In vitro simulation of food effect on dissolution of deramciclane film-coated tablets and correlation with in vivo data in healthy volunteers

Al-Behaisi, Samar; Antal, István; Morovján, György; Szúnyog, József; Drabant, Sándor; Marton, S.; Klebovich, Imre

doi:10.1016/s0928-0987(01)00195-6

Cited by 16 publications

(5 citation statements)

References 22 publications

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“…Five hundred milliliters of complex solution with a pH value of 1.2 was prepared by adding 0.35 g sodium chloride, 0.5 g glycine and 31.6 mL hydrochloric solution of 1 M into distilled water [35]. A given amount of metal salt such as Pb(NO 3 ) 2 , Cu(NO 3 ) 2 or Cd(NO 3 ) 2 , was added into the solution prior to adsorption tests.…”

Section: Materials and Chemicalsmentioning

confidence: 99%

Trapping the lead ion in multi-components aqueous solution by natural clinoptilolite

Qiu

Fang

et al. 2010

Journal of Hazardous Materials

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Section: Materials and Chemicalsmentioning

confidence: 99%

Trapping the lead ion in multi-components aqueous solution by natural clinoptilolite

Qiu

Fang

et al. 2010

Journal of Hazardous Materials

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“…For extended release formulations, reasonable linear correlations have been obtained from a number of IVIVC studies [1,2,3,4,5]. In other cases, linear correlations were not satisfactory [6,7,8,9], or the data could not be correlated [2,10,11]. Although in the case of extended release formulations linear relationships are frequently obtained, both the United States Pharmacopoeia (USP) and the Food and Drug Administration (FDA) state that non-linear models are also acceptable to describe IVIVCs [12,13,14].…”

Section: Introductionmentioning

confidence: 99%

In Vitro–In Vivo Correlations Based on In Vitro Dissolution of Parent Drug Diltiazem and Pharmacokinetics of Its Metabolite

et al. 2019

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In this study a novel type of in vitro–in vivo correlation (IVIVC) is proposed: The correlation of the in vitro parent drug dissolution data with the in vivo pharmacokinetic data of drug’s metabolite after the oral administration of the parent drug. The pharmacokinetic data for the parent drug diltiazem (DTZ) and its desacetyl diltiazem metabolite (DTZM) were obtained from an in vivo study performed in 19 healthy volunteers. The pharmacokinetics of the parent drug and its metabolite followed a pseudomono-compartmental model and deconvolution of the DTZ or DTZM plasma concentration profiles was performed with a Wagner–Nelson-type equation. The calculated in vivo absorption fractions were correlated with the in vitro DTZ dissolution data obtained with USP 2 apparatus. A linear IVIVC was obtained for both DTZ and DTZM, with a better correlation observed for the case of the metabolite. This type of correlation of the in vitro data of the parent compound with the in vivo data of the metabolite could be useful for the development of drugs with active metabolites and prodrugs.

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“…In vitro–in vivo correlations (IVIVCs) are correlations between in vitro dissolution data and in vivo release kinetics, estimated by the deconvolution of pharmacokinetic IVIVCs were constantly recommended by regulatory authorities in the last decades when developing extended-release formulations ( US Food and Drug Administration, 1997a ; US Food and Drug Administration, 1997b ; European Medicines Agency, 2014a ; European Medicines Agency, 2014b ). The correlation can be good and even linear ( Humbert et al, 1994 ; Eddington et al, 1998 ; Emami 2006 ) or nonlinear [ Lake et al, 1999 ; Varshosaz et al, 2000 ; Rao et al, 2001 ; Al-Behaisi et al, 2002 ], or even obscure ( Eddington et al, 1998 ; Mircioiu et al, 2005 ; Meyer et al, 1998 ; Mircioiu et al, 2018 ). Complex models were proposed in cases of nonlinearity ( Polli et al, 1996 ; Dunne et al, 1997 ; Dunne et al, 1999 ), but the number of parameters of models is higher, and the fitting algorithms are more unstable ( Sandulovici et al, 2009 ; Tvrdonova et al, 2009 ).…”

Section: Introductionmentioning

confidence: 99%

Estimation of the In Vivo Release of Amiodarone From the Pharmacokinetics of Its Active Metabolite and Correlation With Its In Vitro Release

et al. 2021

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Due to its very low water solubility and complex pharmacokinetics, a reliable point-to-point correlation of its in vitro release with its pharmacokinetics has not been achieved so far with amiodarone. The correlation of the in vitro dissolution of a drug with the pharmacokinetics of one of its metabolites was recently proposed by the authors of the article as an additional or alternative analysis to the usual in vitro correlations in vivo, mainly in the case of fast-absorbing drugs that have metabolites with a significant therapeutic effect. The model proposed by the authors considers that amiodarone has a slow dissolution, rapid absorption, and rapid metabolism, and before returning to the blood from other compartments, its pharmacokinetics is determined mainly by the kinetics of release in the intestine from the pharmaceutical formulation. Under these conditions, the rate of apparition of desethylamiodarone in the blood is a metric of the release of amiodarone in the intestinal fluid. Furthermore, it has been shown that such an estimated in vivo dissolution is similar, after time scaling, to the dissolution measured experimentally in vitro. Dissolution data of amiodarone and the pharmacokinetic data of its active metabolite desethylamiodarone were obtained in a bioequivalence study of 24 healthy volunteers. The elimination constant of the metabolite from plasma was estimated as the slope of the linear regression of logarithmically transformed data on the tail of plasma levels. Because the elimination of desethylamiodarone was shown to follow a monoexponential model, a Nelson–Wagner-type mass equilibrium model could be applied to calculate the time course of the “plasma metabolite fraction.” After Levi-type time scaling for imposing the in vitro–in vivo correlation, the problem became that of the correlation between in vitro dissolution time and in vivo dissolution time, which was proven to follow a square root model. To validate the model, evaluations were performed for the reference drug and test drug separately. In both cases, the scaled time for in vivo dissolution, t*, depended approximately linearly on the square root of the in vitro dissolution time t, with the two regression lines being practically parallel.

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In vitro simulation of food effect on dissolution of deramciclane film-coated tablets and correlation with in vivo data in healthy volunteers

Cited by 16 publications

References 22 publications

Trapping the lead ion in multi-components aqueous solution by natural clinoptilolite

Trapping the lead ion in multi-components aqueous solution by natural clinoptilolite

In Vitro–In Vivo Correlations Based on In Vitro Dissolution of Parent Drug Diltiazem and Pharmacokinetics of Its Metabolite

Estimation of the In Vivo Release of Amiodarone From the Pharmacokinetics of Its Active Metabolite and Correlation With Its In Vitro Release

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