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Antimicrobial Agents and Chemotherapy, July 1998, p. 1862-1865, Vol. 42, No. 7
0066-4804/98/$04.00+0
Copyright © 1998, American Society for Microbiology. All rights reserved.

Enhanced Bioavailability of Itraconazole in Hydroxypropylbeta -Cyclodextrin Solution versus Capsules in Healthy Volunteers

Joseph A. Barone,1,* Bruce L. Moskovitz,2 Joseph Guarnieri,2 Alan E. Hassell,2 John L. Colaizzi,1 Robert H. Bierman,1 and Lois Jessen1

Rutgers---The State University of New Jersey, Piscataway,1 and Janssen Research Foundation, Titusville,2 New Jersey

Received 7 July 1997/Returned for modification 24 December 1997/Accepted 6 April 1998

The bioavailabilities and bioequivalences of single 200-mg doses of itraconazole solution and two capsule formulations were evaluated in a crossover study of 30 male volunteers. The two capsule formulations were bioequivalent. The bioavailabilities of the solutions itraconazole and hydroxyitraconazole were 30 to 33% and 35 to 37% greater, respectively, than those of either capsule. However, the maximum concentrations of the drug in plasma (Cmax), the times to Cmax, and the terminal half-lives were comparable for all three formulations. These data indicate that the bioavailabilities of itraconazole and hydroxyitraconazole are enhanced when administered as an oral solution instead of capsules.


* Corresponding author. Mailing address: College of Pharmacy, Rutgers---The State University of New Jersey, William Levine Hall, Frelinghuysen Rd., Piscataway, NJ 08855-0789. Phone: (732) 445-3285. Fax: (732) 445-2533. E-mail: jbarone{at}rci.rutgers.edu.


Antimicrobial Agents and Chemotherapy, July 1998, p. 1862-1865, Vol. 42, No. 7
0066-4804/98/$04.00+0
Copyright © 1998, American Society for Microbiology. All rights reserved.



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