Trometamol-fosfomycin (Monuril) bioavailability and food-drug interaction. 1987

E Bergogne-Bérézin, and C Muller-Serieys, and M L Joly-Guillou, and N Dronne

A new water-soluble monobasic salt of fosfomycin with trometamol has recently been developed for oral administration. The objective of this study was to evaluate the pharmacokinetics of trometamol-fosfomycin (Monuril) in serum and in urine in 10 healthy volunteers after oral administration of one single dose (50 mg/kg). In the same volunteers the concentrations of fosfomycin were measured before and after food absorption, in serum and urine samples taken at t = 0, 2, 4, 6, 8 and 24 h after the dose (plus 0.5 and 1 h for serum samples). The measurement of fosfomycin levels was carried out by means of a microbiological procedure using Proteus mirabilis ATCC 21100 as test organism. The results indicated at 2 or 4 h serum peak levels ranging from 9 to 28 micrograms/ml, with mean values of about 17-21 micrograms/ml. The urine concentrations reached 2,000-2,500 micrograms/ml at 2 h, with high levels maintained till the 8th hour (1,200-2,750 micrograms/ml) and persistence of noticeable concentrations at 24 h (100-700 micrograms/ml). The influence of food absorption, even variable, decreased significantly the rate of absorption, with lower serum and urine levels, as measured in the same volunteers. Taking into account this factor influencing the bioavailability and the distribution of the drug, the results of the study confirm that a high proportion of the oral dose of trometamine salt of fosfomycin is absorbed; the extremely high urinary recovery of the drug even after food administration could certainly allow short-course therapy or even single-dose therapy in the treatment of uncomplicated urinary tract infection.

UI MeSH Term Description Entries
D007408 Intestinal Absorption Uptake of substances through the lining of the INTESTINES. Absorption, Intestinal
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008297 Male Males
D005260 Female Females
D005502 Food Substances taken in by the body to provide nourishment. Foods
D005578 Fosfomycin An antibiotic produced by Streptomyces fradiae. Phosphonomycin,Fosfomycin Trometamol Salt,Fosfomycin Tromethamine,Monuril,Phosphomycin,Tromethamine, Fosfomycin
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000284 Administration, Oral The giving of drugs, chemicals, or other substances by mouth. Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D001682 Biological Availability The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action. Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities

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