A valid equation for the well-stirred perfusion limited physiologically based pharmacokinetic model that consistently accounts for the blood-tissue drug distribution in the organ and the corresponding valid equation for the steady state volume of distribution

Journal of Pharmaceutical Sciences

Volumn 99, Issue 1, 2010, Pages 475-485

  Berezhkovskiy, Leonid M ^a  

^a GENENTECH INC   (United States)

Author keywords

Blood plasma concentration ratio; Clearance; Perfusion limited model; Perfusion volume; Physiologically based pharmacokinetic model; Steady state volume of distribution; Tissue plasma partition coefficient; Well stirred model

Indexed keywords

ARTICLE; COMPARTMENT MODEL; DISTRIBUTION VOLUME; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG TISSUE LEVEL; HALF LIFE TIME; HUMAN; MATHEMATICAL MODEL;

EID: 73949125673     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.21798     Document Type: Article

References (30)

1. Teorell T. 1937. Kinetics of distribution of substances administered to the body. Arch Intern Pharmacodyn Ther 57:205-240.
2. Bellman R, Jacquez JA, Kalaba R. 1960. Some mathematical aspects of chemotherapy. I. One-organ models. Bull Math Biol 22:181-198.
3. Bischoff KB, Brown RG. 1966. Drug distribution in mammals. Chem Eng Prog Symp Ser 62:32-45.
4. Bischoff KB, Dedrick RL, Zaharko DS. 1970. Preliminary model for methotrexate pharmacokinetics. Pharm Sci 59:149-154.
5. Rowland M, Benet LZ, Graham GG. 1973. Clearance concepts in pharmacokinetics. J Pharmacokinet Biopharm 1:123-136.
6. Yang RSH, Andersen ME, Dennison JE, Ou YC, Liao KH, Reisfeld B. 2004. Mouse models of cancer. In: Holland EC, editor. Physiologically based pharmacokinetic and pharmacodynamic modeling. New York: Wiley. pp. 391-405.
7. Wagner JG. 1993. Pharmacokinetics for the pharmaceutical scientist. Lancaster: Technomic Publishing Company.
8. Welling PG. 1997. Pharmacokinetics: Processes, mathematics, and applications. Washington, DC: ACS.
9. Reddy MB, Yang RSH, Andersen ME, Clewell HJ III. 2005. Physiologically based pharmacokinetic modeling: Science and applications. Hoboken: Wiley & Sons Inc.
10. Wilkinson GR, Shand DG. 1975. A physiological approach to hepatic drug clearance. Clin Pharmacol Ther 18:377-390.
11. Pang KS, Rowland M. 1977. Hepatic clearance of drugs. I. Theoretical considerations of a "well stirred" model and a "parallel tube" model. Influence of hepatic blood flow, plasma and blood cell binding, and the hepatocellular enzymatic activity on hepatic drug clearance. J Pharmacokinet Biopharm 5:625-653.
12. Yang J, Jamei M, Yeo KR, Rostami-Hodjegan A, Tucker GT. 2007. Misuse of the well-stirred model of hepatic drug clearance. Drug Metab Dispos 35: 501-502.
13. Berezhkovskiy LM. 2004. Volume of distribution at steady state for a linear pharmacokinetic system with peripheral elimination. J Pharm Sci 93:1628-1640.
14. Gerlowski LE, Jain RK. 1983. Physiologically based pharmacokinetic modeling: principles and applications. J Pharm Sci 72:1103-1127.
15. Simcyp Population-based ADME Simulator User Manual, Version 8. 2008. Edited by Turner D. 232 pages including appendices and references.
16. Kwon Y. 2000. Handbook of essential pharmacokinetics, pharmacodynamics and drug metabolism for industrial scientists. New York: Kluwer Academic/Plenum Publishers.
17. Schwab AJ, Barker F III, Goresky CA, Pang KS. 1990. Transfer of enalaprilat across rat liver cell membranes is barrier limited. Am J Physiol 258: G461-G475.
18. Fagerholm U. 2007. Prediction of human pharmacokinetics- evaluation of methods for prediction of hepatic metabolic clearance. J Pharm Pharmacol 59:803-828.
19. Rodgers T, Rowland M. 2006. Physiologically based pharmacokinetic modelling 2: predicting the tissue distribution of acids, very weak bases, neutrals and zwitterions. J Pharm Sci 95:1238-1257.
20. Hinderling PH. 1997. Red blood cells: A neglected compartment in pharmacokinetics and pharmacodynamics. Pharmacol Rev 49:279-295.
21. Berezhkovskiy LM. 2007. On the determination of the time delay in reaching the steady state drug concentration in the organ compared to plasma. J Pharm Sci 96:3432-3443.
22. Hinderling PH. 1988. Drug distribution in the body: in vitro prediction and physiological interpretation. Prog Pharmacol 6:1-30.
23. Beysens AJ, Wijnen RM, Beuman GH, van der Heyden J, Kootstra G, van As H. 1991. FK 506: monitoring in plasma or in whole blood? Transplant Proc 23:2745-2747.
24. Fleuren HL, van Rossum JM. 1977. Nonlinear relationship between plasma and red blood cellpharmacokinetics of chlorthalidone in man. J Pharmacokinet Biopharm 5:359-375.
25. Tett SE, Cutler DJ, Day RO, Brown KF. 1988. A dose-ranging study of the pharmacokinetics of hydroxychloroquine following intravenous administration to healthy volunteers. Br J Clin Pharmacol 26:303-313.
26. MacDonald A, Scarola J, Burke JT, Zimmerman JJ. 2000. Clinical pharmacokinetics and therapeutic drug monitoring of sirolimus. Clin Ther.2000; 22(Suppl B):B101-B121.
27. Brattström C, Säwe J, Jansson B, Lönnebo A, Nordin J, Zimmerman JJ, Burke JT, Groth CG. 2000. Pharmacokinetics and safety of single oral doses of sirolimus (rapamycin) in healthy male volunteers. Ther Drug Monit 22:537-544.
28. Gilman AG, Rall TW, Nies As, Taylor P, editors. 1990. Goodman and Gilman's the pharmacological basis of therapeutics. 8th edition. New York: Pergamon Press.
29. Kuypers DR, Vanrenterghem Y. 2004. Time to reach tacrolimus maximum blood concentration, mean residence time, and acute renal allograft rejection: an open-label, prospective, pharmacokinetic study in adult recipients. Clin Ther 26:1834-1844.
30. Carmichael SJ, Charles B, Tett SE. 2003. Population pharmacokinetics of hydroxychloroquine in patients with rheumatoid arthritis. Ther Drug Monit 25:671-681.