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At least 19 recordsLinked to original sources
PubMed1992

Studies on the intravenous pharmacokinetics in rabbit and in vitro protein binding of two new salts of erythromycin: erythromycin maltobionate and erythromycin fumarate.

Pharmacokinetics in rabbits following intravenous administration and in vitro protein binding were studied for two new salts of erythromycin (erythromycin maltobionate and erythromycin fumarate). Serum erythromycin levels following intravenous injection were described by two compartment model kinetics, and values for the distribution volume of the central compartment, the peripheral compartment and overall distribution volume were calculated. The elimination half-lives of erythromycins in serum were 83 min, 168 min, and 103 min for erythromycin maltobionate, erythromycin fumarate, and erythromycin lactobionate (reference standard), respectively. The erythromycin salts were highly (c. 90 per cent) protein bound, but the binding was found to be reversible. Differences in the pharmacokinetic parameters after administration of equivalent doses of the salts, indicate possible variation in efficacies of different salts.

Animals↗
PubMed1978

Fluorimetric determination of erythromycin and erythromycin ethylsuccinate in serum by a high-performance liquid chromatographic post-column, on-stream derivatization and extraction method.

The method described is capable of detecting less than 0.01 microgram/ml of erythromycin and/or erythromycin ethylsuccinate in serum. Recoveries of erythromycin and erythromycin ethylsuccinate, when added to the level of 0.6 microgram/ml, were 102 and 97% with relative standard deviations of 6.0 and 4.5%, respectively. Erythromycin ethylsuccinate in serum at 37 degrees was shown to degrade rapidly to erythromycin in a first-order rate. When stored at -20 degrees, however, only 10% of the erythromycin ethylsuccinate in serum was hydrolyzed even after storage for 36 days. The method was used to analyze erythromycin and erythromycin ethylsuccinate in sera from ten subjects administered with an oral dose of erythromycin ethylsuccinate. In addition to a small amount of anhydroerythromycin ethylsuccinate and 8,9-anhydro-6,9-hemiketal erythromycin ethylsuccinate, at least two other metabolites were detected in sera and one was tentatively identified as erythralosamine.

Chromatography, High Pressure Liquid↗
PubMed1979

Plasma levels following single and repeated doses of erythromycin estolate and erythromycin stearate.

The pharmacokinetics of erythromycin and erythromycin 2'-propanoate were studied in healthy male volunteers following single and repeated doses of erythromycin stearate tablets, erythromycin estolate capsules, and a suspension. Estolate dosages gave rise to higher plasma levels of total drug than the stearate. However, the stearate yielded higher plasma levels of erythromycin base. Absorption of all dosage forms, except the suspension, was delayed, and pharmacokinetic interpretation of both single- and multiple-dose data required incorporation of an absorption lag time. The absorption of erythromycin stearate was inhibited by food and also by low fluid volumes in fasted subjects. Absorption of erythromycin estolate was increased in the presence of food and was not greatly affected by fluid volume. Although single-dose data poorly predicted circulating levels of erythromycin following repeated doses, trends observed after single doses were maintained during chronic treatment.

Adult↗
PubMed1976

L-aspartate of erythromycin A cyclic 11,12-carbonate, a new semisynthetic erythromycin derivative.

Erythromycin A cyclic 11,12-carbonate, a compound with high antibacterial activity, forms with L-aspartic acid a salt possessing valuable properties as a potential chemotherapeutic agent. The L-aspartate of erythromycin A cyclic 11,12-carbonate exhibits strong anti-bacterial activity, especially against Gram-positive bacteria and shows low toxicity. The serum and the lung tissue levels of the discussed salt after a single dose administration to a rat were measured in comparison with those of erythromycin, its L-aspartate, erythromycin cyclic 11,12-carbonate and its L-glutamate. The new erythromycin derivative showed definitely superior characteristics to those of the other substances tested. The activity of the L-aspartate of erythromycin A cyclic 11,12-carbonate in chemotherapy of experimental staphylococcal infection and experimental pneumococcal bronchopneumonia in mice is superior to that of the parent carbonate and erythromycin itself.

Animals↗
PubMed1977

Effects of erythromycin on membrane-bound chloroplast ribosomes from wild-type Chlamydomonas reinhardi and erythromycin-resistant mutants.

