Imaging of gastrointestinal absorption and biodistribution of an orally administered probe using positron emission tomography in humans

Clinical Pharmacology and Therapeutics

Volumn 91, Issue 4, 2012, Pages 653-659

  Shingaki, T ^a,b,c   Takashima, T ^a,b   Wada, Y ^a,b   Tanaka, M ^b   Kataoka, M ^d   Ishii, A ^b   Shigihara, Y ^b   Sugiyama, Y ^e   Yamashita, S ^d   Watanabe, Y ^a,b  

^a RIKEN   (Japan)

^b OSAKA CITY UNIVERSITY GRADUATE SCHOOL OF MEDICINE   (Japan)

^c ADME Research Inc   (Japan)

^d SETSUNAN UNIVERSITY   (Japan)

^e UNIVERSITY OF TOKYO   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

ATENOLOL; FLUORODEOXYGLUCOSE F 18; GELATIN; MACROGOL 400;

ADULT; ARTICLE; DRUG DISCRIMINATION; DRUG RELEASE; DRUG SAFETY; DRUG SOLUBILITY; DRUG STABILITY; GASTROINTESTINAL ABSORPTION; HUMAN; HUMAN EXPERIMENT; MALE; NORMAL HUMAN; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; SMALL INTESTINE; STOMACH EMPTYING;

ADMINISTRATION, ORAL; ADULT; ATENOLOL; FLUORODEOXYGLUCOSE F18; GASTRIC EMPTYING; GASTROINTESTINAL CONTENTS; HUMANS; INTESTINAL ABSORPTION; MALE; MOLECULAR PROBES; POSITRON-EMISSION TOMOGRAPHY; RADIOPHARMACEUTICALS; STOMACH; TISSUE DISTRIBUTION; YOUNG ADULT;

EID: 84862792340     PISSN: 00099236     EISSN: 15326535     Source Type: Journal    
DOI: 10.1038/clpt.2011.267     Document Type: Article

References (45)

