Irregular absorption profiles observed from diclofenac extended release tablets can be predicted using a dissolution test apparatus that mimics in vivo physical stresses

Garbacz, Grzegorz; Wedemeyer, Ralph-Steven; Nagel, Stefan; Gießmann, Thomas; Mönnikes, Hubert; Wilson, Clive G.; Siegmund, Werner; Weitschies, Werner

doi:10.1016/j.ejpb.2008.05.029

Cited by 149 publications

(128 citation statements)

References 34 publications

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“…This dynamic process provides a better representation of the transit of the drug formulation through the GI tract, which more closely captures the kinetic aspects of the actual in vivo drug release process. Garbacz et al have also showed diclofenac and nifedipine drug dissolution profiles to be predicted using a dissolution apparatus that mimics in vivo physical stresses [146,147]. Kostewicz et al [148] also developed a two-compartmental apparatus using a peristaltic pump using fasted and fed state-simulated media.…”

Section: Dissolution Apparatusesmentioning

confidence: 99%

Drug release from matrix tablets: physiological parameters and the effect of food

Nokhodchi

Asare-Addo

2014

Expert Opinion on Drug Delivery

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Introduction: As dissolution plays an important and vital role in the drug-delivery process of oral solid dosage forms, it is, therefore, essential to critically evaluate the parameters that can affect this process. Areas covered:The consumption of food as well as the physiological environment and properties of the gastrointestinal tract, such as its volume and composition of fluid, the fluid hydrodynamics, properties of the intestinal membrane, drug dose and solubility, pK a , diffusion coefficient, permeability and particle size, all affect drug dissolution and absorption rate. There are several dissolution approaches that have been developed to address the conditions as experienced in the in vivo environment, as the traditional dissolution being a quality control method is not biorelevant and as such do not always produce meaningful data. This review also describes the development of a systematic way that differentiates between robust and non-robust formulations by varying the effects of agitation and ionic strength through the use of the automated United States Pharmacopeia type III Bio-Dis apparatus. Expert opinion:With the improved understanding of the physiological parameters that can affect the oral bioperformance of dosage forms, strides have, therefore, been made in making dissolution testing methods more bio-logically based with the view of obtaining more in vitro--in vivo correlations.Keywords: agitation rate, biodissolution, drug release, effect of food, hydrophilic matrices, ionic strength Highlights -Understanding all the physiological parameters can serve as a basis for designing dissolution testing methods and systems that can more fully represent the gastrointestinal (GI) tract in humans and allow more in vitro-in vivo (IVIVC) correlations to be obtained thereby improving the oral bioperformance of dosage forms.-Simulation of GI conditions is essential to adequately predict the in vivo behaviour of drug formulations.-The choice of appropriate media for in vitro tests is crucial to their ability to correctly forecast the food effect in pharmacokinetic studies.-Several methods of dissolution testing have been conducted and are still ongoing that seek to further understand and develop media and dissolution methods to better represent the in vivo conditions and to aid in the better prediction of in vivo drug release.-Systematic change of agitation method and ionic strength evaluation may be used as additional tools in allowing for the identification of potential fed and fasted effects on drug release from hydrophilic matrices in the drive for developing dissolution methodologies that are more relevant in helping to achieve more IVIVC.

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Section: Dissolution Apparatusesmentioning

confidence: 99%

Drug release from matrix tablets: physiological parameters and the effect of food

Nokhodchi

Asare-Addo

2014

Expert Opinion on Drug Delivery

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“…The mode of movement of the dosage form in the TIM system also differs significantly from conventional apparatus. In their dissolution system, Garbacz et al (5) simulated the different pressure forces that influence the dosage form during its movement along the GI tract. There are other systems described in the literature (6) that simulate at least some of the physical influences to which the dosage form is exposed in the GI tract up to a certain degree of biorelevance.…”

Section: Introductionmentioning

confidence: 99%

Development of a Glass-Bead Device for Dissolution Testing

Bogataj¹,

Cof²,

Mrhar³

2015

Dissolution Technol.

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A device for dissolution testing with a special type of stirring element and typical movement of a dosage form was developed and constructed in our laboratory. It consists of a working vessel in which a suitable amount of small glass beads is pushed by a stirring bar in an appropriate medium. A heap of beads forms in front of the stirring bar and moves around the vessel. A solid dosage form, most frequently a tablet, is placed in the medium on the surface of the bead layer and is moved due to the movement of this bead layer. The newly developed device could be used in experimental work as a part of a dissolution system based on the flow-through principle. Two different series of tablets containing different drugs were tested to show the applicability of this device. Dissolution from one series of tablets was strongly dependent on increasing mechanical influences on the tablet during dissolution testing, while dissolution from the tablets of another series was not susceptible to the change in the same mechanical parameters. Comparison with dissolution results in USP Apparatus 2 also showed differences between different stirring rates in the case of mechanically susceptible tablets, while tablets that were not susceptible to these influences gave very similar dissolution profiles in both systems. Mechanical influences on the dosage form in the newly developed system could be varied by changing the amount of glass beads and the stirring rate; however, the biorelevance of parameters of this system remains to be determined.

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“…These include multicompartmental models such as the artificial stomach duodenal model (ASD), which has been used to evaluate the effect of gastric emptying on drug dissolution, solubilization, and precipitation in separate duodenal compartment in several studies (5)(6)(7)(8). In addition, models exist that are designed to simulate GI physical stress forces such as the novel stress dissolution tester (9,10) or the modified Apparatus 2 by Burke et al (11). Systems that mimic absorption have been described, from the simple partitioning approach using USP apparatus with organic solvents (12)(13)(14) to the more complex models like the FloVitro Dissolution Testing system provided by Rohm and Haas (15).…”

Section: Introductionmentioning

confidence: 99%

A Formulation Case Study Comparing the Dynamic Gastric Model with Conventional Dissolution Methods

Mann¹,

Pygall²

2012

Dissolution Technol.

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Even in the 21st century, conventional compendial dissolution testing remains a key cornerstone of the drug development process and quality control testing. However, opportunities exist with respect to in vitro technology developments that provide the potential for formulation and analytical scientists to exceed the capabilities of the conventional dissolution test toward a more biorelevant testing regime. This work presents a product development case study in which bioequivalence was observed between an immediate-release (IR) innovator product and a comparative singlelayer reference product. Despite this, when the constituent granule of the comparative single-layer reference product was formulated in a bilayer formulation with a nondisintegrating second layer, bioequivalence versus the innovator was not achieved. The use of USP Apparatus 2 dissolution testing failed to predict the bioequivalence failure, and hence an investigation was undertaken to develop a mechanistic understanding of in vivo behavior. Using both USP Apparatus 4 dissolution in the open-loop configuration and the dynamic gastric model (a novel in vitro model designed to mimic the human stomach), an understanding of the dissolution and disintegration properties of the reference product was established. The insights gained using novel technology facilitated the redesign and subsequent improvement in pharmacokinetic parameters of a complex pharmaceutical dosage form.

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Irregular absorption profiles observed from diclofenac extended release tablets can be predicted using a dissolution test apparatus that mimics in vivo physical stresses

Cited by 149 publications

References 34 publications

Drug release from matrix tablets: physiological parameters and the effect of food

Drug release from matrix tablets: physiological parameters and the effect of food

Development of a Glass-Bead Device for Dissolution Testing

A Formulation Case Study Comparing the Dynamic Gastric Model with Conventional Dissolution Methods

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