Determination of the mechanical impact force in the in vitro dissolution test and evaluation of the correlation between in vivo and in vitro release

Aoki, Shigeru; Ando, Hidenobu; Tatsuishi, Kimio; Uesugi, Keizo; Ozawa, Hiroshi

doi:10.1016/0378-5173(93)90391-r

Cited by 42 publications

(22 citation statements)

References 13 publications

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“…As an example, polystyrene pellets have been added to the dissolution medium in order to increase the mechanical agitation rate to improve the simulation of the erosive conditions in the human GI tract [50]. A modification that avoids the spontaneous and most probably artefactual agglomeration of undissolved material directly under the stirrer blade in the paddle apparatus is the brush-like crescent-shaped spindle device [51].…”

Section: Simulation Of Mechanical Conditions Of the Gastrointestinal mentioning

confidence: 99%

A biorelevant dissolution stress test device – background and experiences

Garbacz¹,

Klein²,

Weitschies³

2010

Expert Opinion on Drug Delivery

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The new apparatus was evaluated using extended release (ER) tablets of nifedipine and diclofenac. The dissolution characteristics of some of the tested products were strongly dependent on the test conditions and could be distinctly influenced by the mechanical stress events of biorelevant intensity. Results of these experiments thus indicated that a high sensitivity of dosage forms to GI-specific physical conditions has to be regarded as a major cause of irregularities in the drug release profiles, which may result in fluctuations of the individual drug plasma concentration profiles, as, for example, caused by dose dumping.

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Section: Simulation Of Mechanical Conditions Of the Gastrointestinal mentioning

confidence: 99%

A biorelevant dissolution stress test device – background and experiences

Garbacz¹,

Klein²,

Weitschies³

2010

Expert Opinion on Drug Delivery

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“…Aoki and others (1992, 1993) investigated the dissolution behavior of drug tablets by adding polystyrene beads into dissolution medium to create mechanical destruction or frictional force on the tablets. A modification of this approach was used in this model stomach system.…”

Section: Methodsmentioning

confidence: 99%

“…Various in vitro systems have been considered to model the human GI tract for the purpose of investigating in vivo dissolution of drugs (Aoki and others 1992, 1993), viability of probiotic intake (Molly and others 1993), nutrition availability (Hoebler and others 2002), and contaminant absorption (Oomen and others 2003). To a certain extent, these models simulate the gastric environment, including hydrodynamic flow as well as acidic and enzymatic functions.…”

Section: Introductionmentioning

confidence: 99%

A Model Stomach System to Investigate Disintegration Kinetics of Solid Foods during Gastric Digestion

Kong¹,

Singh²

2008

Journal of Food Science

124

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Knowledge of the disintegration kinetics of food particulates in the human stomach is essential for assessing the bioaccessibility of nutrients in solid foods and understanding stomach emptying. The objective of this study was to develop a model stomach system and to investigate the kinetics of food disintegration. Our system consisted mainly of a turntable and a jacketed glass chamber containing simulated gastric juice in which plastic beads were added to simulate food particulates as well as provide a suitable mechanical destructive force on food samples. The mechanical force on the samples was simultaneously measured using the load cell of a TA-XT2 texture analyzer. Cylindrical carrots and ham samples were used as representative foods. The system is capable of simulating the in vivo stomach in terms of providing a wide range of continuous and periodic forces comparable to those measured in vivo. The modified power exponential function of the form y(t)= 1 - (1 -e(-kt))(beta), where y(t) is the mass retention ratio at time t, provided a reasonable description for the disintegration performance of tested foods. The mass retention curve can be either a sigmoidal decay with an initial delay or an exponential decay, which are decided largely by the hardness of the foods during digestion and the extent of physical force acting on the foods. A good match was observed between the kinetics of food disintegration and in vivo stomach emptying.

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“…Aoki et al tested matrix tablets using apparatus 2 with the addition of polystyrene beads to better reflect in vivo conditions in gastrointestinal tract of beagle dogs. By using different bead amounts, media volumes and revolutions per minute values, they found the optimal conditions that were able to predict in vivo dissolution (24). The use of the USP dissolution apparatus 3 (reciprocating cylinder, Bio-dis) has also been suggested for simulating the mechanical conditions within the GIT, but it was not extensively studied for evaluating matrix tablets (25)(26)(27).…”

Section: Introductionmentioning

confidence: 99%

“…Different hydrodynamic conditions, however, are difficult to simulate with conventional in vitro dissolution methods. So far, some modifications to conventional dissolution apparatus, as well as novel dissolution methods for elucidating the mechanical stress, have been proposed (20)(21)(22)(23)(24). Abrahamsson et al designed a rotation-beaker dissolution apparatus that enabled an in vivo predictable shear stress on the surface of the hydrophilic polymer matrix tablet (20).…”

Section: Introductionmentioning

confidence: 99%

A Novel Beads-Based Dissolution Method for the In Vitro Evaluation of Extended Release HPMC Matrix Tablets and the Correlation with the In Vivo Data

Klančar¹,

Markun²,

Baumgartner

et al. 2012

AAPS J

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Abstract. The aim of this work was to establish alternative in vitro dissolution method with good discrimination and in vivo predictability for the evaluation of HPMC extended release matrix tablets. For this purpose, two different HPMC matrix tablet formulations were first evaluated by a range of conventional dissolution testing methods using apparatus 1, apparatus 2, and apparatus 3 according to US Pharmacopoeia. Obtained results showed low discrimination between the tested samples. Afterward, a novel dissolution testing method which combines plastic beads and apparatus 3 was developed with the aim to better mimic the mechanical forces that occur in vivo. Results showed that sufficiently large mechanical stress with high dips per minute program setting (apparatus 3) was needed to obtain in vitro discriminative results, which are in accordance with the in vivo data. The in vivo relevance of the method was confirmed with the establishment of the level A in vitro-in vivo correlation.

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Determination of the mechanical impact force in the in vitro dissolution test and evaluation of the correlation between in vivo and in vitro release

Cited by 42 publications

References 13 publications

A biorelevant dissolution stress test device – background and experiences

A biorelevant dissolution stress test device – background and experiences

A Model Stomach System to Investigate Disintegration Kinetics of Solid Foods during Gastric Digestion

A Novel Beads-Based Dissolution Method for the In Vitro Evaluation of Extended Release HPMC Matrix Tablets and the Correlation with the In Vivo Data

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