1. Treatment of wild-type cells of Chlamydomonas reinhardi with high concentrations of erythromycin results in increased recovery of membrane-bound chloroplast ribosomes, presumably by preventing polysomal runoff during harvesting of cells. No such membrane-retention effect is detected if erythromycin is added after harvesting of cultures, before cell breakage. 2. Growth of wild-type cells is inhibited by 10 microgram/ml erythromycin, but a concentration twice as high is required to increase recovery of membrane-bound wild-type ribosomes. On the other hand, the concentrations of erythromycin which inhibit growth of mutant ery-M1b produce a membrane-retention effect. Mutant ery-U1a is resistant to high concentrations of erythromycin and no membrane-retention effect is detectable at concentrations which produce one in wild type and ery-M1b. 3. These results can be reconciled by a two-point model of the mechanism of erythromycin action on chloroplast ribosomes in Chlamydomonas.

Chlamydomonas↗
PubMed1978

A comparison of ampicillin, erythromycin and erythromycin with sulphametopyrazine in the treatment of infective exacerbations of chronic bronchitis.

A comparative study of ampicillin (500 mg four times daily), erythromycin (500 mg four times daily) and sulphametopyrazine (1 g at start of exacerbation) followed by erythromycin (500 mg four times daily) was carried out in infective exacerbations of chronic bronchitis. Ampicillin and erythromycin were found to be equally effective, but the combination of erythromycin and sulphametopyrazine was significantly less effective. Unwanted effects were more frequent with ampicillin and with erythromycin plus sulphametopyrazine than with erythromycin alone.

Adult↗
PubMedDate not supplied

Metabolism of propionyl erythromycin lauryl sulfate. I. Fate of the propionyl erythromycin moiety in the rat.

The absorption, excretion, and metabolism of propionyl erythromycin (PE) has been studied in the rat. The major routes of metabolism of PE are ester hydrolysis and N-demethylation. The rates of these two reactions have been examined in vivo using radiolabeled PE. The plasma half-life of the ester is 5.5 hr. The correlation of blood levels of radioactivity with 14CO2 production indicates that the ester is continually hydrolyzed after absorption. The half-life of the dimethyl-amino moiety of the desosamine sugar is estimated at 1.5 hr. This relatively short half-life compared to that of the ester is supported by the fact that at 3.5 hr after dosing there is twice as much desmethyl-PE in plasma as PE. After oral administration of either 14C-PE or 14C-erythromycin, 70% of the radioactivity is absorbed in 6 hr. The major route of excretion is via bile. Approximatley 40% of the absorbed dose is excreted in bile in the first 6 hr after dosing. Tissue levels of radioactivity after administration of 14C-erythromycin or 14C-PE indicate that PE or a metabolite accumulates in the tissue during chronic dosing, whereas erythromycin-related levels are similar after single or multiple doses.

Animals↗
PubMed1979

Erythromycin levels in serum during treatment with erythromycin stearate and base.

The serum concentrations of erythromycin during treatment with erythromycin stearate and erythromycin base were compared in a randomised cross-over study with 21 hospital patients. No statistically significant differences between the brands were found in the serum erythromycin levels at any time or in the areas under the serum level-time curve.

Administration, Oral↗
PubMed1978

Erythromycin VI: kinetics of acid-catalyzed hydrolysis of erythromycin oxime and erythromycylamine.

Kinetic data were obtained, by qualitative and quantitative analysis, of the hydrolytic degradation of erythromycin oxime and erythromycylamine separated by TLC. The pseudo-first-order rate constants were determined at three temperatures (17,26, and 36 degrees), and the temperature dependency of the reaction was studied. The activation energy for the hydrolysis and methanolysis of the compounds was calculated. The factors contributing to the differences in the reaction rate are discussed.

Amines↗
PubMed1976

Polyacrylic bone cement containing erythromycin and colistin. I. In vitro bacteriological activity and diffusion properties of erythromycin, colistin and erythromycin/colistin comibination.

Erythromycin and colistin demonstrate a non-antagonistic ability to inhibit the growth of a wide variety of aerobic and anaerobic bacterial isolates. When incorporated in Surgical Simplex P Radiopaque Bone Cement, fabricated cement pellets were effective in inhibiting 98% of all anaerobic and aerobic test isolates. Separate experiments indicate that each antibiotic can diffuse from polymerized cement, and that the concentration of each antibiotic is consistently above the minimum inhibitory concentration of 96% of the isolates. We conclude that erythromycin/colistin Surgical Simplex P radiopaque Bone Cement is a worthy candidate for clinical investigation.

Bone Cements↗