Pharmacokinetics and biological availability of erythromycin

Chun, Alexander; Seitz, J. A.

doi:10.1007/bf01639131

Cited by 32 publications

(20 citation statements)

References 13 publications

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“…However, considerable variability and unpredictability in serum concentrations result from doses administered this way (Chun & Seitz, 1977;Parsons, Haddock & Hossack, 1975). It is not known how much of the variability is derived from the absorption, or the distribution and elimination of erythromycin.…”

Section: Introductionmentioning

confidence: 99%

Intersubject and dose‐related variability after intravenous administration of erythromycin.

Austin¹,

Mather²,

Philpot³

et al. 1980

Brit J Clinical Pharma

110

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1 It is well‐known that considerable variability and unpredictability in serum concentrations results from orally administered erythromycin. 2 Disposition kinetics and their variability were studies in 24 healthy subjects after a single dose of erythromycin lactobionate and four doses were studied to evaluate dose‐related variability in five other subjects. 3 Erythromycin kinetics were adequately described by a classical two compartment open model with little intersubject variability. 4 Dose‐related variability occurred. Clearance was independent of dose but T1/2 beta and Vdss increased with dose. 5 Data are presented to show that non‐invasive sampling of urine and saliva are of limited value in studying erythromycin pharmacokinetics.

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Section: Introductionmentioning

confidence: 99%

Intersubject and dose‐related variability after intravenous administration of erythromycin.

Austin¹,

Mather²,

Philpot³

et al. 1980

Brit J Clinical Pharma

110

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“…However, erythromycin is sensitive to inactivation by gastric acid, and some preparations are poorly absorbed unless taken before food (1,8,14). Erythromycin ethyl succinate has been available as granules and a suspension for pediatric use, and studies with this preparation taken under nonfasting conditions suggest that its bioavailability is not affected by food (3,5,6,9). The purpose of this study was to determine the effect of food on the absorption of a new tablet formulation of erythromycin ethyl succinate.…”

mentioning

confidence: 99%

Influence of food on absorption of erythromycin ethyl succinate

Thompson¹,

Burgess²,

Marlin³

1980

Antimicrob Agents Chemother

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Erythromycin plasma concentrations were determined in 18 subjects after a single dose (800 mg) of a new formulation of erythromycin ethyl succinate taken immediately before, immediately after, and 1 h after food. Adequate absorption occurred with all treatments, although bioavailability was best when the drug was taken before food. Absorption was delayed by food, with the highest and earliest peak plasma erythromycin levels occurring under fasting conditions. Erythromycin is widely used for the treatment of a variety of infectious diseases, including respiratory tract infections, for which many strains of common upper and lower respiratory pathogens are inhibited by this antibiotic. However, erythromycin is sensitive to inactivation by gastric acid, and some preparations are poorly absorbed unless taken before food (1,8,14). Erythromycin ethyl succinate has been available as granules and a suspension for pediatric use, and studies with this preparation taken under nonfasting conditions suggest that its bioavailability is not affected by food (3,5,6,9). The purpose of this study was to determine the effect of food on the absorption of a new tablet formulation of erythromycin ethyl succinate.Methods. Eighteen healthy subjects (14 males and four females), aged from 20 to 25 years, volunteered for this study. Written consent was given by each subject after the procedure of the study had been fully explained. No antibiotic or other drug therapy had been received for 2 weeks before the commencement of or during the study period. The subjects fasted from midnight before all study days.The fornulation of erythromycin administered in this study was erythromycin ethyl succinate, 800 mg (400-mg film tablet; 5729, Abbott Laboratories). The study was a balanced, randomized Latin square design and was performed on 3 separate days at weekly intervals. The three treatments were: (i) erythromycin ethyl succinate, 800 mg, administered immediately before food; (ii) erythromycin ethyl succinate, 800 mg, administered immediately after food; (iii) erythromycin ethyl succinate, 800 mg, administered 1 h after food. A standard breakfast consisting of cereal with milk, toast, and fruit juice was eaten over a period of 15 min. The drug was given with 120 ml of water. No other food or drinks were allowed until 4 h after drug ingestion.Venous blood samples were collected immediately before drug ingestion and subsequently at 0.5, 1, 1.5, 2, 3, 4, 6, and 8 h after ingestion for erythromycin plasma level determination. Before drug administration, blood was also collected for a biochemical profile (electrolytes, urea, creatinine, protein, albumin, uric acid, bilirubin, alkaline phosphatase, lactic acid dehydrogenase, glutamic oxaloacetic transaminase, and glucose) and a full blood count. The subjects were asked to report any unwanted effects during the study.The assay method for plasma erythromycin followed that described by Bell et al. (2)

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“…however, are situated in the lower range of the AUC for healthy volunteers reported ear lier (table II). Higher AUC was reported for pellets [5]; for stearate tablets [1,3,5,10]; for ethylsuccinate [1,11], Also relatively low peak levels and AUC were found for enteric coated pellets [12.13], for enteric coated tab lets [14], for stearate tablets [15,16] and for ethylsuccinate [9,14], Different meals, vary ing timing of food intake and erythromycin drug ingestion and volumes of fluid taken with a drug may have a marked influence on erythromycin absorption [3], In addition, our subjects constituted a very young and homog enous age group (20-25 years) with presum ably maximal capacity for drug elimination. The relatively short reaction times for stea rate (0.7 h) and ethylsuccinate (0.5 h) were anticipated since these products are not en teric coated (1.2-1.8 h).…”

Section: Discussionmentioning

confidence: 99%

“…The most important are the spe cific form of the erythromycin molecule, the coating of the product, the number of doses given, the interval between food intake and dose, and the volume of fluid accompanying drug intake [1][2][3]. Erythromycin stearate is a salt and dissociates in the duodenum giving erythromycin base, which is then absorbed.…”

Section: Introductionmentioning

confidence: 99%

Relative Bioavailability of Enteric Coated Pellets, Stearate and Ethylsuccinate Formulations of Erythromycin

Tjandramaga¹,

Hecken²,

Mullie³

et al. 1984

Pharmacology

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In a randomized three-phase crossover study, 12 healthy male volunteers were given three 12-hourly 500-mg doses of erythromycin base, as enteric coated pellets in capsules (2 × 250 mg), erythromycin stearate tablet (1 × 500 mg), or erythromycin ethylsuccinate sachet (1 × 500 mg). The reaction time after administration of the pellets is significantly longer than after the stearate or ethylsuccinate formulations. The peak serum concentrations are higher for the pellets after both the 1st and 3rd dose. The time to reach peak concentrations is significantly longer for the pellets than for the stearate and ethylsuccinate formulations. The area under the serum concentration/time curve during 0–8 h after both doses is highest for the pellets. In conclusion, these findings indicate that despite the longer lag (1.8–1.2 h), the extent of gastrointestinal absorption and bioavailability of erythromycin is apparently greater for the base pellets than for the stearate and ethylsuccinate formulations.

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Pharmacokinetics and biological availability of erythromycin

Cited by 32 publications

References 13 publications

Intersubject and dose‐related variability after intravenous administration of erythromycin.

Intersubject and dose‐related variability after intravenous administration of erythromycin.

Influence of food on absorption of erythromycin ethyl succinate

Relative Bioavailability of Enteric Coated Pellets, Stearate and Ethylsuccinate Formulations of Erythromycin

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