Physiological Parameters Relevant to Dissolution Testing

Diebold, Steffen M.

doi:10.1201/9780849359170.ch6

Cited by 12 publications

(13 citation statements)

References 53 publications

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“…At 50 rpm the USP2 apparatus produces maximum velocities between 0.049 and 0.067 m/s (D'Arcy et al, 2005), while the USP1 apparatus has shown to have maximum velocities generally lower than the USP2 apparatus at the same rotational speed and with a maximum value of 0.026 m/s (D'Arcy et al, 2009). The calculated velocities in the stomach due to retropulsive jets has been calculated to be around 0.0075 m/s (Pal et al, 2004), while the average transit time in the intestine ranges between 0.0002 and 0.0008 m/s (Diebold, 2005). So even at 50 rpm, the velocities experienced by the formulation in vitro are much higher than those in vivo, which is reflected by the observed IVIVCs.…”

Section: Resultsmentioning

confidence: 90%

“…and USP2 apparatus is much higher than the in vivo hydrodynamics. The fluid velocities generally produced by the dissolution apparatus are very high and have Reynolds numbers between 5000 and 10000 (Mudie et al, 2010), while in vivo the flow is non turbulent and the Reynolds number range between 1 and 30 (Mudie et al, 2010), with maximum values between 35 and 100-125 when considering spikes due to high flow (Diebold, 2005). At 50 rpm the USP2 apparatus produces maximum velocities between 0.049 and 0.067 m/s (D'Arcy et al, 2005), while the USP1 apparatus has shown to have maximum velocities generally lower than the USP2 apparatus at the same rotational speed and with a maximum value of 0.026 m/s (D'Arcy et al, 2009).…”

Section: Resultsmentioning

confidence: 99%

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An in vitro–in vivo correlation study for nifedipine immediate release capsules administered with water, alcoholic and non-alcoholic beverages: Impact of in vitro dissolution media and hydrodynamics

Mercuri

Fares

Bresciani

et al. 2016

International Journal of Pharmaceutics

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The impact of hydrodynamics and media composition on nifedipine dissolution profile from IR (immediate release) soft capsules was investigated using dissolution apparatus USP1, USP2, USP3 and USP4 (United State Pharmacopoeia). Media composition was varied in terms of pH and content, to mimic the dosage form intake with water or non-alcoholic beverages (orange juice) and alcoholic beverages (orange juice/ethanol mixture (47% v/v)). Through construction of in vitro-in vivo correlations (IVIVC) with corresponding in vivo data from the literature, it was possible to evaluate the in vitro conditions that are likely to simulate the in vivo formulation behaviour. Both linear and nonlinear correlations were obtained depending on experimental set-ups. Testing of 20mg nifedipine capsules in FaSSGFst (Fasted State Simulated Gastric Fluid pH 1.6; water administration) produced IVIVC with the USP3 (after time scaling) and USP4 apparatus. IVIVC were obtained for USP2, USP3 and USP4 in FaSSGFoj (Fasted State Simulated Gastric Fluid pH 3.4; orange juice administration). Linear and nonlinear correlations were obtained with the USP1, USP2 and USP3 apparatus when testing the capsules in FaSSGFoj/EtOH (orange juice/ethanol administration). This study highlighted that selection of physiologically relevant dissolution set-ups is critical for predicting the in vivo impact of formulations co-administration with water, non-alcoholic and alcoholic beverages.

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Section: Resultsmentioning

confidence: 90%

Section: Resultsmentioning

confidence: 99%

An in vitro–in vivo correlation study for nifedipine immediate release capsules administered with water, alcoholic and non-alcoholic beverages: Impact of in vitro dissolution media and hydrodynamics

Mercuri

Fares

Bresciani

et al. 2016

International Journal of Pharmaceutics

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“…In most cases, compendial hydrodynamics are such that simulation of lumenal linear flow rates, [68] Reynolds number in the lumen, [69] lumenal volumes [55] and/or radial disappearance of API, due to the absorption via the mucosa, is inadequate. Based on various successful predictions of formulation and food effects on plasma levels by using compendial setups, it may be argued, that lumenal composition is more important than lumenal hydrodynamics for the dissolution of immediate release dosage forms and for the drug release from certain extended release dosage forms.…”

Section: Evaluation Of Dosage Form Related Processes With Biorelevantmentioning

confidence: 99%

“…Unlike with the USP 2 apparatus, the USP 3 or USP 4 apparatus may be used without modelling for evaluating Table 6 Composition and physicochemical characteristics of fed state simulating intestinal fluids [29] Early lumenal performance of extended release products, especially when attention is given to the application of biorelevant flow rates. [30,57,65] In most cases, compendial hydrodynamics are such that simulation of lumenal linear flow rates, [68] Reynolds number in the lumen, [69] lumenal volumes [55] and/or radial disappearance of API, due to the absorption via the mucosa, is inadequate. Based on various successful predictions of formulation and food effects on plasma levels by using compendial setups, it may be argued, that lumenal composition is more important than lumenal hydrodynamics for the dissolution of immediate release dosage forms and for the drug release from certain extended release dosage forms.…”

Section: Evaluation Of Dosage Form Related Processes With Biorelevantmentioning

confidence: 99%

Biorelevant in-vitro performance testing of orally administered dosage forms

Reppas

2012

Journal of Pharmacy and Pharmacology

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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%

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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Physiological Parameters Relevant to Dissolution Testing

Cited by 12 publications

References 53 publications

An in vitro–in vivo correlation study for nifedipine immediate release capsules administered with water, alcoholic and non-alcoholic beverages: Impact of in vitro dissolution media and hydrodynamics

An in vitro–in vivo correlation study for nifedipine immediate release capsules administered with water, alcoholic and non-alcoholic beverages: Impact of in vitro dissolution media and hydrodynamics

Biorelevant in-vitro performance testing of orally administered dosage forms

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

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