Active transport of benzylpenicillin across the blood-milk barrier
Autor: | Folke Rasmussen, Hans-Hasso Frey, Carl-Christian Merck, Angelika-Maria Schadewinkel-Scherkl, Poul Nielsen |
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Rok vydání: | 1993 |
Předmět: |
medicine.medical_specialty
Health Toxicology and Mutagenesis Biological Transport Active Absorption (skin) Toxicology Benzylpenicillin Epithelium Absorption Absorption rate chemistry.chemical_compound Mammary Glands Animal Internal medicine polycyclic compounds medicine Animals Infusions Parenteral Infusions Intravenous Chromatography High Pressure Liquid Pharmacology Chromatography Probenecid organic chemicals Goats Area under the curve food and beverages Penicillin G biochemical phenomena metabolism and nutrition Endocrinology Blood Milk chemistry Plasma concentration Urea Systemic administration bacteria Cattle Female medicine.drug Half-Life |
Zdroj: | Pharmacologytoxicology. 73(1) |
ISSN: | 0901-9928 |
Popis: | Passage of benzylpenicillin across the mammary gland epithelium was studied both after systemic administration of benzylpenicillin in four goats and after intramammary infusion in three goats and two cows. The results after benzylpenicillin administration alone were compared with the results after combined administration of benzylpenicillin and probenecid. The studies on passage of benzylpenicillin through the blood-milk barrier showed, when milk to plasma ultrafiltrate ratios of benzylpenicillin were plotted versus time for each half of the udders, that active transport takes place from blood to milk during steady-state plasma concentrations. Active transport was demonstrated by inhibition with probenecid: (1) The entry of benzylpenicillin into milk was slowed down under the influence of probenecid. The AUC (area under the curve)-values during the first 30 min. were reduced by 66 +/- 9% compared with the AUC-values found without coadministration of probenecid. (2) In the presence of probenecid and during equilibrium between blood and milk concentrations, benzylpenicillin reached concentration ratios in the ultrafiltrates of milk and plasma which corresponded to those expected for diffusion alone. Without probenecid these ultrafiltrate concentration ratios were more than two times higher indicating an active transport of benzylpenicillin from blood to milk. After intramammary infusion of benzylpenicillin, active transport was demonstrated from milk into blood. The absorption rate for benzylpenicillin from the mammary gland was reduced by probenecid, as measured by the ratio of benzylpenicillin to urea absorption half-life, which was increased by 40-50% in the presence of probenecid. |
Databáze: | OpenAIRE |
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