Compartment- and model-independent linear plateau principle of drugs during a constant-rate absorption or intravenous infusion
Tóm tắt
A simple general equation is derived to show the linear plateau principle under various conditions during or after a constant or changing rate of absorption or intravenous infusion. The time required to cause a certain fraction (ft) of the total shift or change between the two steady-state plasma concentrations is equal to the time required for the cumulative (from time zero) plasma area, AUC0→t, to reach the same fraction of AUC0→∞ assumed to be obtained after an instantaneousintravenous dosing. The role of the terminal biological half-life and the importance of the earlydistribution phase and its exponential half-life or lives in the plateau principle are discussed.Clinical implications and applications to multiple dosage regimens are also discussed.
Tài liệu tham khảo
A. Goldstein, L. Aronow, and S. M. Kaiman.Principles of Drug Actions: The Basis of Pharmacology, Harper & Row, New York, 1969, pp. 292–317.
A. Goldstein, L. Aronow, and S. M. Kaiman.Principles of Drug Action: The Basis of Pharmacology, 2nd ed., Wiley, 1974, pp. 311–332.
M. Gibaldi and D. Perrier.Pharmacokinetics, Dekker, New York, 1975, p. 71.
J. G. Wagner.Fundamentals of Clinical Pharmacokinetics, Drug Intelligence Publications, Hamilton Press, Hamilton, Ill., 1976, p. 91.
R. E. Notari.Biopharmaceutics and Pharmacokinetics, An Introduction, 2nd ed., Dekker, New York, 1976.
S. Riegelman, J. C. K. Loo, and M. Rowland. Shortcomings in pharmacokinetic analysis by conceiving the body to exhibit properties of a single compartment.J. Pharm. Sci. 57:117–122 (1968).
J. G. Wagner. Model-independent linear pharmacokinetics.Drug Intell. Clin. Pharm. 10:179–180 (1976).
W. L. Chiou. A simple equation to estimate the percent of drug remaining in the body after an intravenous injection.J. Pharm. Pharmacol. 24:343–344 (1972).
J. G. Wagner. Linear pharmacokinetic equations allowing direct calculation of many needed pharmacokinetic parameters from the coefficients and exponents of polyexponential equations which have been fitted to the data.J. Pharmacokin. Biopharm. 4:443–467 (1976).
D. D. Breimer, C. Honhoff, W. Zilly, E. Richter, and J. M.van Rossum. Pharmacokinetics of hexobarbital in man after intravenous infusion.J. Pharmacokin. Biopharm. 3:1–11 (1975).
J. M. van Rossum. Significance of pharmacokinetics for drug design and the planning of dosage regimens, In E. J. Ariens (ed.),Drug Design, Vol. 1, Academic Press, New York, 1971, pp. 469–521.
W. L. Chiou. Rapid compartment-and model-independent estimation of times required to attain various fractions of steady-state plasma level during multiple dosing of drugs obeying superposition principle and having various absorption or infusion kinetics.J. Pharm. Sci. 68:1546–1547 (1979).
W. L. Chiou. New compartment-and model-independent method for the rapid calculation of the absorption rate of drugs. Presented to the APhA Academy of Sciences Meeting, Kansas City, M. November 10–15, 1979.
W. L. Chiou. New compartment-and model-independent method for the rapid calculation of the absorption rate of drugs.J. Pharm. Sci. 69:57–62 (1980).
J. C. K. Loo and S. Riegelman. Assessment of pharmacokinetic constants from post-infusion blood curves obtained after i.v. infusion.J. Pharm. Sci. 59:53–55 (1970).
C. Graffner, G. Johnson, and J. Sjögren. Pharmacokinetics of procainamide intravenously and orally as conventional and slow-release tablets.Clin. Pharmacol. Ther. 17:414–423 (1975).
T. N. Calvey, N. E. Williams, K. T. Muir, and H. E. Barber. Plasma concentration of edrophonium in man.Clin. Pharmacol. Ther. 19:813–820 (1976).
S. Niazi and W. L. Chiou. Fluorocarbon aerosol propellants. X. Pharmacokinetics of dichlorotetrafluoroethane in dogs following single and multiple dosing.J. Pharm. Sci. 65:60–64 (1976).
J. M. van Rossum and A. H. J. M. Tomey, Multicompartment-kinetics and the accumulation plateau.Arch. Int. Pharmacodyn. 188:200–203 (1970).
L. Z. Benet. Pharmacokinetics/pharmacodynamics of furosemide in man.J. Pharmacokin. Biopharm. 7:1–27 (1979).
W. L. Chiou, S. M. Huang, and Y. C. Huang. Midpoint backextrapolation method for the rapid estimation of volume of distribution and dosage adjustments of drugs exhibiting multicompartmental characteristics.Int. J. Clin. Pharmacol, Ther. Toxicol. 18:1–4 (1980).
M. Gibaldi, G. Levy and H. Weintraub. Drug distribution and pharmacologic effects.Clin. Pharmacol. Ther. 12:734–742 (1971).
G. Levy. Pharmacokinetic control and clinical interpretation of steady-state blood levels of drugs.Clin. Pharmacol. Ther. 16:130–134 (1974).
W. L. Chiou. Critical evaluation of the potential error in pharmacokinetic studies of using the linear trapezoidal rule method for the calculation of the area under the plasma level-time curve.J. Pharmacokin. Biopharm. 6:539–546 (1978).