Formulation-dependent food effects demonstrated for nifedipine modified-release preparations marketed in the European Union

Schug, Barbara; Brendel, E.; Wolf, D; Wonnemann, Meinolf; Wargenau, Manfred; Blume, Henning

doi:10.1016/s0928-0987(02)00008-8

Cited by 63 publications

(47 citation statements)

References 6 publications

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“…Data on nifedipine pharmacokinetics following administration of osmotic controlled--release tablets under fasted and fed state conditions reported in the study of Schug et al (14) were evaluated as the response function. Plasma concentration-time (c-t) profiles following intravenous and/or oral administration of a nifedipine immediate-release (IR) capsule reported by Rashid et al (18) were used as the reference/weighting function.…”

Section: In Vivo Datamentioning

confidence: 99%

“…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%

“…Literature data on nifedipine pharmacokinetics after drug administration with or without food are available from a number of sources. It has been reported that nifedipine food effect may be formulation specific (14)(15)(16)(17). Such data imply that the drug/food interactions observed are physicochemically based and emphasize the importance of bioperformance in vitro testing for the prediction of in vivo behavior of a drug product (10,14).…”

mentioning

confidence: 91%

“…Numerous nifedipine modified release formulations have been marketed in order to improve therapeutic compliance in chronic treatment of hypertension and angina pectoris and to reduce the concentration-related adverse effects associated with peak plasma levels (12,14). Literature data on nifedipine pharmacokinetics after drug administration with or without food are available from a number of sources.…”

mentioning

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: In Vivo Datamentioning

confidence: 99%

Section: The Extent Of Food Effectmentioning

confidence: 99%

mentioning

confidence: 91%

mentioning

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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“…After administration of formulation, where as in test (optimized formulation), area under plasma concentration (AUC 0−t ) was found to be 126 ng-h/ml, AUC (0-∞) was found to be 205 ng-h/ml, AUMC (0-t) was found to be 630 ng-h*h/ml, AUMC (0-∞) was found to be 1665 ng-h*h/ml, and its C max was found to be 28 ng/ml, where as t max at 4 h. However, values reported [21] were 23.2 µg/l and 9 h when nifedipine administered as fed state with 60 mg dose for the human volunteer.…”

Section: In Vivo Studiesmentioning

confidence: 87%

Untitled

Kumaravelrajan¹

2017

AJP

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Aims: Sustained-release formulations have been widely developed to improve the therapeutic performance of drugs, in particular, to increase pharmacological efficacy and reduce side effects. Developing spansule dosage form of nifedipine using extrusion and spheronization technique provides efficient control of delivery of drugs over the period of 8 h. Nifedipine pellets coated with hydrophilic hydroxypropyl methylcellulose polymer, hydrophobic polymer (ethyl cellulose), and semipermeable polymer (cellulose acetate) to sufficient weight gain. Desired rate of release achieved by of blend of polymers after optimization of variable. Settings and Design: A rotatable central composite design used with five levels and three polymers for 15 formulations. Based on rate of drug release, formulation optimized backward two-factor interaction and polynomial regression equation. Materials and Methods: Initially nifedipine pellets prepared by extruder and spheronizer and later coated up to desired weight gain by conventional coating pan utilizing various polymers. After coating, pilot blend was prepared with all three polymers. In vitro dissolution carried out to find out release rate and percent of dissolution at t95% as dependent variable. Then, optimized formulation compared with market preparation and in vivo animal study done using mice. Results: In vitro dissolution rate of drug indicated the drug release depends on thickness of coat. However, formulation shown considerable release even with higher level of coat thickness with ethyl cellulose because of other two polymers present in the blend dominates the release pattern. The ratio of mixing of pilot blends also a critical factor in developing spansule dosage form. Desired release pattern achieved after equal ratio of mixing polymer pilot blend and optimization of polymer level. Conclusion: The prototype of this formulation design can use for developing spansule dosage form of any drug.

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Effects of Food on Drug Absorption

Marasanapalle

Jasti

2011

Oral Bioavailability

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Formulation-dependent food effects demonstrated for nifedipine modified-release preparations marketed in the European Union

Cited by 63 publications

References 6 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

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Effects of Food on Drug Absorption

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