Prediction of the human pharmacokinetics of troglitazone, a new and extensively metabolized antidiabetic agent, after oral administration, with an animal scale-up approach

Journal of Pharmacology and Experimental Therapeutics

Volumn 277, Issue 3, 1996, Pages 1630-1641

  Izumi, Takashi ^a   Enomoto, Sachiko ^a   Hosiyama, Kazuko ^a   Sasahara, Kunihiro ^a   Shibukawa, Akimasa ^b   Nakagawa, Terumichi ^b   Sugiyama, Yuichi ^c  

^a DAIICHI SANKYO CO   (Japan)

^b KYOTO UNIVERSITY   (Japan)

^c UNIVERSITY OF TOKYO   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIDIABETIC AGENT; GLUCURONIDE; PENTOBARBITAL; SULFATE; TROGLITAZONE;

ALLOMETRY; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BODY WEIGHT; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DOG; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG METABOLISM; HUMAN; HUMAN EXPERIMENT; INTRAPERITONEAL DRUG ADMINISTRATION; INTRAVENOUS DRUG ADMINISTRATION; MALE; MONKEY; MOUSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; NORMAL HUMAN; ORAL DRUG ADMINISTRATION; PHASE 1 CLINICAL TRIAL; PREDICTION; PRIORITY JOURNAL; RAT;

ADMINISTRATION, ORAL; ANIMALS; CHROMANS; DOGS; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; HYPOGLYCEMIC AGENTS; MACACA; MALE; MICE; MICE, INBRED STRAINS; RATS; RATS, WISTAR; THIAZOLES; THIAZOLIDINEDIONES;

EID: 0030438721     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (44)

