PMID- 16490584
OWN - NLM
STAT- MEDLINE
DCOM- 20060525
LR  - 20131121
IS  - 0149-2918 (Print)
IS  - 0149-2918 (Linking)
VI  - 28
IP  - 1
DP  - 2006 Jan
TI  - Bioavailability of two oral formulations of loratadine 20 mg with concomitant 
      ketoconazole: an open-label, randomized, two-period crossover comparison in 
      healthy Mexican adult volunteers.
PG  - 110-5
AB  - BACKGROUND: Loratadine is a long-acting antihistamine with selective peripheral 
      histamine H(1)-receptor antagonistic activity and fewer sedative effects compared 
      with conventional antihistamines, and is widely used in Mexico. Although several 
      generic formulations of loratadine are available in Mexico, based on a literature 
      search, information concerning the bioavailability of each formulation in the 
      Mexican population is not available. OBJECTIVE: The aim of this study was to 
      compare the bioavailability and tolerability of 2 oral formulations of loratadine 
      20 mg (two 10-mg tablets) used in Mexico: Sensibit (test formulation; 
      Laboratorios Liomont S.A. de C.V., Mexico City, Mexico) and Clarityne (reference 
      formulation; Schering-Plough S.A. de C.V., Mexico City, Mexico) in healthy 
      volunteers. METHODS: This open-label, randomized, 2-period crossover study was 
      conducted at Universidad Autonoma de Nuevo Leon, Monterrey, Nuevo Leon, Mexico. 
      Eligible subjects were healthy male Mexican volunteers aged > or=18 years. 
      Subjects were randomly assigned to receive a single 20-mg dose (two 10-mg 
      tablets) of the test or reference formulation, followed by a 2-week washout 
      period, followed by the same dose of the alternate formulation. A 400-mg dose of 
      ketoconazole (2 doses in 24 hours) was administered to each subject before the 
      administration of each formulation, and a 200-mg dose of ketoconazole was given 
      together with each formulation (ie, a total of 600 mg of ketoconazole was 
      administered). Doses were administered after a 12-hour overnight fast. For 
      analysis of pharmacokinetic properties, including C(maX), AUC(0-t), and 
      AUC(0-infinity), blood samples were drawn at 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 
      2.5, 3, 5, 8, 12, 16, and 22 hours after dosing. The formulations were considered 
      bioequivalent if the geometric mean ratios of C(maX) and AUC were within the 
      predetermined equivalence range of 80% to 125%. Tolerability was assessed by 
      monitoring vital signs and subject interview regarding the potential presence of 
      adverse events (AEs). RESULTS: Thirty-two subjects were enrolled in the study 
      (mean age, 22 years [range, 18-28 years]; mean weight, 68.9 kg [range, 58-79 kg]; 
      mean height, 170.8 cm [range, 158-183 cm]). Sixteen subjects received the test 
      formulation first. No period or sequence effect was observed. The 90% CIs for the 
      corresponding ratios of CmaX, AUC(0-t), and AUC(0-infinity) were 81.43% to 
      106.01%, 83.12% to 100.23%, and 84.06% to 101.10% (all, P < 0.05), meeting the 
      predetermined criteria for bioequivalence. Similar results were found for data 
      without a logarithmic transformation. No AEs were reported throughout the study. 
      CONCLUSIONS: In this small study in healthy Mexican volunteers, a single, 20-mg 
      dose of the test formulation of loratadine was found to be bioequivalent to that 
      of the reference formulation based on the rate and extent of absorption when 
      concomitantly administered with ketoconazole. Both formulations were well 
      tolerated.
FAU - Pineyro-Lopez, Alfredo
AU  - Pineyro-Lopez A
AD  - Department of Pharmacology and Toxicology, Universidad Autonoma de Nuevo Leon, 
      Monterrey, NuevoLeon, Mexico.
FAU - Pineyro-Garza, Everardo
AU  - Pineyro-Garza E
FAU - Torres-Alanis, Oscar
AU  - Torres-Alanis O
FAU - Reyes-Araiza, Raul
AU  - Reyes-Araiza R
FAU - Gomez Silva, Magdalena
AU  - Gomez Silva M
FAU - Wacksman, Noemi
AU  - Wacksman N
FAU - Lujan Rangel, Ruben
AU  - Lujan Rangel R
FAU - de Lago, Alberto
AU  - de Lago A
FAU - Trejo, Daniel
AU  - Trejo D
FAU - Gonzalez-de la Parra, Mario
AU  - Gonzalez-de la Parra M
FAU - Namur, Salvador
AU  - Namur S
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PT  - Randomized Controlled Trial
PT  - Research Support, Non-U.S. Gov't
PL  - United States
TA  - Clin Ther
JT  - Clinical therapeutics
JID - 7706726
RN  - 0 (Antifungal Agents)
RN  - 0 (Histamine H1 Antagonists, Non-Sedating)
RN  - 7AJO3BO7QN (Loratadine)
RN  - R9400W927I (Ketoconazole)
SB  - IM
MH  - Administration, Oral
MH  - Adolescent
MH  - Adult
MH  - Antifungal Agents/administration & dosage/*pharmacokinetics
MH  - Biological Availability
MH  - Cross-Over Studies
MH  - Drug Interactions
MH  - Drug Therapy, Combination
MH  - Follow-Up Studies
MH  - Histamine H1 Antagonists, Non-Sedating/administration & dosage/*pharmacokinetics
MH  - Humans
MH  - Hypersensitivity/*blood/drug therapy
MH  - Ketoconazole/administration & dosage/*pharmacokinetics
MH  - Loratadine/administration & dosage/*pharmacokinetics
MH  - Male
MH  - Mexico
MH  - Middle Aged
MH  - Reference Values
EDAT- 2006/02/24 09:00
MHDA- 2006/05/26 09:00
CRDT- 2006/02/24 09:00
PHST- 2005/10/27 00:00 [accepted]
PHST- 2006/02/24 09:00 [pubmed]
PHST- 2006/05/26 09:00 [medline]
PHST- 2006/02/24 09:00 [entrez]
AID - S0149-2918(06)00026-9 [pii]
AID - 10.1016/j.clinthera.2006.01.012 [doi]
PST - ppublish
SO  - Clin Ther. 2006 Jan;28(1):110-5. doi: 10.1016/j.clinthera.2006.01.012.