1. Yuen, K.H. The transit of dosage forms through the small intestine. Int. J. Pharm. 395, 9-16 (2010).
2. Wilson, C.G. et al. Do gastrointestinal transit parameters influence the pharmacokinetics of gefitinib? Int. J. Pharm. 376, 7-12 (2009).
3. Yano, K., Masaoka, Y., Kataoka, M., Sakuma, S. & Yamashita, S. Mechanisms of membrane transport of poorly soluble drugs: role of micelles in oral absorption processes. J. Pharm. Sci. 99, 1336-1345 (2010).
4. Buch, P., Langguth, P., Kataoka, M. & Yamashita, S. IVIVC in oral absorption for fenofibrate immediate release tablets using a dissolution/permeation system. J. Pharm. Sci. 98, 2001-2009 (2009).
5. Takano, R. et al. Quantitative analysis of the effect of supersaturation on in vivo drug absorption. Mol. Pharm. 7, 1431-1440 (2010).
6. Kleberg, K., Jacobsen, J. & M?lertz, A. Characterising the behaviour of poorly water soluble drugs in the intestine: application of biorelevant media for solubility, dissolution and transport studies. J. Pharm. Pharmacol. 62, 1656-1668 (2010).
7. Kataoka, M., Masaoka, Y., Sakuma, S. & Yamashita, S. Effect of food intake on the oral absorption of poorly water-soluble drugs: in vitro assessment of drug dissolution and permeation assay system. J. Pharm. Sci. 95, 2051-2061 (2006). (Pubitemid 44433034)
8. Kataoka, M., Masaoka, Y., Yamazaki, Y., Sakane, T., Sezaki, H. & Yamashita, S. In vitro system to evaluate oral absorption of poorly water-soluble drugs: simultaneous analysis on dissolution and permeation of drugs. Pharm. Res. 20, 1674-1680 (2003). (Pubitemid 37268286)
9. 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 31, 161-165 (1994). (Pubitemid 24195219)
10. Azad Khan, A.K., Piris, J. & Truelove, S.C. An experiment to determine the active therapeutic moiety of sulphasalazine. Lancet 2, 892-895 (1977).
11. Murata, K., Noda, K., Kohno, K. & Samejima, M. Pharmacokinetic analysis of concentration data of drugs with irregular absorption profiles using multifraction absorption models. J. Pharm. Sci. 76, 109-113 (1987). (Pubitemid 17043675)
12. Lukacova, V., Woltosz, W.S. & Bolger, M.B. Prediction of modified release pharmacokinetics and pharmacodynamics from in vitro, immediate release, and intravenous data. AAPS J. 11, 323-334 (2009).
13. Parrott, N. & Lave, T. Applications of physiologically based absorption models in drug discovery and development. Mol. Pharm. 5, 760-775 (2008).
14. Bod? S., Dreyer, M. & Greisen, G. Gastric emptying and small intestinal transit time in preterm infants: a scintigraphic method. J. Pediatr. Gastroenterol. Nutr. 39, 378-382 (2004).
15. Kimura, T. & Higaki, K. Gastrointestinal transit and drug absorption. Biol. Pharm. Bull. 25, 149-164 (2002). (Pubitemid 39592096)
16. Schiller, C. et al. Intestinal fluid volumes and transit of dosage forms as assessed by magnetic resonance imaging. Aliment. Pharmacol. Ther. 22, 971-979 (2005). (Pubitemid 41634879)
17. Combes, R.D. et al. Early microdose drug studies in human volunteers can minimise animal testing: Proceedings of a workshop organised by Volunteers in Research and Testing. Eur. J. Pharm. Sci. 19, 1-11 (2003). (Pubitemid 36506932)
18. Yano, T. & Watanabe, Y. [Microdose clinical trial-impact of PET molecular imaging]. Gan To Kagaku Ryoho. 37, 1839-1848 (2010).
19. Yamashita, S. et al. PET imaging of the gastrointestinal absorption of orally administered drugs in conscious and anesthetized rats. J. Nucl. Med. 52, 249-256 (2011).
20. Wakita, K. et al. Simplification for measuring input function of FDG PET: investigation of 1-point blood sampling method. J. Nucl. Med. 41, 1484-1490 (2000).
21. Takashima, T. et al. Positron emission tomography studies using (15R)-16-m-[11C]tolyl-17,18,19,20-tetranorisocarbacyclin methyl ester for the evaluation of hepatobiliary transport. J. Pharmacol. Exp. Ther. 335, 314-323 (2010).
22. Choi, S.R. et al. Preclinical properties of 18F-AV-45: a PET agent for Abeta plaques in the brain. J. Nucl. Med. 50, 1887-1894 (2009).
23. Stabin, M.G., Sparks, R.B. & Crowe, E. OLINDA/EXM: the second-generation personal computer software for internal dose assessment in nuclear medicine. J. Nucl. Med. 46, 1023-1027 (2005). (Pubitemid 43733519)
24. International Commission on Radiation Protection. ICRP Publication 60: Recommendations of the International Commission on Radiological Protection (1991).
25. Maschauer, S., Prante, O., Hoffmann, M., Deichen, J.T. & Kuwert, T. Characterization of 18F-FDG uptake in human endothelial cells in vitro. J. Nucl. Med. 45, 455-460 (2004). (Pubitemid 47618621)
26. Yamaoka, K., Tanigawara, Y., Nakagawa, T. & Uno, T. A pharmacokinetic analysis program (multi) for microcomputer. J. Pharmacobiodyn. 4, 879-885 (1981). (Pubitemid 12174128)
27. The European Agency for the Evaluation of Medicinal Products. Evaluation of Medicines for Human Use. Position Paper On Non-Clinical Safety Studies to Support Clinical Trials With a Single Microdose (2003).
28. US Food and Drug Administration. Center for Drug Evaluation and Research. Guidance for Industry, Investigators and Reviewers, Exploratory IND Studies (2006).
29. Ministry of Health, Labour and Welfare, Pharmaceutical and Food Safety Bureau: Guidance for Microdose Clinical Studies (2008).
30. International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use. ICH harmonized tripartite guideline: Guidance on nonclinical safety studies for the conduct of human clinical trials and marketing authorization for pharmaceuticals M3(R2). Current Step 4 version (2009).
31. Yamane, N., Takami, T., Tozuka, Z., Sugiyama, Y., Yamazaki, A. & Kumagai, Y. Microdose clinical trial: quantitative determination of nicardipine and prediction of metabolites in human plasma. Drug Metab. Pharmacokinet. 24, 389-403 (2009).
32. Sugiyma, Y. et al. Impact of microdosing clinical study-Why necessary and how useful? Adv. Drug Deliv. Rev. 63, 494-502 (2011).
33. Ferl, G.Z., Zhang, X., Wu, H.M., Kreissl, M.C. & Huang, S.C. Estimation of the 18F-FDG input function in mice by use of dynamic small-animal PET and minimal blood sample data. J. Nucl. Med. 48, 2037-2045 (2007). (Pubitemid 350232315)
34. Roh, J.L. et al. Use of 18F-fluorodeoxyglucose positron emission tomography in patients with rare head and neck cancers. Clin. Exp. Otorhinolaryngol. 1, 103-109 (2008).
35. International Commission on Radiation Protection. ICRP Publication 103: Recommendations of the International Commission on Radiological Protection. (2008).
36. International Commission on Radiation Protection. ICRP Publication 49: Recommendations of the International Commission on Radiological Protection. (1986).
37. Silverman, M. Glucose transport in the kidney. Biochim. Biophys. Acta 457, 303-351 (1976).
38. Kleinzeller, A., McAvoy, E.M. & McKibbin, R.D. Active renal hexose transport. Structural requirements. Biochim. Biophys. Acta 600, 513-529 (1980). (Pubitemid 10023561)
39. 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 Deliv. Rev. 19, 359-376 (1996). (Pubitemid 26227526)
40. Sutton, S.C. Role of physiological intestinal water in oral absorption. AAPS J. 11, 277-285 (2009).
41. Yu, L.X. An integrated model for determining causes of poor oral drug absorption. Pharm. Res. 16, 1883-1887 (1999). (Pubitemid 30040706)
42. L?enberg, R. & Amidon, G.L. Modern bioavailability, bioequivalence and biopharmaceutics classification system. New scientific approaches to international regulatory standards. Eur. J. Pharm. Biopharm. 50, 3-12 (2000). (Pubitemid 30326685)
43. Dressman, J.B. & Reppas, C. In vitro-in vivo correlations for lipophilic, poorly water-soluble drugs. Eur. J. Pharm. Sci. 11 (suppl. 2), S73-S80 (2000).
44. Hamacher, K., Coenen, H.H. & St?klin, G. Efficient stereospecific synthesis of no-carrier-added 2-[18F]-fluoro-2-deoxy-D-glucose using aminopolyether supported nucleophilic substitution. J. Nucl. Med. 27, 235-238 (1986). (Pubitemid 17024868)
45. Takashima, T. et al. The involvement of organic anion transporting polypeptide in the hepatic uptake of telmisartan in rats: PET studies with [(11) C]telmisartan. Mol. Pharm. 8, 1789-1798 (2011).