-CD,HPbetaCD,Hydroxypropyl Betadex,Hydroxypropyl-beta-cyclodextrin,beta-Hydroxypropylcyclodextrin,2 Hydroxypropyl beta cyclodextrin,Betadex, Hydroxypropyl,Hydroxypropyl beta cyclodextrin,beta Hydroxypropylcyclodextrin
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D001682 Biological Availability The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action. Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities
D012995 Solubility The ability of a substance to be dissolved, i.e. to form a solution with another substance. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed) Solubilities
D013607 Tablets Solid dosage forms, of varying weight, size, and shape, which may be molded or compressed, and which contain a medicinal substance in pure or diluted form. (Dorland, 28th ed) Tablet

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