Absorption of ester prodrugs in Caco-2 and rat intestine models

Antimicrobial Agents and Chemotherapy

Volumn 48, Issue 7, 2004, Pages 2604-2609

  He, Xin ^a   Sugawara, Mitsuru ^a   Takekuma, Yoh ^a   Miyazaki, Katsumi ^a  

^a HOKKAIDO UNIVERSITY HOSPITAL   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

4 NITROPHENYL ACETATE; ACETIC ACID DERIVATIVE; AMPICILLIN; CEFCAPENE PIVOXIL; ESTERASE; PIVAMPICILLIN; PRODRUG; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; CELL STRAIN CACO 2; DRUG ABSORPTION; DRUG DEGRADATION; DRUG HYDROLYSIS; DRUG METABOLISM; DRUG SOLUBILITY; DRUG TRANSPORT; ENZYME ACTIVITY; GASTROINTESTINAL TRACT; INTESTINE EPITHELIUM; INTESTINE MUCOSA PERMEABILITY; JEJUNUM; MALE; MONOLAYER CULTURE; NONHUMAN; PRIORITY JOURNAL; RAT; STOMACH PH;

ANIMALS; CACO-2 CELLS; CEPHALOSPORINS; EPITHELIAL CELLS; ESCHERICHIA COLI; ESTERS; GRAM-NEGATIVE BACTERIA; GRAM-POSITIVE BACTERIA; HUMANS; HYDROGEN-ION CONCENTRATION; INTESTINAL ABSORPTION; INTESTINES; MALE; NITROPHENOLS; PRODRUGS; RATS; RATS, WISTAR; SERRATIA; SPECTROPHOTOMETRY, ULTRAVIOLET; STAPHYLOCOCCUS AUREUS;

EID: 3042533894     PISSN: 00664804     EISSN: None     Source Type: Journal    
DOI: 10.1128/AAC.48.7.2604-2609.2004     Document Type: Article

References (14)

1. Augustijns, P., P. Annaert, P. Heylen, G. Van den Mooter, and R. Kinget. 1998. Drug absorption studies of prodrug esters using the Caco-2 model: evaluation of ester hydrolysis and transepithelial transport. Int. J. Pharm. 166:45-53.
2. Balant, L. P., E. Doelker, and P. Buri. 1990. Prodrugs for the improvement of drug absorption via different routes of administration. Eur. J. Drug Metab. Dispos. 15:143-153.
3. Fujimoto, M. 2001. Pharmacokinetics of cefcapene pivoxil and AS-924 in gastrectomized patients. Int. J. Antimicrob. Agents 18:489-494.
4. He, X., S. Kadomura, Y. Takekuma, M. Sugawara, and K. Miyazaki. 2004. A new system for prediction of drug absorption using a pH-controlled Caco-2 model: evaluation of pH-dependent soluble drug absorption and pH-related changes in absorption. J. Pharm. Sci. 93:71-77.
5. He, X., M. Sugawara, M. Kobayashi, Y. Takekuma, and K. Miyazaki. 2003. An in vitro system for prediction of oral absorption of relatively water-soluble drugs and ester prodrugs. Int. J. Pharm. 263:35-44.
6. Hidalgo, I. J., T. J. Raub, and R. T. Borchardt. 1989. Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability. Gastroenterology 96:736-749.
7. Hilgers, A. R., R. A. Conradi, and P. S. Burton. 1990. Caco-2 cell monolayers as a model for drug transport across the intestinal mucosa. Pharm. Res. 7:902-910.
8. Kimura, Y., M. Nakano, H. Nakasimizu, S. Nakamoto, Y. Watanabe, and S. Otubo. 1993. Study on the pharmacokinetics of S-1008 in experimental animals, a new ester-type oral cephem antibiotic. Chemotherapy 41(Suppl. 1):163-176.
9. Lowry, O. H., N. J. Rosebrough, A. L. Farr, and R. J. Randall. 1951. Protein measurement with the folin phenol regent. J. Biol. Chem. 193:265-275.
10. 14C]-S-1008 in rats and dogs. Chemotherapy 41(Suppl. 1):177-188.
11. Nakajima, M., T. Uematsu, T. Oguma, T. Yoshida, Y. Kimura, and M. Konishi. 1993. Phase I clinical study of S-1008, a new ester-type cephem antibiotic. Chemotherapy 41(Suppl. 1):109-125.
12. Saha, P., and J. H. Kou. 2002. Effect of bovine serum albumin on drug permeability estimation across Caco-2 monolayers. Eur. J. Pharm. Biopharm. 54:319-324.
13. Tanimura, H., K. Johata, H. Kashiwagi, Y. Aoki, S. Oka, and M. Nakamura. 1993. Biliary excretion and clinical efficacy of S-1008 in surgical infections. Chemotherapy 41(Suppl. 1):566-577.
14. Taylor, M. D. 1996. Improved passive oral drug delivery via prodrugs. Adv. Drug Deliv. Rev. 19:131-148.