Pharmacokinetics of High‐Dose Oral Cephalosporins

Chow, Moses S. S.; Quintiliani, Richard; Cunha, Burke A.; Thompson, M I; Finkelstein, Elaine R.; Nightingale, Charles H.

doi:10.1002/j.1552-4604.1979.tb01650.x

Cited by 14 publications

(10 citation statements)

References 11 publications

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“…However, since cephalexin does not suffer hepatic biotransformation, being completely eliminated by renal excretion, k is equal to ku. The results obtained for products A and B were in agreement with data described by Chow and colleagues (1979) and Finkelstein and colleagues (1978), which found k values of 0.015 ± 0.003 min -1 (Chow et al, 1979;Finkelstein et al, 1978).…”

Section: Bioequivalence Studysupporting

confidence: 82%

“…The medium values of elimination half-life (t(½) b ) for normal individuals are in agreement with that described by other authors, in the range of 36 to 126 min (Nightingale, Greene, Quintiliani, 1975). Mean values of 50 ± 10 min after oral administration to normal fasting individuals were reported (Chow et al, 1979;Finkelstein et al, 1978;Greene et al, 1976). Concomitant administration of food changes the elimination half-life to 77 min (Greene, Quintiliani, Nightingale, 1975).…”

Section: Bioequivalence Studysupporting

confidence: 78%

“…In adults with normal renal function, following oral administration of a single 250-500 mg dose, peak blood concentration can be obtained within 1 hour. Approximately 70-90% of cephalexin is excreted unchanged in urine (Chow et al, 1979;Ding et al, 2011;Nightingale, Greene, Quintiliani, 1975).…”

Section: Introductionmentioning

confidence: 99%

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Dissolution efficiency and bioequivalence study using urine data from healthy volunteers: a comparison between two tablet formulations of cephalexin

Serra

Chang

Dezani

et al. 2015

Braz. J. Pharm. Sci.

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The aim of the present study was to assess the bioequivalence of two cephalexin tablet formulations available in the Brazilian market (product A as reference formulation and product B as test formulation). Dissolution efficiency (DE%) was calculated for both formulations to evaluate their in vitro biopharmaceutical features. The oral bioequivalence study was performed in twenty-four healthy volunteers in a crossover design. Single oral dose (tablet containing 500 mg of cephalexin) of each product was administered with two weeks of washout period. Urinary concentrations of cephalexin were measured by high-performance liquid chromatography (HPLC) method and pharmacokinetics parameters were estimated by urinary excretion data. The bioequivalence was determined by the following parameters: the cumulative amount of cephalexin excreted in the urine, the total amount of cephalexin excreted in the urine and the maximum urinary excretion rate of cephalexin. DE values of immediaterelease cephalexin tablets (500 mg) were 68.69±4.18% for product A and 71.03±6.63% for product B.Regarding the dissolution test of the two brands (A and B) analysed, both were in compliance with the official pharmacopeial specifications, since the dissolution of both formulations was superior to 80% of the amount declared in the label after 45 minutes of test (A=92.09%±1.84; B=92.84%±1.08). The results obtained indicated that the products A and B are pharmaceutical equivalents. Confidence intervals for the pharmacokinetic parameters were in compliance with the international standards, indicating that products A and B can be considered bioequivalents and, therefore, interchangeable.Uniterms: Tablets/formulations/bioequivalence study. Cephalexin/dissolution efficiency.O objetivo do presente estudo foi avaliar a bioequivalência de duas formulações de cefalexina disponíveis no mercado brasileiro (produto A como formulação referência e produto B como formulação teste). A eficiência de dissolução (DE%) foi calculada para ambas as formulações para avaliar suas características biofarmacêuticas. O estudo de bioequivalência oral foi realizado em vinte e quatro voluntários sadios utilizando um desenho cruzado. Uma dose oral única (comprimido contendo 500 mg de cefalexina) de cada produto foi administrada com um período de washout de duas semanas. Concentrações urinárias de cefalexina foram mensuradas por método de cromatografia líquida de alta eficiência (CLAE) e os parâmetros farmacocinéticos foram estimados por dados de excreção urinária. A bioequivalência foi determinada pelos seguintes parâmetros: quantidade acumulada da cefalexina excretada na urina, quantidade total da cefalexina excretada na urina e a taxa de excreção máxima da cefalexina. Os valores de DE dos comprimidos de liberação imediata de cefalexina (500 mg) foram 68,69±4,18% para o produto A e de 71,03±6,63% para o produto B. Com relação ao teste de dissolução das duas marcas analisadas (A e B), ambas apresentaram-se de acordo com as especificações farmacopéicas, uma vez que a dissolução de ...

