Effect of Isoxazolyl-penicillin on the Rectal Absorption of Ampicillin in Rabbits and Humans

• Published in: Chemical & pharmaceutical bulletin Vol. 31; no. 5; pp. 1708 - 1713
• Main Authors: MURAKAMI, TERUO, YATA, NOBORU, KAMADA, AKIRA
• Format: Journal Article
• Language: English
• Published: Tokyo The Pharmaceutical Society of Japan 01.01.1983; Maruzen; Japan Science and Technology Agency
• Subjects: Adult; Ampicillin - metabolism; Animals; Antibacterial agents; Antibiotics. Antiinfectious agents. Antiparasitic agents; Biological and medical sciences; Humans; Intestinal Absorption - drug effects; Male; Medical sciences; Middle Aged; Penicillins - pharmacology; Pharmacology. Drug treatments; promoting effect of isoxazolyl-penicillins for rectal absorption of ampicillin; Rabbits; Rectum - metabolism; Species Specificity; Human; Animal
• ISSN: 0009-2363; 1347-5223
• DOI: 10.1248/cpb.31.1708

The effects of isoxazolyl-penicillins on the rectal absorption of ampicillin were investigated in rabbits and humans. The bioavailability of ampicillin following administration of a suppository in the presence or absence of an isoxazolyl-penicillin was determined from the blood level in rabbits and from the urinary excretion (0-6 h) in humans. Rectal absorption of ampicillin from the suppository was enhanced by the presence of an isoxazolyl-penicillin in both rabbits and humans, though the effect was much greater in rabbits than in humans. The absorption-promoting effects of isoxazolyl-penicillins appeared to be related to their partition coefficients between n-octanol and buffer solution (pH 7.4).