Oral absorption efficiency of acid-labile antibiotics from lipid-drug delivery systems.
The utility of cholesterol, cholesteryl acetate, and beta-sitosterol in protecting and improving the oral absorption efficiency of acid-labile antibiotics is discussed. The potassium salts of penicillin G and penicillin V and erythromycin lactobionate were studied. The stability of the two penicillins in simulated gastric fluid was determined iodometrically. The rank order of acid protective activity was: cholesteryl acetate greater than beta-sitosterol greater than cholesterol. Oral administration of erythromycin lactobionate coated with cholesteryl acetate produced a twofold increase in human urinary excretion of erythromycin when compared with the uncoated material. Potassium salts of penicillin G and penicillin V coated with cholesteryl acetate yielded 1.6- and 2-fold higher urine levels, respectively, as compared with the uncoated candidates.
D000042:Absorption; D000284:Administration, Oral; D000328:Adult; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000378:metabolism*; D001682:Biological Availability; D002784:Cholesterol; D004355:Drug Stability; D004917:Erythromycin / Q000378:metabolism; D006801:Humans; D008055:Lipids; D008297:Male; D010400:Penicillin G / Q000378:metabolism; D010404:Penicillin V / Q000378:metabolism; D014677:Pharmaceutical Vehicles; D012855:Sitosterols; D013608:Tablets, Enteric-Coated
D000900:Anti-Bacterial Agents; D008055:Lipids; D014677:Pharmaceutical Vehicles; D012855:Sitosterols; D013608:Tablets, Enteric-Coated; D004917:Erythromycin; D002784:Cholesterol; D010400:Penicillin G; D010404:Penicillin V