Analysis of enterohepatic circulation of cefixime in rat by fast inverse Laplace transform (FILT)

Yamaoka, Kiyoshi; Kanba, M.; Toyoda, Yoko; Yano, Yoshitaka; Nakagawa, Terumichi

doi:10.1007/bf01073938

Cited by 19 publications

(16 citation statements)

References 20 publications

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“…We can apply the recirculatory concept (Yamaoka et al 1990) in the present model. The extraction ratio throughout the single-pass (one-cycle) process between compartment 1 and compartment B can be estimated by equation 10.…”

Section: Theorymentioning

confidence: 99%

“…Several pharmacokinetic models have been tried to explain the enterohepatic circulation of a drug ; the most popular are compartment models with a lag time (sometimes called gap time), from bile compartment to plasma compartment (Dahlstrom & Paalzow 1978 ;Pedersen & Miller 1980a, b ;Steimer et al 1982 ;Colburn 1984 ;Miller 1984 ;Shepard et al 1985Shepard et al , 1989Plusquellec & Houin 1992, 1995Hoglund & Ohlin 1993 ;Khalil et al 1993 ;Plusquellec et al 1998 ;Funaki 1999). To simulate the secondary peaks in a plasma concentration pro® le due to enterohepatic circulation, the recirculatory concept, in which enterohepatic circulation is regarded as a recirculation process of drug molecules between the bile and the plasma compartments, has also been proposed (Yamaoka et al 1990 ;Fukuyama et al 1994 ;Yasui et al 1994Yasui et al , 1996. However, these methods have only been used to explain the data in a single dosing study, and there have been few reports on pharmacokinetic models applied to data analysis in a repeated dosing study.…”

Section: Introductionmentioning

confidence: 99%

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A pharmacokinetic model for analysis of drug disposition profiles undergoing enterohepatic circulation

Wajima

Yano

Oguma

2002

Journal of Pharmacy and Pharmacology

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A new and simple pharmacokinetic model that can explain enterohepatic circulation profiles for both single and repeated dosing was developed, and its applicability and usefulness were assessed by an actual published data set and simulation study. The model is basically a conventional compartment model, and the transfer rate from the bile compartment to the central compartment is assumed to change periodically, with the sine function being used to describe this periodical change. Using this model, the effect of the parameter values on plasma time-course profiles was examined by simulation, and the applicability of the model was tested by curve fitting to obtain the parameter estimates using an actual published data set. These studies confirmed that our model can simulate the periodical increase of the concentration due to re-absorption. By averaging the sine function in the transfer rate from the bile compartment to the central compartment, a smoothed time-course profile in the elimination phase that is independent of the enterohepatic cycle can be obtained. Also, the apparent half-life in the elimination phase can be estimated, whith is useful especially for evaluating drug accumulation during repeated dosing. It was suggested that the present model can be used to evaluate the drug disposition profile with enterohepatic circulation. The effects of sampling points and sampling time on parameter estimation are also discussed.

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Section: Theorymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

A pharmacokinetic model for analysis of drug disposition profiles undergoing enterohepatic circulation

Wajima

Yano

Oguma

2002

Journal of Pharmacy and Pharmacology

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“…Recirculatory Model for EHC of Drug and MetabolitesA recirculatory model was introduced for the understanding of the EHC of a drug, [21][22][23] and it was shown that the proposed concept included not only simple EHC models [24][25][26] but the EHC models extended by Shepard et al 27,28 and Ribera et al 29 Figure 1 represents an expanded X Abstract published in Advance ACS Abstracts, April 1, 1996.…”

Section: Theoretical Sectionmentioning

confidence: 99%

“…21 Considering the difficulty in the Laplace inversion of the image equations, MULTI(FILT) incorporating a fast inverse Laplace transform (FILT) was adopted to kinetically investigate EHC. 22,23 It is attempted in the present investigation to simply evaluate the stereoselective EHC and the synchronous chiral inversion of ketoprofen enantiomers by means of moment analysis.…”

Section: Introductionmentioning

confidence: 99%

Moment Analysis of Stereoselective Enterohepatic Circulation and Unidirectional Chiral Inversion of Ketoprofen Enantiomers in Rat

Yasui

Yamaoka

Nakagawa

1996

Journal of Pharmaceutical Sciences

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The stereoselective enterohepatic circulation (EHC) and the synchronous chiral inversion of ketoprofen enantiomer in rat were evaluated by moment analysis based on the recirculatory concept. (R)-(-)- and (S)-(+)-ketoprofen were independently administered into rats, and the plasma and bile concentrations of both enantiomers were determined by a column-switching HPLC. (S)-Ketoprofen was generated by the chiral inversion from (R)-ketoprofen, whereas (R)-ketoprofen was not generated from (S)-ketoprofen. Within 30 min after intravenous administrations, the plasma time courses of R- and S-enantiomers were almost the same between rats with laparotomy and those with bile-duct cannula. After 30 min, the plasma concentrations in rats with laparotomy were significantly higher than those in rats with bile-duct cannula. The Laplace-transformed equations for stereoselective EHC and the synchronous chiral inversion were derived by means of the transfer function method on the basis of the recirculatory theory. The global moments (AUC and MRT) which were derived directly from the transformed equations were related to the local moments for the single EHC. The recirculation ratios of (R)- and (S)-ketoprofen for the single EHC were estimated to be 15.4% and 63.6%, respectively. The absorption ratios of (R)- and (S)-ketoprofen for the absorption process from the gastrointestinal tract into the systemic circulation were 87.0% and 83.8%, respectively. The biliary excretion rations of (R)- and (S)-ketoprofen for the disposition process through the systemic circulation into the bile were 17.7% and 75.8%, respectively. The chiral inversion ratio from (R)-ketoprofen into (S)-ketoprofen was 59.5%. The complicated disposition of ketoprofen, i.e., the simultaneous EHC and chiral inversion, was able to be analyzed by a moment method in a simple way.

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“…1,[3][4][5][6][7][8] (14) where F a is absorption ratio from intestinal tract into the portal system and D p.o. is orally administered drug amount and Q p is blood flow rate of portal vein, respectively.…”

Section: Sysmentioning

confidence: 99%

Introduction of Recirculatory Analysis into Portal and Systemic Concentration Difference Method.

Ueda

Yamaoka

Sawai

et al. 2001

Biological & Pharmaceutical Bulletin

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Recirculatory analysis was introduced into the portal and systemic concentration difference method with double dosing (PS-DD method), which is an evaluation system for the local intestinal and hepatic first-pass effect. 5-Fluorouracil (5-FU) and cephalexin (CEX) were selected as model drugs. A new recirculatory system was constructed to predict the time courses of a drug concentration in the systemic and portal bloods. Bioavailability (F), local absorption ratio (F a ), hepatic recovery ratio (F H ), and local mean absorption time (t a ) estimated by recirculatory analysis were close to those calculated by moment analysis with numerical integration. Using recirculatory analysis, the sampling period was considerably shortened and the sampling number was also reduced, which demonstrates that recirculatory analysis is useful in PS-DD method.

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Analysis of enterohepatic circulation of cefixime in rat by fast inverse Laplace transform (FILT)

Cited by 19 publications

References 20 publications

A pharmacokinetic model for analysis of drug disposition profiles undergoing enterohepatic circulation

A pharmacokinetic model for analysis of drug disposition profiles undergoing enterohepatic circulation

Moment Analysis of Stereoselective Enterohepatic Circulation and Unidirectional Chiral Inversion of Ketoprofen Enantiomers in Rat

Introduction of Recirculatory Analysis into Portal and Systemic Concentration Difference Method.

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