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PubMed1973

Maridomycin, a new macrolide antibiotic. In vitro antibacterial activity of 9-propionylmaridomycin.

9-Propionylmaridomycin shows in vitro antibacterial activity against gram-positive bacteria and has some action on Neisseria gonorrhoeae and Vibrio cholerae, but is generally inactive against many gram-negative rods. This antibiotic exhibits strong activity against clinical isolates of Staphylococcus aureus which are highly resistant to erythromycin or oleandomycin, or both, but which are sensitive to josamycin and kitasamycin. Strains resistant to josamycin and kitasamycin were also found to be resistant to this antibiotic. A significant feature of 9-propionylmaridomycin is a lack in its ability to induce resistance induction in resistance-inducible strains of staphylococci to erythromycin. Several antibacterial features of 9-propionylmaridomycin such as the influence of medium pH, inoculum size, effect of addition of horse serum, development of resistance, cross resistance, and bacteriostatic activity were shown to be almost identical to those of josamycin and kitasamycin. The antibacterial activity of 9-propionylmaridomycin was stable in solutions at pH levels of 4, 7, and 9.

Aminoglycosides↗
PubMed1987

Gas chromatographic-mass spectrometric determination of macrolide antibiotics in beef and pork using single ion monitoring.

A gas chromatographic-mass spectrometric (GC-MS) method using single ion monitoring (SIM) is described for the determination of residual macrolide antibiotics, oleandomycin, kitasamycin, spiramycin and tylosin, in beef and pork. For GC-MS determination, oleandomycin is acid hydrolysed to desoleandomycin and acetylated, in the same way as erythromycin. However, for elution from a GC column, the carbon-carbon double bonds in the antibiotics must be hydrogenated to single bonds before acid hydrolysis. Kitasamycin and spiramycin are therefore converted into hydroforocidine acetate and tylosin into hydro-O-mycaminosyl tylonolide acetate, which are determined by GC-MS with SIM.

Acetylation↗
PubMed1998

Simultaneous determination of five macrolide antibiotics in meat by high-performance liquid chromatography.

A simple and rapid method using high-performance liquid chromatography (HPLC) for the simultaneous determination of five macrolides (josamycin, kitasamycin, mirosamicin, spiramycin and tylosin) in meat has been developed. The drugs were extracted with 0.3% metaphosphoric acid-methanol (7:3, v/v), and the extracts were cleaned up on a Bond Elut SCX (500 mg) cartridge. The HPLC separation was performed on a Puresil 5C18 column (150 x 4.6 mm I.D.) with a gradient system of 0.025 M phosphate buffer (pH 2.5)-acetonitrile as the mobile phase at a flow-rate of 1.0 ml/min. The drugs were detected at 232 mn for josamycin, kitasamycin, mirosamicin and spiramycin, and 287 mn for tylosin. The calibration graphs were rectilinear from 2.5 to 100 ng for each drug. The recoveries at the level of 1.0 microgram/g were 70.8-90.4%, and detection limits were 0.05 microgram/g for each drug.

Animals↗
PubMed1993

Susceptibilities of Mycoplasma bovis, Mycoplasma dispar, and Ureaplasma diversum strains to antimicrobial agents in vitro.

The purpose of this study was to determine the susceptibility of various strains of Mycoplasma bovis, Mycoplasma dispar, and Ureaplasma diversum, which are prevalent causes of pneumonia in calves, to 16 antimicrobial agents in vitro. The MICs of the antimicrobial agents were determined by a serial broth dilution method for 16 field strains and the type strain of M. bovis, for 19 field strains and the type strain of M. dispar, and for 17 field strains of U. diversum. Final MICs for M. bovis and M. dispar were read after 7 days and final MICs for U. diversum after 1 to 2 days. All strains tested were susceptible to tylosin, kitasamycin, and tiamulin but were resistant to nifuroquine and streptomycin. Most strains of U. diversum were intermediately susceptible to oxytetracycline but fully susceptible to chlortetracycline; most strains of M. bovis and M. dispar, however, were resistant to both agents. Strains of M. dispar and U. diversum were susceptible to doxycycline and minocycline, but strains of M. bovis were only intermediately susceptible. Susceptibility or resistance to chloramphenicol, spiramycin, spectinomycin, lincomycin, or enrofloxacin depended on the species but was not equal for the three species. The type strains of M. bovis and M. dispar were more susceptible to various antimicrobial agents, including tetracyclines, than the field strains. This finding might indicate that M. bovis and M. dispar strains are becoming resistant to these agents. Antimicrobial agents that are effective in vitro against all three mycoplasma species can be considered for treating mycoplasma infections in pneumonic calves. Therefore, tylosin, kitasamycin, and tiamulin may be preferred over oxytetracycline and chlortetracycline.

Animals↗
PubMed1989

[The compatibility of the new ionophore-coccidiostats with other chemotherapeutics in broilers].

