Biliary Excretion of Ampicillin: Experimental and Clinical Study

The biliary elimination of mezlocillin, a new semisynthetic penicillin of the acyl-ureido-penicillin group, was investigated in vitro in rabbit liver preparations and in vivo in humans. Experimentally, mezlocillin recovery in the bile during perfusion of isolated rabbit liver (3 h; n = 5) averaged 20.3% of the administered dose (10 mg). The mean peak concentration in the bile (758 ± 129.3 ,ug/ml) was reached between 0.5 and 1 h. Biliary clearance was 169 ml/h. In healthy subjects (n = 5), the concentrations of antibiotic measured in the duodenal fluid during a period of 4 h after intravenous administration of 5 g of mezlocillin ranged between 440 and 637 ,ug/ml. In 10 cholecystectomized patients provided with a T-tube, intramuscular injection of 1 g of mezlocillin resulted in a biliary peak concentration of 295.7 ± 58.1 ,ug/ml. Mean total amount of antibiotic eliminated in the bile over 12 h corresponded to 2.6% of the administered dose. Assays performed during surgery after intravenous administration of 2 g of mezlocillin (n = 10) showed antibiotic activity of 895 ± 196 ,ug/ml in the common duct bile and 402 ± 133 ytg/ ml in the gallbladder bile. These data were compared with the values determined for 11 other beta-lactamines studied under identical conditions.

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“…These investigations were part of a more general comparative study of biliary elimination of the beta-lactamines (2,3).…”

mentioning

confidence: 99%

Biliary elimination of mezlocillin: an experimental and clinical study

Jm¹,

Kopferschmitt²,

Arnaud³

et al. 1980

Antimicrob Agents Chemother

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“…Due to the oral way of administration, the serum concen tration curves observed in humans expressed both an absorption and an elimination phase, and were studied with reference to a Bateman function as suming a one-compartment model. Pharmacoki netic data (including biliary clearance, Ci" and bil iary elimination rate constant, Ki,) were determin ed applying formulas previously described [2,5].…”

Section: Clinical Study: Selection Of Patients and Procedures Cholecysmentioning

confidence: 99%

Biliary Excretion of Cefaclor

Jm¹,

Pinget²,

Comte³

et al. 1982

Chemotherapy

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Biliary excretion of cefaclor, a new orally active cephalosporin, was studied in vitro using an isolated rabbit liver preparation perfused for 3 h (n = 5). Under these conditions, bile recovery amounted to 2.3% of the cefaclor dose added to the circulating blood (10 mg). In humans, after oral administration of a 1-gram dose of cefaclor to cholecystec-tomized patients provided with a T tube (n = 10), a mean biliary peak concentration of 7.6 ± 2.4 µg/ml was observed at the 3rd hour. Cumulative biliary excretion amounted to 0.05% of the administered dose. Assays performed on samples collected during chole-cystectomy in 10 patients 1 h after intake of a 1-gram dose of cefaclor showed mean concentrations of 13.7 ± 1.2 µg/ml in serum, 8.1 ± 1.3 µg/ml in common duct bile and 5.9 ± 1.4 µg/ml in gallbladder bile. These results were compared with the data obtained after administration of seven other cephalosporins studied under identical conditions.

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Pharmacokinetics of β-Lactam Antibiotics

Kwan¹

1983

Antibiotics

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Biliary Excretion of Ampicillin: Experimental and Clinical Study

Cited by 8 publications

References 6 publications

Biliary elimination of mezlocillin: an experimental and clinical study

Biliary elimination of mezlocillin: an experimental and clinical study

Biliary Excretion of Cefaclor

Pharmacokinetics of β-Lactam Antibiotics

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