Dynamic analysis of fluid distribution in the gastrointestinal tract in rats: Positron emission tomography imaging after oral administration of nonabsorbable marker, [18F]deoxyfluoropoly(ethylene glycol)

Molecular Pharmaceutics

Volumn 10, Issue 6, 2013, Pages 2261-2269

  Takashima, Tadayuki ^a   Shingaki, Tomotaka ^a,b   Katayama, Yumiko ^a   Hayashinaka, Emi ^a   Wada, Yasuhiro ^a   Kataoka, Makoto ^c   Ozaki, Daiki ^a   Doi, Hisashi ^a   Suzuki, Masaaki ^a   Ishida, Sho ^d   Hatanaka, Kentaro ^d   Sugiyama, Yuichi ^a   Akai, Shuji ^d   Oku, Naoto ^d   Yamashita, Shinji ^c   Watanabe, Yasuyoshi ^a  

^a RIKEN   (Japan)

^b ADME Research Inc   (Japan)

^c SETSUNAN UNIVERSITY   (Japan)

^d UNIVERSITY OF SHIZUOKA   (Japan)

Author keywords

deoxyfluoropoly(ethylene glycol)s (FPEG); effective fluid volume; gastrointestinal transit; oral absorption; positron emission tomography (PET)

Indexed keywords

DEOXYFLUOROPOLY(ETHYLENE GLYCOL) F 18; TRACER; UNCLASSIFIED DRUG; WATER;

ANIMAL EXPERIMENT; ARTICLE; BLOOD SAMPLING; DRUG BIOAVAILABILITY; DRUG ELIMINATION; GASTROINTESTINAL ABSORPTION; GASTROINTESTINAL TRACT; IMAGE ANALYSIS; INTESTINE MUCOSA; MALE; METABOLITE; MOLECULAR WEIGHT; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; RADIOACTIVITY; RAT; SMALL INTESTINE; STOMACH; TISSUE DISTRIBUTION;

ADMINISTRATION, ORAL; ANIMALS; ETHYLENE GLYCOL; GASTROINTESTINAL TRACT; MALE; POSITRON-EMISSION TOMOGRAPHY; RATS; RATS, SPRAGUE-DAWLEY;

EID: 84878660237     PISSN: 15438384     EISSN: 15438392     Source Type: Journal    
DOI: 10.1021/mp300469m     Document Type: Article

References (29)

