Dosage form-related food interaction observed in a marketed once-daily nifedipine formulation after a high-fat American breakfast

Bs, Schug; Brendel, E.; Wonnemann, Meinolf; Wolf, D; Wargenau, Manfred; Dingler, A; Hh, Blume

doi:10.1007/s00228-002-0444-7

Cited by 50 publications

(33 citation statements)

References 7 publications

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“…Food co-administration with the »erosive tablet« caused much faster drug release, described as a »dose dumping« phenomenon (14). Similar results were obtained for the nifedipine extended release formulation containing encapsulated HPMC-based mini tablets, where »a significant loss of modified-release characteristics« was detected under fed conditions (29). In a separate study, it was found that food caused a pronounced delay in nifedipine absorption from Slofedipine ® XL, an enteric coated modified release tablet with erosive polymer matrix (30).…”

Section: The Extent Of Food Effectsupporting

confidence: 68%

“…In further investigations, hydrodynamic mechanical stress was considered to be the main factor responsible for postprandial effects on tablet erosion (10). Schug et al (14,29,30) reported formulationspecific food effects for different nifedipine modified release preparations. In vivo drug delivery profiles obtained by numerical deconvolution using p.o.…”

Section: The Extent Of Food Effectmentioning

confidence: 99%

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Deciphering nifedipine in vivo delivery from modified release dosage forms: Identification of food effect

2015

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With the increased reliance on in vitro dissolution testing as an indicator of in vivo drug behavior and the trend towards the in silico modeling of dosage form performance, the need for bioperformance dissolution methodology development has been enhanced. Determination of the in vivo drug delivery profile is essential for the bioperformance dissolution test development and in vitro/in vivo correlation modeling, as well as the understanding of absorption mechanisms. The aim of this study was to compare different methods in terms of their usefulness and applicability in deciphering in vivo delivery of nifedipine administered in modified release dosage forms. A detailed survey of publications on nifedipine pharmacokinetics was done and used to identify the magnitude of food effect. In vitro dissolution testing was performed under various experimental conditions. Obtained results indicate the potential for using the developed in silico model coupled with discriminative in vitro dissolution data for identification of the in vivo drug product behavior

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Section: The Extent Of Food Effectsupporting

confidence: 68%

Section: The Extent Of Food Effectmentioning

confidence: 99%

Deciphering nifedipine in vivo delivery from modified release dosage forms: Identification of food effect

2015

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“…Formulations utilizing capsules containing mini tablets,20 an eroding matrix,21 and a monolayer matrix22 all exhibited similar discrepancies when compared to nifedipine GITS. In all cases, this was characterized by inconsistent in vitro release properties at different pH values and a failure to demonstrate pharmacokinetic bioequivalence to nifedipine GITS.…”

Section: Comparisons Of Different Drugs and Formulationsmentioning

confidence: 98%

“…These have employed erosive tablet technology,19 a capsule containing several mini tablets,20 hydrophilic matrix tablets,21 a monolithic enteric-coated-like tablet with an erosive polymer matrix,22 an eroding matrix,23 and a monolayer matrix 24…”

Section: Other Once-daily Formulationsmentioning

confidence: 99%

“…In general, there were significant alterations in the plasma concentration–time relationship in both the extent and the rate of drug absorption for each of the test formulations compared to nifedipine GITS. It is also important to note that, when the concentration–time curves for individual subjects were examined, the non-GITS formulations exhibited considerable inter-subject variability, while, in contrast, there was minimal inter-subject variability in either the fasted or fed studies with the nifedipine GITS 20,24…”

Section: Comparisons Of Different Drugs and Formulationsmentioning

confidence: 99%

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A review of the gastrointestinal therapeutic system (GITS) formulation and its effectiveness in the delivery of antihypertensive drug treatment (focus on nifedipine GITS)

Meredith

Elliott²

2013

IBPC

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Hypertension treatment guidelines do not discriminate within drug classes and, furthermore, do not consider whether or not all of the formulations of any given drug licensed for once-daily administration can be considered to be therapeutically interchangeable. This article focuses on this issue with respect to nifedipine and the development of the gastrointestinal therapeutic system (GITS) formulation. Nifedipine GITS is regarded as the gold standard once-daily formulation of nifedipine and, as such, it is anticipated that alternative formulations will be therapeutically equivalent to nifedipine GITS. In general, this depends on demonstrating pharmacokinetic bioequivalence. This article is intended to focus attention on generic substitution and, in particular, on aspects of the scientific basis for the substitution of generic products in place of branded products. Such substitution is required for cost-saving or cost-containment reasons and is justified on the basis that the generic (substitute) drug is “therapeutically” equivalent to the branded drug. Unfortunately, there are serious shortcomings in the current methods of assessment insofar as they are typically based on statistical comparisons of average pharmacokinetic parameter values, using arbitrary comparative criteria. This article illustrates the shortcomings of the current approaches to generic substitution and concludes that, in regulatory terms, either more rigorous pharmacokinetic criteria are required or pharmacodynamic indices should be added to reinforce the regulatory criteria. Generic substitution is a balancing act but, at the moment, the cost issue is dominant. To restore the balance, equivalent efficacy must be confirmed. At present, therefore, in the absence of such regulatory rigor, the obvious course is to prefer the branded product, the therapeutic efficacy of which (including outcome benefits) has been established.

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Application of the Simcyp Population‐based PBPK Simulator to the Modelling of MR Formulations

Patel

Pathak

Turner

2022

Oral Drug Delivery for Modified Release Formulations

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Dosage form-related food interaction observed in a marketed once-daily nifedipine formulation after a high-fat American breakfast

Cited by 50 publications

References 7 publications

Deciphering nifedipine in vivo delivery from modified release dosage forms: Identification of food effect

Deciphering nifedipine in vivo delivery from modified release dosage forms: Identification of food effect

A review of the gastrointestinal therapeutic system (GITS) formulation and its effectiveness in the delivery of antihypertensive drug treatment (focus on nifedipine GITS)

Application of the Simcyp Population‐based PBPK Simulator to the Modelling of MR Formulations

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