The compatibility of Salinomycin, Narasin or Maduramycin with Tiamulin, Erythromycin, Tylosin, Kitasamycin, Flumequine, Sulfachlorpyrazine or Sulfaquinoxaline was tested in cockerels in three experiments. It was found that Salinomycin and Narasin are incompatible with Tiamulin, Erythromycin, Sulfachlorpyrazine and Sulfaquinoxaline. The effect of incompatibility was shown more markedly with the administration of Salinomycin than with Narasin. Maduramycin was also shown as incompatible with Tiamulin although this interaction was nowhere near as severe as in the case of Salinomycin or Narasin. It caused a significant weight gain depression without mortality. Because of the significant weight gain depression, however, the administration of Tiamulin in the presence of Maduramycin in feed will not be recommended. At the same time, Maduramycin proved to be fully compatible with Erythromycin, Sulfachlorpyrazine and Sulfaquinoxaline. All three anticoccidials tested showed total compatibility with Tylosin, Kitasamycin and Flumequine.

Animals↗
PubMed1995

Toxicological studies on potentiated ionophores in chickens. II. Compatibility study.

Two trials were carried out on a total of 2 x 360 Tetra-82 broiler chickens to study how the presence of the antioxidant duokvin as potentiating agent influenced the compatibility of reduced doses of monensin (12.5 mg/kg of feed) or maduramicin (3.0 mg/kg of feed) with other chemotherapeutic agents (tiamulin, erythromycin, sulfaquinoxaline, sulfachlorpyrazine, flumequine, tylosin, kitasamycin) widely used in broiler rearing. Compatibility was assessed on the basis of the appearance of clinical signs suggestive of toxic interaction, the mortality rate, body mass gain, feed consumption and drinking water intake, and changes in AST and LDH activities of the blood plasma. The monensin-duokvin combination (12.5 mg monensin/kg of feed + 120 mg duokvin/kg of feed) was found to be compatible with erythromycin, sulfaquinoxaline, sulfachlorpyrazine, flumequine, tylosin and kitasamycin. For tiamulin, a slight incompatibility was observed; however, this was much less severe than that found for monensin administered at a dose of 100 mg/kg of feed. The maduramicin-duokvin combination (3.0 mg maduramicin/kg of feed + 120 mg duokvin/kg of feed) was compatible with all the compounds tested; thus, it can be safely applied also in combination with tiamulin.

Animals↗
PubMed1996

In vitro susceptibility of Mycoplasma hyosynoviae and M. hyorhinis to antimicrobial agents.

Fifty-four Japanese strains of Mycoplasma hyosynoviae isolated from porkers during 1980 to 1995, and 107 Japanese strains of M. hyorhinis isolated from piglets with respiratory disease during 1991 to 1994 were investigated for the in vitro activities of 13 antimicrobial agents [josamycin, tylosin, spiramycin, kitasamycin, erythromycin, lincomycin (LCM), kanamycin (KM), chloramphenicol (CP), thiamphenicol (TP), tiamulin (TML), oxytetracycline (OTC), chlortetracycline (CTC), and enrofloxacin (ERFX)] by the agar dilution method. Of the drugs tested TML showed the highest activity with minimum inhibitory concentration (MIC) of 0.013 to 0.1 microgram/ m/ (MIC90; 0.05 microgram/ml) against strains of M. hyosynoviae, and 0.2 to 0.78 microgram/ml (MIC90; 0.39 microgram/ml) against strains of M. hyorhinis. ERFX, LCM, most of the 16-membered macrolide antibiotics and tetracyclines also showed low MICs against both mycoplasma species. The susceptibility of KM, CP and TP to the mycoplasmas was considered to be of a secondary grade. Two of 54 strains of M. hyosynoviae, and 11 of 107 strains of M. hyorhinis showed resistance to all 14- and 16-membered macrolide antibiotics tested. Tetracyclines (OTC and CTC) showed a relatively broad MIC distribution from 0.1 to 6.25 micrograms/ml against the M. hyosynoviae strains tested. All of the strains isolated during 1980 to 1984 were susceptible at the concentration of 0.78 microgram/ml or less (MIC90; 0.78 microgram/ml) to OTC and 1.56 micrograms/ml or less (MIC90; 1.56 micrograms/ml) to CTC, while the susceptibility of strains isolated recently, during 1994 to 1995, was more than 0.78 microgram/ml (MIC90; 3.13 micrograms/ml) to OTC, and more than 1.56 micrograms/ml (MIC90; 6.25 micrograms/ml) to CTC.

Animals↗
PubMed2006

[Identification of the components and products of hydrolysis in acetylleucomycin by LC-MS].

