title: Effect of Lactobacillus casei on the absorption of nifedipine from rat small intestine.
abstract: Lactobacillus casei Shirota strain (L. casei) has a modulating effect on the production of cytokines, which often play important roles in drug metabolism, in the inflamed intestinal mucosa. We evaluated the effect of L. casei administered orally in advance for 4 weeks on the absorption of nifedipine from the rat small intestine. The maximum concentration of nifedipine in plasma after administration into the intestinal loop (0.8 mg/kg) was significantly higher in L. casei-treated rats (3.26 microg/mL) than in those untreated rats (2.33 microg/mL) by 40%. Accordingly, the bioavailability of nifedipine was tended to be higher in the former, while the effect of L. casei on the disposition of intravenously administered nifedipine was negligible. We also found that the availability of nifedipine for the passage through the intestinal mucosa was significantly increased in L. casei-treated rats from the single-pass intestinal perfusion experiments. Therefore, it is likely that the exposure to nifedipine after its administration into rat intestine was increased by oral ingestion of L. casei due to an increase in absorption by increased intestinal availability (decreased metabolic extraction) during passage through the intestinal mucosa. This study has suggested that L. casei has some effect on the metabolic activity in the intestinal mucosa, though it seems to be only mild.
authors.affiliation: Department of Clinical Pharmacy and Clinical Pharmacokinetics, Osaka University of Pharmaceutical Sciences, Japan. rkato@gly.oups.ac.jp
authors.forename: Ryuji
authors.initials: R
authors.lastname: Kato
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Yuasa
authors.forename: Katsuhisa
authors.initials: K
authors.lastname: Inoue
authors.forename: Takahiro
authors.initials: T
authors.lastname: Iwao
authors.forename: Kazuhiko
authors.initials: K
authors.lastname: Tanaka
authors.forename: Kazuya
authors.initials: K
authors.lastname: Ooi
authors.forename: Yayoi
authors.initials: Y
authors.lastname: Hayashi
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002121:Calcium Channel Blockers / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D051544:Cytochrome P-450 CYP3A / Q000378:metabolism; D007275:Injections, Intravenous; D007408:Intestinal Absorption; D007421:Intestine, Small / Q000201:enzymology / Q000378:metabolism* / Q000382:microbiology; D007780:Lacticaseibacillus casei; D008297:Male; D008954:Models, Biological; D009543:Nifedipine / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D019936:Probiotics; D051381:Rats; D017208:Rats, Wistar
chemical_list: D002121:Calcium Channel Blockers; D051544:Cytochrome P-450 CYP3A; D009543:Nifedipine