1. BENOWITZ, N., FORSYTH, R. P., MELMON, K. L. AND ROWLAND, M.: Lidocain disposition kinetics in monkey and man I. Prediction by a perfusion model. Clin. Pharmacol. Ther., 16: 87-98, 1974.
2. BHARGAVA, H. N., VILLAR, V. M., GULATI, A. AND CHARI, G.: Analgesic and hyperthermic effects of intravenously administrated morphine in the rat are related to its serum levels. J. Pharmacol. Exp. Ther. 258: 511-516, 1991.
3. BOXENBAUM, H.: Interspecies variation in liver weight, hepatic blood flow, and antipyrine intrinsic clearance: extrapolation of data to bezodiazepines and phenytoin. J. Pharmacokinet. Biopharm. 8: 165-176, 1980.
4. BOXENBAUM, H.: Interspecies scaling, allometry, physiological time, and the ground plan of pharmacokinetics. J. Phannacokinet. Biopharm. 10: 201-227, 1982a.
5. BOXENBAUM, H.: Comparative pharmacokinetics of benzodiazepines in dog and man. J. Pharmacokinet. Biopharm. 10: 411-426, 1982b.
6. BOXENBAUM, H. AND RONFELD, R.: Interspecies pharmacokinetic scaling and the Dedrick plots. Am. J. Physiol. 245: R768-R774, 1983.
7. BOXENBAUM, H. AND FERTIG, J. B.: Scaling of antipyrine intrinsic clearance of unbound drug in 15 mammalian species. Eur. J. Drug Metab. Pharmacokinet. 9: 177-183, 1984.
8. BREWSTER, D., HUMPHREY, M. J. AND MCLEAVY, M. A.: Biliary excretion, metabolism and enterohepatic circulation of buprenorphine. Xenobiotica 11: 189-196, 1981.
9. DAVIES, B. AND MORRIS, T.: Physiological parameters in laboratory animals and humans. Pharm. Res. 10: 1093-1095, 1993.
10. DEDRICK, R. L., BISCHOFF, K. B. AND ZAHRKO, D. S.: Interspecies correlation of plasma concentration history of methotrexate. Cancer Chemother. Rep. Part 1 54: 95-101, 1970.
11. DEDRICK, R. L.: Animal scale-up. J. Pharmacokinet. Biopharm. 1: 435-461, 1973.
12. EL-SAYED, Y. M. AND HASAN, M. M.: Enhancement of morphine clearance following intravenous administration by oral activated charcoal in rabbits. J. Pharm. Pharmacol. 42: 538-541, 1989.
13. FUJIWARA, T., YOSHIOKA, A., TOSHIOKA, T., USHIYAMA, I. AND HORIKOSHI, H.: Characterization of new antidiabetic agent CS-045. Studies in KK and ob/ob mice and Zucker fatty rats. Diabetes 37: 1549-1558, 1988.
14. GÁRDMARK, M., EKBLOM, M., BOUW, R. AND HAMMARLUND-UDENAES, M.: Quantification of effect deley and acute tolerance development to morphine in the rat. J. Pharmacol. Exp. Ther. 267: 1061-1067, 1993.
15. GARRETT, E. R. AND CHANDRAN, V. R.: Pharmacokinetice of morphine and its surogates X: Analyses and pharmacokinetics of buprenorphine in dogs. Biopharm. Drug Dispos. 11: 311-350, 1990.
16. GILLETTE, J. R. AND PANG, K. S.: Theoretic aspects of pharmacokinetic drug interaction. Clin. Pharmacol. Ther. 22: 623-639, 1977.
17. GREENS, D. S., QUINTILIANI, R. AND NIGHTINGALE, C. H.: Physiological perfusion model for cephalosporin antibiotics 1: model selection based on blood drugconcentration. J. Pharm. Sci. 67: 191-196, 1978.
18. HASSELSTROM, J. AND SAWE, J.: Morphine pharmacokinetics and metabolism in humans. Clin. Pharmacokinet. 24: 344-354, 1993.
19. HO, S.-T., WANG, J.-J. AND HO, W.: Determination of buprenorphine by high-performance liquid chromatography with fluorescence detection: Application to human and rabbit pharmacokinetic studies. J. Chromatogr. 570: 339-350, 1991.
20. HOUSTON, J. B.: Utility of in vitro drug metabolism data in predicting in vivo metabolic clearance. Biochem. Pharmacol. 47: 1469-1479, 1994.
21. IWATSBO, T., SUZUKI, H. AND SUGIYAMA, Y.: Prediction of in vivo drug disposition from in vitro data based on physiological pharmacokinetics (review). Biopharm. Drug Dispos., in press, 1996.
22. JACQZ, E., WARD, S., JOHNSON, R., SCHENKER, S., GERKENS, J. AND BRANCH, R. A.: Extrahepatic glucuronidation of morphine in the dog. Drug Metab. Dispos. 14: 627-630, 1986.
23. MCNAMARA, P. J.: Interspecies scaling in pharmacokinetics. In Pharmaceutical Bioequivalence, ed. by P. G. Welling, F. L. S. Tse and S. V. Digne, Marcel Dekker, Inc., New York, 1991.
24. MIYAMOTO, Y., OZAKI, M. AND YAMAMOTO, H.: Effects of adrenalectomy on pharmacokinetics and antinociceptive activity of morphine in rats. Jpn. J. Pharmacol. 45: 379-386, 1988.
