A Novel in Vitro and Numerical Analysis of Shear-Induced Drug Release from Extended-Release Tablets in the Fed Stomach

Abrahamsson, Bertil; Pal, Anupam; Sjöberg, Marie; Carlsson, Maria; Laurell, Emma; Brasseur, James G.

doi:10.1007/s11095-005-5272-x

Cited by 111 publications

(99 citation statements)

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“…Periodically generated ACWs induce the motion of the gastric contents, mix the gastric contents, and grind bulk solid foods to reduce their particle size (Kong and Singh, 2008). Several research groups have reported that fluid motions in the stomach promote the emulsification of oil components and drug release from matrix tablets (Schwizer et al, 2006;Abrahamsson et al, 2005). Ajaj et al (2004) reported unusual peristaltic motions in gastroparesis patients having a decreased ACW speed or different degrees of ACW contractions, which were monitored by magnetic resonance imaging (MRI).…”

Section: Introductionmentioning

confidence: 99%

Development of a Human Gastric Digestion Simulator Equipped with Peristalsis Function for the Direct Observation and Analysis of the Food Digestion Process

Kozu

Nakata

Nakajima

et al. 2014

FSTR

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A novel in vitro gastric device, the Gastric Digestion Simulator (GDS), was developed for the direct observation and quantitative analysis of the food digestion process in the human stomach. In addition to simulating the chemical digestion environment, this device provides a physical digestion environment comparable to that found in the stomach by simulating peristalsis, which is assumed to contribute to solid food disintegration. The GDS was successfully used to directly observe the disintegration process of Tofu (bean curd) as a typical solid food containing protein. The size distribution and protein content of Tofu particles during the digestion experiments were investigated. The results demonstrated the difference in particle disintegration between GDS and flask shaking experiments, which may be due to the lack of peristalsis in the latter case. Moreover, the size distribution of Tofu particles after the GDS experiments was affected by the physical properties of Tofu, thus revealing the usefulness of GDS for food digestion analysis.Keywords: GI tract, gastric digestion, in vitro gastric device, peristalsis, direct observation, solid food IntroductionIn the human gastrointestinal (GI) tract, foods are digested by a combination of physical and chemical processes. Chemical digestive processes are catalyzed by digestive enzymes secreted in the stomach and small intestine, and disintegrate foods down to the molecular scale. However, physical digestive processes, which are induced mainly by peristalsis, mix and empty gastric and intestinal contents, and thus play an important role in promoting food digestion in the GI tract. Peristalsis in the GI tract is caused by peristaltic wall motion (e.g., antral contraction waves (ACWs)) in the stomach. Periodically generated ACWs induce the motion of the gastric contents, mix the gastric contents, and grind bulk solid foods to reduce their particle size (Kong and Singh, 2008) Food digestion in the human GI tract has been studied using in vivo, in vitro, and in silico approaches. MRI has been used for in vivo studies on gastric peristaltic motion and the physical properties of gastric contents. The speed of ACWs and the ACW amplitude in the human stomach were calculated using data obtained by real-*To whom correspondence should be addressed. time MRI (King et al., 1984;Pallotta et al., 1998). The timedependent change of the viscosity of the gastric contents was measured using echo planar MRI (Marciani et al., 2000). This study seeks to develop a new in vitro gastric digestion device that focuses mainly on the physical digestion environment of the human stomach, and to assess the device's performance. The gastric digestion simulator (GDS) that we developed here can simulate peristaltic motion in the human stomach and enables direct observation of the digestion process in real time. In this study, two different types of Tofu were used as model solid foods.We investigated food digestion characteristics using GDS to quantitatively understand the dynamic digestion processes in t...

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Section: Introductionmentioning

confidence: 99%

Development of a Human Gastric Digestion Simulator Equipped with Peristalsis Function for the Direct Observation and Analysis of the Food Digestion Process

Kozu

Nakata

Nakajima

et al. 2014

FSTR

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“…The hydrodynamic conditions generated in a USP II apparatus can be compared to the expected in vivo hydrodynamics by using the Reynolds number and the Reynolds numbers for bulk flow in the USP II apparatus are around 2000 [141] which is significantly greater than the physiological range (0.1 -30) as suggested by Abrahamsson et al [51,140].…”

Section: Dissolution Apparatusesmentioning

confidence: 99%

“…Viscosity is also affected by pH in addition to soluble meal content and concentration [4]. Test meals containing dietary fibres are administered that have viscosities ranging from 10 to > 10,000 cP [4,48,49] [4,50,51].…”

Section: Physiological Parametersmentioning

confidence: 99%

“…This is depicted as Equation The four types of compendial dissolution apparatuses used for testing the oral dosage forms include the USP I (basket) and the USP II (paddle) apparatuses which can be successfully used for QC purposes, such as lot-to-lot quality testing [65]. These methods, however, are not physiologically relevant as they use large volume of media (500 -1000 ml), enable the use of one dissolution medium at a time and have hydrodynamics that do not resemble the GI tract [51,65]. Several studies have investigated the flow pattern of the dissolution apparatuses USP I (basket) and USP II (paddle) at various speeds by using computational fluid dynamics [131].…”

Section: Dissolution Apparatusesmentioning

confidence: 99%

“…The USP III apparatus provides a means of stepping through different buffers and has been reported to be a very useful technique for extended release dosage forms [138][139][140]. The Reynolds number is a non-dimensional parameter in fluid dynamics which provides an estimate of the ratio of fluid inertia (or flow acceleration) to frictional force in the flow around a dosage form [51,140].…”

Section: Dissolution Apparatusesmentioning

confidence: 99%

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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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Dissolution

Batchelor

Butler

2021

Biopharmaceutics

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A Novel in Vitro and Numerical Analysis of Shear-Induced Drug Release from Extended-Release Tablets in the Fed Stomach

Abstract: Shear force effects on drug release from matrix tablets relevant for fed state are for the first time possible to predict by in vitro dissolution testing.

Cited by 111 publications

References 17 publications

Development of a Human Gastric Digestion Simulator Equipped with Peristalsis Function for the Direct Observation and Analysis of the Food Digestion Process

Development of a Human Gastric Digestion Simulator Equipped with Peristalsis Function for the Direct Observation and Analysis of the Food Digestion Process

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

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