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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
Hydroxypropyl
-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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