Drug Bioavailability Information and Its Utility

Chun, Alexander; Seitz, J. A.

doi:10.1016/s0003-0465(16)34349-x

Cited by 7 publications

(2 citation statements)

References 12 publications

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“…Large intersubject variability in serum concentrations of erythromycin occurs after oral administration even under standardised conditions (Chun & Seitz, 1974. It has been shown that intersubject variability in pharmacokinetic parameters after intravenous erythromycin is small (Austin et al, 1980), hence it may be inferred that the majority of intersubject variability is due to erratic absorption and differences in absolute bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Absorption and bioavailability of oral erythromycin.

Mather

Austin

Philpot

et al. 1981

Brit J Clinical Pharma

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1 Extent and rate of absorption of erythromycin were studied in 24 healthy volunteers whose disposition kinetics after i.v. injections had been previously documented. 2 Two clinically attractive oral dosage regimens were administered: erythromycin stearate tablets 1 h before meals (Regimen A), and erythromycin base capsules 30 min after start of meals (Regimen B), each equivalent to erythromycin 250 mg, 6 h apart for 9 doses. 3 Serum concentrations of erythromycin measured during the 1st and 9th (steady-state) dosing intervals resulted in higher maximum serum concentrations for Regimen A (median 1.1, range 0-3.3 and 2.7, 0.6-7.3 mg/l for Doses 1 and 9, respectively) compared with Regimen B (0.4, 0-2.2 and 1.4, 0.2-4.9 mg/l). 4 Absorption occurred earlier with Regimen A with times to maximum concentrations (median, range) being 128, 60-greater than 360 and 118, 75-210 min for doses 1 and 9 respectively, (lag times 75, 15- greater than 360 and 73, 10-110 min) compared with 303, 130-greater than 360 and 173, 45-greater than 360 min (lag times 183, 70-greater than 360 and 190, 20-330 min) for Regimen B. 5 Where it could be assessed, absolute bioavailability for Regimen A was approximately 30% (Dose 1) and 65% (Dose 9) and 40% for both doses of Regimen B. 6 Whereas individual serum concentration-time curves were accurately predicted by the mean for Regimen A, predictability for Regimen B was impossible due to prolonged and variable lag time. 7 The large intersubject variability in erythromycin serum concentration after oral administration, has been shown conclusively to be related to variability in absorption kinetics and absolute bioavailability rather than to variability in disposition kinetics.

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Section: Introductionmentioning

confidence: 99%

Absorption and bioavailability of oral erythromycin.

Mather

Austin

Philpot

et al. 1981

Brit J Clinical Pharma

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“…Erythromycin is unstable under the acidic conditions of the stomach or in pH values less than 4.0 (4). Large intersubject variability in serum concentration occurs after oral administration even under standardized conditions (5,6), whereas intersubject variability in pharmacokinetic parameters after intravenous erythromycin is small (7), indicating that the majority of intersubject variability is due to erratic absorption and differences in absolute bioavailability. Due to this reason, the drug was listed by the American Pharmacy Association Academy of Pharmaceutical Sciences as having serious bioavailability and/or quality assurance problems.…”

Section: Introductionmentioning

confidence: 99%

Studies of Erythromycin Maltobionate, a New Derivative of Erythromycin

Manna

Basu

1999

Drug Development and Industrial Pharmacy

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Erythromycin maltobionate, a new water-soluble derivative of erythromycin, was prepared, and its physiochemical and biological properties were evaluated. The derivative has considerable solubility in organic solvents. Its partition coefficient data in different organic solvent-water systems indicate it is possibly well distributed in various tissues in vivo. Antimicrobial potency in vitro of the derivative is 589 micrograms/mg, and its antimicrobial spectrum is comparable to that of the parent antibiotic. The LD50 value of the new derivative in mice intraperitoneally is 244.7 mg/kg. Results of this and the previous investigation of pharmacokinetics and protein binding indicate that the new derivative erythromycin maltobionate has a potential for possible clinical application.

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Single-dose fasting bioequivalence assessment of erythromycin stearate tablets in man

Yakatan

Poynor

Harris

et al. 1979

Journal of Pharmacokinetics and Biopharmaceutics

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The bioequivalence of film-coated erythromycin stearate tablets produced by five different manufacturers was evaluated in a balanced incomplete block design involving the five formulations given to 30 fasted subjects over a 3-week study period. Serum levels of erythromycin activity were determined microbiologically. Statistical analysis of variance was performed on the observed bioavailability parameters: maximum serum concentration (Cmax), time to maximum serum concentration (Tmax), and area under the serum concentration-time curve (AUC). There was no statistical difference between formulations for the Tmax parameter. Formulation differences were found, however, based on the analysis of variance of the Cmax and AUC parameters. Two products, although not significantly different from one another, showed significantly greater Cmax and AUC values than the other three products.

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Drug Bioavailability Information and Its Utility

Cited by 7 publications

References 12 publications

Absorption and bioavailability of oral erythromycin.

Absorption and bioavailability of oral erythromycin.

Studies of Erythromycin Maltobionate, a New Derivative of Erythromycin

Single-dose fasting bioequivalence assessment of erythromycin stearate tablets in man

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