AIM: To identify the components of acetylleucomycin and its hydrolytic products by LC-MS. METHODS: Acetylleucomycin was separated on a Diamonsil C18 column with 0.1 mol x L(-1) ammonium acetate-acetontrile (35 : 65) as mobile phase. The LC-MS was equipped with an electorspray ion source (ESI), which was set at the positive ion mode, and the mass spectra of each component in chromatogram were obtained with difference cone voltage. RESULTS: The components of acetylleucomycin and its hydrolytic products can be separated by HPLC. The components were identified according to the molecular weight and its major mass fragment ions. The major components identified in domastic acetylleucomycin were acetylleucomycin A4, A5; acetylleucomycin A1, A3; acetylleucomycin A6, A7, and acetylleucomycin A13. The hydrolytic products of acetylleucomycin were not kitasamycin, but some non-complete hydrolytic product. CONCLUSION: The method is rapid, sensitive and specific. It' s suitable to application in the fields of multi-components antibiotics analysis.

Chromatography, Liquid↗
PubMed2006

High-throughput screening for multi-class veterinary drug residues in animal muscle using liquid chromatography/tandem mass spectrometry with on-line solid-phase extraction.

A rapid qualitative method using on-line column-switching liquid chromatography/tandem mass spectrometry (LC/MS/MS) was developed and validated for screening 13 target veterinary drugs: four macrolides - erythromycin A, josamycin (leucomycin A3), kitasamycin (leucomycin A5), and tylosin A; six (fluoro)quinolones - ciprofloxacin, danofloxacin, enrofloxacin, flumequine, oxolinic acid, and sarafloxacin; and lincomycin, virginiamycin M1, and trimethoprim in different animal muscles. Clindamycin, norfloxacin, nalidixic acid, oleandomycin, ormetoprim, and roxithromycin were used as the internal standards. After simple deproteination and analyte extraction of muscle samples using acetonitrile, the supernatant was subjected to on-line cleanup and direct analysis by LC/MS/MS. On-line cleanup with an extraction cartridge packed with hydrophilic-hydrophobic polymer sorbent followed by fast LC using a short C18 column resulted in a total analysis cycle of 6 min for 19 drugs. This screening method considerably reduced the time and the cost for the quantitative and confirmatory analyses. The application of a control point approach was also introduced and explained.

Animals↗
PubMed2004

Determination of macrolide antibiotics in porcine and bovine urine by high-performance liquid chromatography coupled to coulometric detection.

A high-performance liquid chromatography method coupled to coulometric detection has been applied for the determination, in a single run, of up to eight macrolide antibiotics (erythromycin [ERY], tylosin [TYL], tilmicosin [TILM], spiramycin 2 [SPI 2], spiramycin 3 [SPI 3], josamycin [JOS], kitasamycin [KIT], and rosamicin [ROS]) in spiked porcine and bovine urine. Quantification was performed using matrix-matched calibration with roxithromycin (ROX) as the internal standard. The detection limits for each drug were below 3.5 ng injected (equivalent to an initial concentration below 0.07 mg L(-1)) for porcine urine and below 5 ng injected (equivalent to an initial concentration below 0.10 mg L(-1)) for bovine urine. Recoveries from urine samples spiked at three different concentrations within the linear range were not significantly dependent on concentration. The entire procedure provides average macrolide recoveries ranging from 69.7 to 96.6% for bovine urine and from 75.5 and 96.1% for porcine urine.

Animals↗
PubMed2006

Analysis of macrolide antibiotics in river water by solid-phase extraction and liquid chromatography-mass spectrometry.

A liquid chromatography-mass spectrometry (LC-MS) method was developed for the determination of five macrolides in natural water samples, using kitasamycin as surrogate. The macrolides were extracted from water samples using Oasis HLB cartridges. Pre-concentration factors up to 250 were obtained. Separation was carried out in an end-capped silica-based C18 column and mobile phases consisting of water/acetonitrile mixtures containing ammonium acetate. Detection was performed by mass spectrometry with a single quadrupole and a triple quadrupole using an electrospray interface. The quality parameters obtained with these two approaches were compared. The detection limits of the whole process were about 1 ng l(-1). The recoveries from 250 ml of water samples spiked at 25-125 ng l(-1) level were in the range 85-115%, except for azithromycin levels, which were around 70%. Erythromycin-H2O, clarithromycin and azithromyzin were found, at the sub ng l(-1) level, in the studied rivers.

Anti-Bacterial Agents↗
PubMed1998

Analysis of macrolide antibiotics.

The following macrolide antibiotics have been covered in this review: erythromycin and its related substances, azithromycin, clarithromycin, dirithromycin, roxithromycin, flurithromycin, josamycin, rokitamycin, kitasamycin, mycinamycin, mirosamycin, oleandomycin, rosaramicin, spiramycin and tylosin. The application of various thin-layer chromatography, paper chromatography, gas chromatography, high-performance liquid chromatography and capillary zone electrophoresis procedures for their analysis are described. These techniques have been applied to the separation and quantitative analysis of the macrolides in fermentation media, purity assessment of raw materials, assay of pharmaceutical dosage forms and the measurement of clinically useful macrolide antibiotics in biological samples such as blood, plasma, serum, urine and tissues. Data relating to the chromatographic behaviour of some macrolide antibiotics as well as the various detection methods used, such as bioautography, UV spectrophotometry, fluorometry, electrochemical detection, chemiluminescence and mass spectrometry techniques are also included.

Animals↗