Tablet disintegration and drug dissolution in viscous media: Paracetamol IR tablets

Parojčić, Jelena; Vasiljević, Dragana; Ibrić, Svetlana; Djurić, Z.

doi:10.1016/j.ijpharm.2007.11.058

Cited by 55 publications

(33 citation statements)

References 26 publications

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“…It is also anticipated that »the use of biorelevant media may improve the correlation to in vivo data and may detect a potential food effect« (9). The potential of viscous media to reflect food effect has also been investigated (10,11).…”

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confidence: 99%

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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confidence: 99%

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

2015

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“…For immediate-release (IR) formulations, many studies have shown that compendial in vitro dissolution tests with Apparatus 2 make it difficult to show the differences among them. This is mainly related to the higher agitation level that causes the rapid disintegration of the tablet (6). Therefore, FTC Apparatus 4 is more suitable to assess excipient and process changes that could affect the release rate of drug from the dosage form during formulation development.…”

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confidence: 99%

In Vitro Dissolution Studies of Immediate-Release and Extended-Release Formulations Using Flow-Through Cell Apparatus 4

Qiu¹,

Wang²,

Li³

2014

Dissolution Technol.

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The aims of this study were to evaluate the dissolution performance of solid dosage forms using the open and closed modes of the FTC Apparatus 4 under different flow rates and provide examples to demonstrate the advantages of the FTC method, in particular the possibility of changing the pH during experiments, in studying the release mechanisms of extended-release products. Immediate-release (IR) paracetamol and extended-release (ER) theophylline formulations were used in this study. Results from commercially available IR paracetamol tablets using FTC Apparatus 4 have shown similar dissolution behavior in the closed and open systems, reflecting well-maintained apparent sink conditions and controlled hydrodynamics in the test cells. The flow rate of FTC Apparatus 4 significantly affected the disintegration process of IR tablets. This information can be used as a discriminating tool to support formulation development and to set quality control standards and specifications. To mimic the continuous absorption of theophylline during the passage at different pH values through the whole gastrointestinal tract, dissolution tests were conducted using FTC Apparatus 4 with pH-dependent media for three different commercially available theophylline formulations. Two formulations of Uniphyllin 200-mg tablets and Nuelin SA 175-mg tablets provided a constant release rate during the course of medium pH changes, and their release behavior was predicted with accuracy by appropriate mathematical models. However, wide intervariability and biphasic release in the dissolution profiles were found for Slo-Phyllin 125-mg capsules.

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“…The extent of the effect depended upon the aggregation state of the drug contained in the dosage form and on the components of the dosage form. It is well known that increasing dissolution media viscosity retards release by increasing disintegration and dissolution time (Parojcic et al, 2008, Radwan et al, 2014, but, as shown in…”

Section: Discussionmentioning

confidence: 99%

“…Co-administration of drugs with a meal is associated with a higher viscosity of stomach contents, which prolongs tablet disintegration time (Parojcic et al, 2008) and causes simulated oral absorption to be slower for drugs with limited permeability such as atenolol, metformin hydrochloride, furosemide and metoprolol tartrate (Cvijić et al, 2014). After ingestion of a meal, water penetration rate decreased resulting in a reduction of diffusivity which reduced disintegration and dissolution of trospium tablets (Radwan et al, 2013, Radwan et al, 2014.…”

Section: Drug Delivery From Thickened Fluidsmentioning

confidence: 99%

“…The presence of dietary fibers in food products increases the viscosity of the dissolution media and forms a physical barrier that prevents mixing with gastrointestinal fluids (Shono et al, 2009, Abrahamsson et al, 2004, Parojcic et al, 2008. Furthermore, there is evidence that absorption of whole digoxin, penicillin and metformin tablets may be reduced when consumed with guar gum as a source of dietary fibre (Huupponen et al, 1984, Gin et al, 1989, and the increased viscosity resulting from guar gum consumption in dogs reduced absorption of paracetamol and hydrochlorothiazide by decreasing dissolution rate and gastric emptying rate .…”

Section: Drug Delivery From Thickened Fluidsmentioning

confidence: 99%

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Understanding the mechanism of drug delivery from thickened fluids to aid swallowing of medications

Torres¹,

Juliana²

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Medications are often crushed and mixed with foods or fluids to aid drug delivery for those who cannot or prefer not to swallow whole tablets or capsules. Dysphagic patients have the added problem of being unable to safely swallow fluids, so thickeners are added to ensure safe swallowing. These thickened fluids are then also used to deliver crushed medications in replacement of water. This thesis explores the influence of thickened water co-administration on drug release in gastric fluid, the effect of rheological properties of these agents and their contribution to describing the mechanism of release. The literature review (Chapter 1) examines oral dosage form administration, rheological properties of these agents as a means to ensure medication delivery and mechanisms of drug release. It is highlighted that thickened fluids have the potential to alter drug release but prediction of the effect of co-administration is not currently reported.Chapter 2 investigates the delivery of medications with thickened fluids as an indicator for potential compromise of drug bioavailability. In vitro dissolution in simulated gastric fluid is investigated for crushed atenolol immediate release tablets mixed with thickened fluids. Five commercial viscosityincreasing agents of varied polysaccharide composition are used at three thickness levels prescribed for dysphagic patients (levels 150, 400, 900). All types of thickening agents are non-Newtonian shear thinning fluids. The greatest thickness (level 900) significantly restricts dissolution, and products that are primarily based on xanthan gum also significantly delay dissolution at the intermediate thickness level (level 400). The interactions of the polysaccharide chains, particularly the rigid rod type conformation of xanthan gum, traps drug molecules within it resulting in impaired dissolution. Under the conditions of this experiment, the higher concentrations of thickening agents remain in large lumps rather than disintegrating into the media. Drug release is generally affected to a greater extent by high-viscosity fluids than low-viscosity fluids at 50 s -1 , but viscosity at this single shear rate of 50 s -1 is not a good indicator for effect on drug dissolution because viscosity changes with shear rate. The determination of other rheological parameters such as viscoelasticity and the effect of breaking up of the structures may be required.To investigate whether it is possible to improve drug release from thickened fluids, in Chapter 3 the effect of the state of aggregation of the active ingredient with thickened fluids is investigated.Paracetamol is the model drug because it is available in a range of formulations with the drug in solution (elixir, dissolved effervescent tablet) or dispersion (suspension). Xanthan gum, which causes the greatest restriction on dissolution (Chapter 2), is used at level 900 as the thickener.ii Crushed tablets with thickener are prepared using manual (i.e. the standard method in clinical practice) or mechanical mixing. The unthickene...

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Tablet disintegration and drug dissolution in viscous media: Paracetamol IR tablets

Cited by 55 publications

References 26 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

In Vitro Dissolution Studies of Immediate-Release and Extended-Release Formulations Using Flow-Through Cell Apparatus 4

Understanding the mechanism of drug delivery from thickened fluids to aid swallowing of medications

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