Document Detail

Effect of food on the pharmacokinetics of rifalazil, a novel antibacterial, in healthy male volunteers.
MedLine Citation:
PMID:  17463218     Owner:  NLM     Status:  MEDLINE    
Rifalazil is a new antibiotic structurally related to rifampin but devoid of the metabolic liabilities typically associated with the rifamycin class of antibiotics. A randomized, 3-way crossover study in healthy male volunteers (n = 12) investigated the safety and pharmacokinetics of a single 25-mg oral rifalazil dose administered under a standard breakfast containing fat as 30% of calories, a high-fat breakfast containing fat as 60% of calories, and an overnight fast of 10 hours with a 21- to 28-day washout between doses. Systemic exposure to rifalazil based on Cmax, AUC(0-Tlast), and AUC(0-infinity) was increased progressively as the fat content of the test breakfast was increased from 30% to 60% compared with fasting. The confidence intervals for both fat-containing breakfasts are outside the limits of 80% to 125% allowed for food effect bioequivalence based on Cmax, AUC(0-Tlast), and AUC(0-infinity). This food effect may be a result of increased fractional absorption with increasing dietary fat content. Another striking finding was the large reduction of the pharmacokinetic intersubject variability after rifalazil administration with food. Rifalazil was safe and well tolerated under fed and fasted conditions.
Y-X Chen; B Cabana; N Kivel; A Michaelis
Related Documents :
19091798 - Continuous dose-response relationship of the ldl-cholesterol-lowering effect of phytost...
22414488 - Diagnostic oral food challenges: procedures and biomarkers.
24976408 - Effects of different concentrations of salt and sugar on biogenic amines and quality ch...
17576058 - Effect of maltodextrin and superdisintegrant in directly compressible powder mixtures p...
17370808 - Maturation feeding and transmission of bursaphelenchus xylophilus (nematoda: parasitaph...
11534628 - Determination of ascorbyl 6-palmitate in food matrices by amperometric flow injection a...
Publication Detail:
Type:  Comparative Study; Journal Article; Randomized Controlled Trial     Date:  2007-04-26
Journal Detail:
Title:  Journal of clinical pharmacology     Volume:  47     ISSN:  0091-2700     ISO Abbreviation:  J Clin Pharmacol     Publication Date:  2007 Jul 
Date Detail:
Created Date:  2007-06-22     Completed Date:  2007-08-20     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0366372     Medline TA:  J Clin Pharmacol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  841-9     Citation Subset:  IM    
ActivBiotics, Inc, Lexington, MA,
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Anti-Bacterial Agents / administration & dosage,  adverse effects*,  blood,  pharmacokinetics*
Area Under Curve
Biological Availability
Chromatography, High Pressure Liquid
Cross-Over Studies
DNA-Directed DNA Polymerase / antagonists & inhibitors
Dietary Fats
Food-Drug Interactions*
Gastric Emptying
Mass Spectrometry
Middle Aged
Rifamycins / administration & dosage,  adverse effects*,  blood,  pharmacokinetics*
Therapeutic Equivalency
Reg. No./Substance:
0/Anti-Bacterial Agents; 0/Dietary Fats; 0/Rifamycins; 129791-92-0/KRM 1648; EC DNA Polymerase

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

Previous Document:  Coadministration of estradiol/drospirenone and indomethacin does not cause hyperkalemia in healthy p...
Next Document:  Pharmacokinetics of an oral drug (acetaminophen) administered at various times relative to subcutane...