Based on the convolution integral, equations have been derived for the ratio of the first to the zeroth moments of the plasma concentration-time curve (AUMC/AUC) parameters for a drug (p) undergoing first-pass and reversible metabolism and its reversible metabolite (m). According to these equations,
A method for calculating the mean absorption time of drugs undergoing reversible and first-pass metabolism
โ Scribed by Haiyung Cheng; Linyee Shum
- Publisher
- John Wiley and Sons
- Year
- 1993
- Tongue
- English
- Weight
- 412 KB
- Volume
- 14
- Category
- Article
- ISSN
- 0142-2782
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โฆ Synopsis
A method has been derived for calculating the mean absorption time of an oral drug and its interconversion metabolite which is generated from the drug systemically and presystemically. The method evolves from the convolution integral and requires plasma AUC and AUMC values after separate intravenous administration of the drug and its interconversion metabolite and oral administration of the drug. It can also be used to calculate the mean input time of a drug undergoing reversible metabolism and administered by any other extravascular route. Results of a simulation study using both errorless and errant data indicate that, when the absorption rate constant of a drug or its interconversion metabolite is not much larger than the apparent elimination rate constant, the proposed method performs satisfactorily. However, when the absorption rate constant of a drug or its interconversion metabolite is much larger than the apparent elimination rate constant, the proposed method appears to be inaccurate.
๐ SIMILAR VOLUMES
Based on disposition decomposition analysis (DDA), equations for the mean residence times (MRT) in the body are derived for a drug and its interconversion metabolite that undergo linear tissue distribution and linear or non-linear elimination from the central compartment after non-instantaneous admi
A general method for calculating the mean transit times and distribution rate parameters is described. The calculations require the AUC, AUMC, and derivatives of the plasma concentration profiles of the metabolites and its precursor. The method is applicable to catenary metabolites with any precurso