25. OHTANI, M., KOTAKI, H., UCHINO, L., SAWADA, Y. AND IGA, T.: Pharmacokinetic analysis of enterohepatic circulation of buprenorphine and its active metabolite, norbuprenorphine, in rats. Drug Metab. Dispos. 22: 2-7, 1994.
26. Øie, S. and Tozer, T. N.: Effect of altered plasma protein binding on apparent volume of distribution. J. Pharm. Sci. 68: 1203-1205, 1979.
27. PROTHERO, J. W.: Scaling of blood parameters in mammals. Comp. Biochem. Physiol. 67A: 649, 1980.
28. RANE, A., WILKINSON, G. W. AND SHAND, D. G.: Prediction of hepatic extraction ratio from in vitro measurement of intrinsic clearance. J. Pharmacol. Exp. Ther. 200: 420-424, 1977.
29. ROBERTS, S. M. AND ROWLAND, M.: Correlation between in-vitro microsomal enzyme activity and whole organ hepatic elimination kinetics: analysis with a dispersion model. J. Pharm. Pharmacol. 38; 177-181, 1985.
30. SANGALLI, L., BORTOLOTTI, A., JIRITANO, L. AND BONATI, M.: Cyclosporine pharmacokinetics in rats and interspecies comparision in dogs, rabbits, rate and humans. Drug Metab. Dispos. 16: 749-753, 1988.
31. SAWADA, Y., HANANO, M., SUGIYAMA, Y. AND IGA, T.: Prediction of the distribution of β-lactam antibiotics in human from pharmacokinetic parameters in animals. J. Pharmacokinet. Biopharm. 12: 241-264, 1984a.
32. SAWADA, Y., HANANO, M., SUGIYAMA, Y., HARASHIMA, H. AND IGA, T.: Prediction of the volumes of distribution of basic drugs in humans based on data from animals. J. Pharmacokinet. Biopharm. 12: 587-596, 1984b.
33. SAWADA, Y., HANANO, M., SUGIYAMA, Y. AND IGA, T.: Prediction of the volumes of distribution of nine weakly acidic and six weakly basic drugs in humans from pharmacokinetic parameters in rats. J. Pharmacokinet. Biopharm. 13: 477-492, 1985.
34. SHIBATA, H., ARAI, S., KOBAYASHI, M., IZUMI, T., MAEDA, E., SASAHARA, K., YAMAGUCHI, K., MORITA, A. AND NISHIWAKI, A.: A phase I study of new hypoglycemic agent CS-045 in healthy volunteers: safety and pharmacokinetics in single administration. J. Clin. Ther. Med. 9: 1503-1518, 1993.
35. SHIBUKAWA, A., NAKAGAWA, T., NISHIMURA, N., MIYAKE, M. AND TANAKA, H: Determination of free drug in protein binding equilibrium by high-performance frontal analysis using internal-surface reversed phase support. Chem. Pharm. Bull. 37: 702-706, 1989.
36. SHIBUKAWA, A., NAKAO, C., SAWADA, T., MOROKOSHI, N. AND NAKAGAWA, T.: Determination of unbound concentration of hydrophobic drugs in albumin solution by high-performance frontal analysis using a diol-silica column. J. Pharm. Sci. 83: 868-876, 1994.
37. SHIBUKAWA, A., SAWADA, T., NAKAO, C., IZUMI, T. AND NAKAGAWA, T.: High-performance frontal analysis for the study of protein binding of troglitazone (CS-045) in albumin solution and human plasma. J. Chromatogr. A 697: 337-347, 1995.
38. SUOIYAMA, Y. AND IWATSBO, T.: Physiological pharmacokinetics: Prediction of human disposition and pharmacokinetics from animal data, and from in vitro to in vivo. In Proceedings of The International Symposium of The Role of Drug Metabolism and Pharmacokinetic Research in New Drug Development, pp. 45-63, Doping Control Center, Korea Institute of Science and Technology (KIST), Korea, 1994.
39. SUQIYAMA, Y., SAWADA, Y., IGA, T. AND HANANO, M.: Reconstruction of in vivo metabolism from in vitro data. In Xenobiotic Metabolism and Disposition. Proceedings of the Second International Meeting of International Society for the Study of Xenobiotics, ed. by R. Kato, R. W. Estabrook and M. N. Cayen, pp. 225-235, Taylor & Francis, London, 1989.
40. SUTER, S. I., NOLAN, J. J., WALLACE, P., GUMBINER, B. AND OLEPSKY, J. M.: Metabolic effects of new oral hypoglycemic agent CS-045 in NIDDM subjects. Diabetes Care 14: 1083-1086, 1992.
41. TOON, S. AND ROWLAND, M.: Structure-pharmacokinetics relationships among the barbiturates in the rat. J. Pharmacol. Exp. Ther. 225: 752, 1983.
42. WILKINSON, G. R.: Clearance approaches in pharmacology. Pharmacol. Rev. 39: 1-47, 1987.
43. YAMAOKA, K., TANIGAWARA, Y., NAKAGAWA, T. AND UNO, T.: A pharmacokinetic analysis program (MULTI) for microcomputer. J. Pharm. Dyn. 4: 879-885, 1981.
44. YOSHIOKA, T., FUJITA, T., AIZAWA, T., KURUWADA, T. AND HASEGAWA, K.: Studies on hindered phenols and analogues. 1. Hypolipidemic and hypoglycemic agenys with ability to inhibit lipid peroxidation. J. Med. Chem. 32: 421-428, 1989.