PMID- 16330296
OWN - NLM
STAT- MEDLINE
DCOM- 20060201
LR  - 20061115
IS  - 0149-2918 (Print)
IS  - 0149-2918 (Linking)
VI  - 27
IP  - 10
DP  - 2005 Oct
TI  - Bioavailability of two oral formulations of azithromycin 500 mg: a randomized, 
      open-label, two-period crossover comparison in healthy Mexican adult subjects.
PG  - 1607-11
AB  - BACKGROUND: Azithromycin is related to erythromycin but is more active against 
      gram-negative bacteria and less active against streptococci and staphylococci 
      compared with erythromycin. For these reasons, and because of convenience of 
      dosing (QD for 3 days), azithromycin is widely used in Mexico. Although several 
      generic formulations of azithromycin are available in Mexico, 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 azithromycin 500 mg 
      used in Mexico: Macrozit (trademark of Laboratorios Liomont, S.A. de C.V., Mexico 
      City, Mexico; test formulation) and Azitrocin (trademark of Pfizer, S.A. de C.V., 
      Mexico City, Mexico; reference formulation). METHODS: This 2 x 2, crossover, 
      randomized, open-label study was conducted at the Department of Pharmacology and 
      Toxicology, Universidad Automa de Nuevo Leon, Monterrey, Mexico. Eligible 
      subjects were healthy volunteers of either sex and with the following 
      characteristics: age > or =19 to 25 years, weight 54 to 77 kg, and height 159 to 
      177 cm. Subjects were randomly assigned to receive Macrozit followed by 
      Azitrocin, or vice versa, with a 3-week washout period between doses. After a 
      12-hour (overnight) fast, subjects received a single, 500-mg dose of each 
      formulation. For analysis of pharmacokinetic properties, including C(max), 
      AUC(0-t), and AUC(0-infinity), blood samples were drawn at 0.5, 1, 1.5, 2, 2.5, 
      3, 4, 6, 12, 24, 48, 72, 96, and 120 hours after dosing. The formulations were 
      considered bioequivalent if the logarithm (ln)-transformed ratios of C(max) and 
      AUC were within the predetermined equivalence range of 80% to 125% and if P < or 
      = 0.05 for the 90% CIs. Tolerability was assessed by monitoring and subject 
      interview regarding the potential presence of adverse events (AEs). RESULTS: 
      Twenty-eight subjects were enrolled in the study; 27 completed it (14 men, 13 
      women; mean age, 21.7 years). Fourteen subjects received the test formulation 
      first. No period or sequence effect was observed. The 90% CIs for the 
      corresponding ratios of C(max), AUC(0-t), and AUC(0-infinity) were 80.67 to 
      107.21, 91.39 to 107.59, and 90.61 to 106.19 (all, P < 0.05). Similar results 
      were found for data without a logarithmic transformation. No AEs were found 
      throughout the study. CONCLUSIONS: In this small study in healthy Mexican 
      volunteers, a single, 500-mg dose of Macrozit was found to be bioequivalent to 
      that of Azitrocin based on the rate and extent of absorption. 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, 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 - Rangel, Ruben Lujan
AU  - Rangel RL
FAU - de Lago, Alberto
AU  - de Lago A
FAU - Gonzalez-de la Parra, Mario
AU  - Gonzalez-de la Parra M
FAU - Namur, Salvador
AU  - Namur S
LA  - eng
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 (Anti-Bacterial Agents)
RN  - 83905-01-5 (Azithromycin)
SB  - IM
MH  - Administration, Oral
MH  - Anti-Bacterial Agents/*pharmacokinetics
MH  - Azithromycin/*pharmacokinetics
MH  - Biological Availability
MH  - Chemistry, Pharmaceutical
MH  - Cross-Over Studies
MH  - Humans
MH  - Male
MH  - Mass Spectrometry
MH  - Therapeutic Equivalency
EDAT- 2005/12/07 09:00
MHDA- 2006/02/02 09:00
CRDT- 2005/12/07 09:00
PHST- 2005/08/17 00:00 [accepted]
PHST- 2005/12/07 09:00 [pubmed]
PHST- 2006/02/02 09:00 [medline]
PHST- 2005/12/07 09:00 [entrez]
AID - S0149-2918(05)00188-8 [pii]
AID - 10.1016/j.clinthera.2005.10.002 [doi]
PST - ppublish
SO  - Clin Ther. 2005 Oct;27(10):1607-11. doi: 10.1016/j.clinthera.2005.10.002.