PMID- 23390369
OWN - NLM
STAT- PubMed-not-MEDLINE
DCOM- 20130208
LR  - 20211021
IS  - 1179-1438 (Print)
IS  - 1179-1438 (Electronic)
IS  - 1179-1438 (Linking)
VI  - 5
DP  - 2013
TI  - A Phase 1, randomized, open-label crossover study to evaluate the safety and 
      pharmacokinetics of 400 mg albaconazole administered to healthy participants as a 
      tablet formulation versus a capsule formulation.
PG  - 23-31
LID - 10.2147/CPAA.S39600 [doi]
AB  - BACKGROUND: Albaconazole is a novel triazole being developed for the oral 
      treatment of fungal diseases. Once-weekly oral dosing with 400 mg albaconazole 
      for 24 or 36 weeks resulted in high rates of clinical and mycological resolution 
      for distal subungual onychomycosis, as well as a favorable safety and 
      tolerability profile. PURPOSE: To compare four 100-mg albaconazole capsules to 
      one 400-mg albaconazole tablet for bioavailability, bioequivalence, tolerability, 
      and safety. PATIENTS AND METHODS: Forty participants were enrolled in this Phase 
      I, open-label, two-sequence crossover study. Twenty participants were exposed to 
      a single 400-mg tablet dose of albaconazole before being crossed over to a single 
      dose of four 100-mg albaconazole capsules. The second group of 20 participants 
      received the study products in reverse order. Blood samples were taken over 15 
      days post-dose to assess the plasma concentrations and pharmacokinetic parameters 
      of albaconazole and its primary metabolite, 6-hydroxyalbaconazole. Safety was 
      assessed throughout the study. RESULTS: The area under the curve (AUC) and 
      maximum measured plasma concentration (C(max)) of the albaconazole tablet were 
      approximately 10% and 22% lower, respectively, than for the albaconazole 
      capsules. Statistical significance was reached for the C(max) but not for the AUC 
      measurements (AUC(0-t) and AUC(0-inf)). Because the 90% confidence intervals 
      based on the differences between the tablet and capsule were outside the 80%-125% 
      range for both the C(max) and AUC, we concluded that the formulations were not 
      bioequivalent with respect to the rate or extent of absorption. Both formulations 
      were safe and well-tolerated in this study. All adverse events (AEs) were 
      generally mild and were mainly gastrointestinal- or nervous system-related (eg, 
      dizziness, headache). No electrocardiogram findings were reported as an AE, and 
      no serious AEs or deaths were reported. CONCLUSION: The AUC and C(max) of 
      albaconazole after a single 400-mg oral dose administered as a tablet formulation 
      were lower than those of a capsule formulation. Albaconazole tablets and capsules 
      cannot, therefore, be considered bioequivalent.
FAU - van Rossem, Koen
AU  - van Rossem K
AD  - Stiefel, Research Triangle Park, NC, USA.
FAU - Lowe, Jenny A
AU  - Lowe JA
LA  - eng
PT  - Journal Article
DEP - 20130130
PL  - New Zealand
TA  - Clin Pharmacol
JT  - Clinical pharmacology : advances and applications
JID - 101564865
PMC - PMC3564460
OTO - NOTNLM
OT  - albaconazole
OT  - onychomycosis
OT  - pharmacokinetics
OT  - triazole
EDAT- 2013/02/08 06:00
MHDA- 2013/02/08 06:01
PMCR- 2013/01/30
CRDT- 2013/02/08 06:00
PHST- 2013/02/08 06:00 [entrez]
PHST- 2013/02/08 06:00 [pubmed]
PHST- 2013/02/08 06:01 [medline]
PHST- 2013/01/30 00:00 [pmc-release]
AID - cpaa-5-023 [pii]
AID - 10.2147/CPAA.S39600 [doi]
PST - ppublish
SO  - Clin Pharmacol. 2013;5:23-31. doi: 10.2147/CPAA.S39600. Epub 2013 Jan 30.