1. Artursson, P.; Karlsson, J. Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells Biochem. Biophys. Res. Commun. 1991, 175 (3) 880-5
2. Irvine, J. D.; Takahashi, L.; Lockhart, K.; Cheong, J.; Tolan, J. W.; Selick, H. E.; Grove, J. R. MDCK (Madin-Darby canine kidney) cells: A tool for membrane permeability screening J. Pharm. Sci. 1999, 88 (1) 28-33
3. Salphati, L.; Childers, K.; Pan, L.; Tsutsui, K.; Takahashi, L. Evaluation of a single pass intestinal-perfusion method in rat for the prediction of absorption in man J. Pharm. Pharmacol. 2001, 53, 1007-1013
4. Azad Khan, A. K.; Piris, J.; Truelove, S. C. An experiment to determine the active therapeutic moiety of sulphasalazine Lancet 1977, 2 (8044) 892-5
5. Hatanaka, S.; Kondoh, M.; Kawarabayashi, K.; Furuhama, K. The measurement of gastric emptying in conscious rats by monitoring serial changes in serum acetaminophen level J. Pharmacol. Toxicol. Methods 1994, 31 (3) 161-5
6. Murata, K.; Noda, K.; Kohno, K.; Samejima, M. Pharmacokinetic analysis of concentration data of drugs with irregular absorption profiles using multi-fraction absorption models J. Pharm. Sci. 1987, 76 (2) 109-13
7. Yuen, K. H. The transit of dosage forms through the small intestine Int. J. Pharmaceutics 2010, 395 (1-2) 9-16
8. Kimura, T.; Higaki, K. Gastrointestinal transit and drug absorption Biol. Pharm. Bull. 2002, 25 (2) 149-64
9. Haruta, S.; Kawai, K.; Jinnouchi, S.; Ogawara, K. I.; Higaki, K.; Tamura, S.; Arimori, K.; Kimura, T. Evaluation of absorption kinetics of orally administered theophylline in rats based on gastrointestinal transit monitoring by gamma scintigraphy J. Pharm. Sci. 2001, 90 (4) 464-73
10. Schiller, C.; Frohlich, C. P.; Giessmann, T.; Siegmund, W.; Monnikes, H.; Hosten, N.; Weitschies, W. Intestinal fluid volumes and transit of dosage forms as assessed by magnetic resonance imaging Aliment Pharmacol. Ther. 2005, 22 (10) 971-9
11. Shingaki, T.; Takashima, T.; Wada, Y.; Tanaka, M.; Kataoka, M.; Ishii, A.; Shigihara, Y.; Sugiyama, Y.; Yamashita, S.; Watanabe, Y. Imaging of gastrointestinal absorption and biodistribution of an orally administered probe using positron emission tomography in humans Clin. Pharmacol. Ther. 2012, 91 (4) 653-9
12. Yamashita, S.; Takashima, T.; Kataoka, M.; Oh, H.; Sakuma, S.; Takahashi, M.; Suzuki, N.; Hayashinaka, E.; Wada, Y.; Cui, Y.; Watanabe, Y. PET imaging of the gastrointestinal absorption of orally administered drugs in conscious and anesthetized rats J. Nucl. Med. 2011, 52 (2) 249-56
13. Kataoka, M.; Takashima, T.; Shingaki, T.; Hashizume, Y.; Katayama, Y.; Wada, Y.; Oh, H.; Masaoka, Y.; Sakuma, S.; Sugiyama, Y.; Yamashita, S.; Watanabe, Y. Dynamic Analysis of GI Absorption and Hepatic Distribution Processes of Telmisartan in Rats Using Positron Emission Tomography Pharm. Res. 2012, 29, 2419-31
14. Wagner, C. C.; Langer, O. Approaches using molecular imaging technology-use of PET in clinical microdose studies Adv. Drug Delivery Rev. 2011, 63 (7) 539-46
15. Bergstrom, M.; Grahnen, A.; Langstrom, B. Positron emission tomography microdosing: a new concept with application in tracer and early clinical drug development Eur. J. Clin. Pharmacol. 2003, 59 (5-6) 357-66
16. Fischman, A. J.; Alpert, N. M.; Rubin, R. H. Pharmacokinetic imaging: a noninvasive method for determining drug distribution and action Clin. Pharmacokinet. 2002, 41 (8) 581-602
17. Wolf, W. Imaging can be much more than pretty pictures Pharm. Res. 1995, 12 (12) 1821-2
18. Akai, S.; Ishida, S.; Hatanaka, K.; Ishii, T.; Harada, N.; Tsukada, H.; Oku, N. Synthesis of long-chain [(18)F]Deoxyfluoropoly(ethylene glycol) methyl ethers and their noninvasive pharmacokinetic analysis by positron emission tomography Mol. Pharmaceutics 2011, 8 (1) 302-8
19. Yamaoka, K.; Tanigawara, Y.; Nakagawa, T.; Uno, T. A pharmacokinetic analysis program (multi) for microcomputer J. Pharmacobiodyn. 1981, 4 (11) 879-85
20. Lennernas, H.; Regardh, C. G. Regional gastrointestinal absorption of the beta-blocker pafenolol in the rat and intestinal transit rate determined by movement of 14C-polyethylene glycol (PEG) 4000 Pharm. Res. 1993, 10 (1) 130-5
21. Yu, L. X.; Amidon, G. L. A compartmental absorption and transit model for estimating oral drug absorption Int. J. Pharmaceutics 1999, 186 (2) 119-25
22. Yu, L. X.; Lipka, E.; Crison, J. R.; Amidon, G. L. Transport approaches to the biopharmaceutical design of oral drug delivery systems: prediction of intestinal absorption Adv. Drug Delivery Rev. 1996, 19 (3) 359-76
23. McConnell, E. L.; Basit, A. W.; Murdan, S. Measurements of rat and mouse gastrointestinal pH, fluid and lymphoid tissue, and implications for in-vivo experiments J. Pharm. Pharmacol. 2008, 60 (1) 63-70
24. Roma, M. G.; Marinelli, R. A.; Rodriguez Garay, E. A. Biliary excretion of polyethylene glycol molecular weight 900. Evidence for a bile salt-stimulated vesicular transport mechanism Biochem. Pharmacol. 1991, 42 (9) 1775-81
25. Abuchowski, A.; Kazo, G. M.; Verhoest, C. R., Jr.; Van Es, T.; Kafkewitz, D.; Nucci, M. L.; Viau, A. T.; Davis, F. F. Cancer therapy with chemically modified enzymes. I. Antitumor properties of polyethylene glycol-asparaginase conjugates Cancer Biochem. Biophys. 1984, 7 (2) 175-86
26. Gragoudas, E. S.; Adamis, A. P.; Cunningham, E. T., Jr.; Feinsod, M.; Guyer, D. R. Pegaptanib for neovascular age-related macular degeneration N. Engl. J. Med. 2004, 351 (27) 2805-16
27. Ng, E. W.; Shima, D. T.; Calias, P.; Cunningham, E. T., Jr.; Guyer, D. R.; Adamis, A. P. Pegaptanib, a targeted anti-VEGF aptamer for ocular vascular disease Nat. Rev. Drug Discovery 2006, 5 (2) 123-32
28. Zhao, H.; Lee, C.; Sai, P.; Choe, Y. H.; Boro, M.; Pendri, A.; Guan, S.; Greenwald, R. B. 20-O-acylcamptothecin derivatives: evidence for lactone stabilization J. Org. Chem. 2000, 65 (15) 4601-6
29. Greenwald, R. B.; Gilbert, C. W.; Pendri, A.; Conover, C. D.; Xia, J.; Martinez, A. Drug delivery systems: water soluble taxol 2′-poly(ethylene glycol) ester prodrugs-design and in vivo effectiveness J. Med. Chem. 1996, 39 (2) 424-31