The relationship between drug input and mean residence time in the body

Meir Bialer; Zee M. Look; B. Michael Silber; Avraham Yacobi

doi:10.1002/bdd.2510070607

The relationship between drug input and mean residence time in the body

Meir Bialer^*, Zee M. Look, B. Michael Silber, Avraham Yacobi

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

8 Scopus citations

Abstract

The relationship between the mean residence time after oral dosing or any other non‐instantaneous mode of administration (MRT_ni) was explored by a series of computer simultations. MRT_ni was calculated from the ratio of AUMC to AUC (where AUC and AUMC are the zeroth and first statistical moments, respectively, of the drug concentration‐time curve). A continuous linear relationship between MRT_ni and 1/k_a or 1/k_O was observed. In the ‘flip‐flop’ case where k_a < K (where K is the elimination rate constant), the extrapolation from t* to infinity (where t* is the last observed plasma concentration) should be done using k_a instead of K. If K is used, underestimated values of MRT_ni will be obtained. The findings from this investigation have practical application in the design and pharmacokinetic evaluation of novel sustained‐release dosage forms.

Original language	English
Pages (from-to)	577-583
Number of pages	7
Journal	Biopharmaceutics and Drug Disposition
Volume	7
Issue number	6
DOIs	https://doi.org/10.1002/bdd.2510070607
State	Published - 1986
Externally published	Yes

Keywords

Absorption kinetics
Drug input–first and zero order absorption
Mean residence time
Oral administration

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title = "The relationship between drug input and mean residence time in the body",

abstract = "The relationship between the mean residence time after oral dosing or any other non‐instantaneous mode of administration (MRTni) was explored by a series of computer simultations. MRTni was calculated from the ratio of AUMC to AUC (where AUC and AUMC are the zeroth and first statistical moments, respectively, of the drug concentration‐time curve). A continuous linear relationship between MRTni and 1/ka or 1/kO was observed. In the {\textquoteleft}flip‐flop{\textquoteright} case where ka < K (where K is the elimination rate constant), the extrapolation from t* to infinity (where t* is the last observed plasma concentration) should be done using ka instead of K. If K is used, underestimated values of MRTni will be obtained. The findings from this investigation have practical application in the design and pharmacokinetic evaluation of novel sustained‐release dosage forms.",

keywords = "Absorption kinetics, Drug input–first and zero order absorption, Mean residence time, Oral administration",

author = "Meir Bialer and Look, {Zee M.} and Silber, {B. Michael} and Avraham Yacobi",

year = "1986",

doi = "10.1002/bdd.2510070607",

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T1 - The relationship between drug input and mean residence time in the body

AU - Bialer, Meir

AU - Look, Zee M.

AU - Silber, B. Michael

AU - Yacobi, Avraham

PY - 1986

Y1 - 1986

N2 - The relationship between the mean residence time after oral dosing or any other non‐instantaneous mode of administration (MRTni) was explored by a series of computer simultations. MRTni was calculated from the ratio of AUMC to AUC (where AUC and AUMC are the zeroth and first statistical moments, respectively, of the drug concentration‐time curve). A continuous linear relationship between MRTni and 1/ka or 1/kO was observed. In the ‘flip‐flop’ case where ka < K (where K is the elimination rate constant), the extrapolation from t* to infinity (where t* is the last observed plasma concentration) should be done using ka instead of K. If K is used, underestimated values of MRTni will be obtained. The findings from this investigation have practical application in the design and pharmacokinetic evaluation of novel sustained‐release dosage forms.

AB - The relationship between the mean residence time after oral dosing or any other non‐instantaneous mode of administration (MRTni) was explored by a series of computer simultations. MRTni was calculated from the ratio of AUMC to AUC (where AUC and AUMC are the zeroth and first statistical moments, respectively, of the drug concentration‐time curve). A continuous linear relationship between MRTni and 1/ka or 1/kO was observed. In the ‘flip‐flop’ case where ka < K (where K is the elimination rate constant), the extrapolation from t* to infinity (where t* is the last observed plasma concentration) should be done using ka instead of K. If K is used, underestimated values of MRTni will be obtained. The findings from this investigation have practical application in the design and pharmacokinetic evaluation of novel sustained‐release dosage forms.

KW - Absorption kinetics

KW - Drug input–first and zero order absorption

KW - Mean residence time

KW - Oral administration

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The relationship between drug input and mean residence time in the body

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Keywords

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