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Section: Bioequivalence Studysupporting

confidence: 82%

Section: Bioequivalence Studysupporting

confidence: 78%

See 1 more Smart Citation

Dissolution efficiency and bioequivalence study using urine data from healthy volunteers: a comparison between two tablet formulations of cephalexin

Serra

Chang

Dezani

et al. 2015

Braz. J. Pharm. Sci.

View full text Add to dashboard Cite

show abstract

“…As suggested earlier, cephalexin is well absorbed following a wide range (0.125-2.0 g) of oral doses administered as capsule, tablet, solution, or suspension (THORNHILL et al 1969;GOWER and DASH 1969;BERGAN et al 1970;GRIFFITH and BLACK 1971;O'CALLAGHAN et al 1971;LoDE et al 1979;BARRIOS et al 1975;Ac-TOR et al 1976a;PFEFFER et al 1977;HARTSTEIN et al 1977;HENNESS et al 1978;FINKELSTEIN et al 1978;CHOW et al 1979;BUSTRACK et al 1980;SIMON 1980 a;LE-CAILLON et al 1980;LODE et al 1980c). Peak serum concentrations of cephalexin occur within 1-2 h, dependent upon the formulation.…”

Section: Cephalexinmentioning

confidence: 88%

Pharmacokinetics of β-Lactam Antibiotics

Kwan¹

1983

Antibiotics

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“…A comparison of cephalexin kinetics among our patients and normal volunteers or non-CF patients reported previously [1,3,9,12,14] suggests that cephalexin clearance may not increase in CF of minimal severity characterized by excellent Shwachman score. This differs from previous studies with semisynthetic penicillins [5,15] and aminoglycosides [2,6,7] in CF.…”

Section: Discussionmentioning

confidence: 99%

Cephalexin Pharmacokinetics in Patients with Cystic Fibrosis

Mc¹,

Ah²,

Ja³

1984

Dev Pharmacol Ther

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Pharmacokinetics of cephalexin were studied in 7 pediatric and 4 adult patients with cystic fibrosis (CF) and 4 normal adult volunteers. Cephalexin, 250-500 mg. was given as a single dose in suspension. The area under the cephalexin serum concentration-time curve normalized for dose per kilogram averaged 0.185, 0.242, and 0.272 ml/min/kg^-1 in pediatric CF patients, adult CF patients, and normal adults, respectively (p > 0.05). A threefold interindividual variation was observed in cephalexin renal clearance in CF patients. Renal clearance of cephalexin averaged 5.85 ml/min/kg in pediatric and 4.61 ml/min/kg in adult CF patients (p > 0.05). Elimination half-life of cephalexin averaged 0.74, 0.76, and 1.04 h in pediatric patients, adult patients, and normal adults (p > 0.05). Cephalexin was well absorbed based on a mean 24-hour urinary recovery of 89 and 93% in pediatric and adult patients. A trend for higher renal clearance of cephalexin was observed among pediatric compared to adult patients. These results indicate that clearance of cephalexin may not increase in patients with CF of minimal severity characterized by an excellent Shwachman score.

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Pharmacokinetics of High‐Dose Oral Cephalosporins

Cited by 14 publications

References 11 publications

Dissolution efficiency and bioequivalence study using urine data from healthy volunteers: a comparison between two tablet formulations of cephalexin

Dissolution efficiency and bioequivalence study using urine data from healthy volunteers: a comparison between two tablet formulations of cephalexin

Pharmacokinetics of β-Lactam Antibiotics

Cephalexin Pharmacokinetics in Patients with Cystic Fibrosis

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