Effect of ionic strength and pH of dissolution media on theophylline release from hypromellose matrix tablets—Apparatus USP III, simulated fasted and fed conditions

Asare-Addo, Kofi; Levina, Marina; Rajabi‐Siahboomi, Ali R.; Nokhodchi, Ali

doi:10.1016/j.carbpol.2011.04.014

Cited by 47 publications

(31 citation statements)

References 33 publications

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“…The varying ionic strengths were likened to low salt content and high salt content of food. K100M HPMC tablet matrices had the lowest drug release rate for all three model drugs and produced a strong gel layer suggesting high viscosity grades to perhaps be the best candidates for producing controlled release profiles that are less affected by food [7].…”

Section: Numerous Other In-vitromentioning

confidence: 99%

“…These two proper-ties vary greatly along the GI tract under fasted and fed conditions [91,95,166]. These factors may affect the rate at which a drug is released from its hydrophilic gel matrix [6][7][8][9][10]165,167,168].…”

Section: Numerous Other In-vitromentioning

confidence: 99%

“…This review looks to summarise the physiological parameters that can affect drug release, discuss food effect on drug release and some of the dissolution methods used in trying to predict in vivo dissolution behaviour. This review will also look at a simple in vitro methodology developed by Asare-Addo et al by varying agitation in ascending and descending sequences as a systematic process for potentially discriminating fasted and fed states to represent the various levels of agitation to mimic the fed and fasted states in man [6][7][8][9][10].…”

Section: Introductionmentioning

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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Section: Numerous Other In-vitromentioning

confidence: 99%

Section: Numerous Other In-vitromentioning

confidence: 99%

Section: Introductionmentioning

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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“…In order to mimic the fasted state, this time may be increased to 4 hours, followed by 1 hour of agitation in the second line. In both cases, the appropriate agitation period in other lines must be selected depending on the type of product to be analyzed, compared to the drug delivery time, which may be from 8 to 24 hours (Yang, 2008;Asare-Addo et al, 2011).…”

Section: Simulation Of Fasted and Fed Statesmentioning

confidence: 99%

Applications of USP apparatus 3 in assessing the in vitro release of solid oral dosage forms

Pezzini

Issa

Duque

et al. 2015

Braz. J. Pharm. Sci.

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USP Apparatus 3 (reciprocating cylinder) is a very versatile device for the in vitro assessment of release characteristics of solid oral dosage forms, because it enables the product to be subjected to different dissolution media and agitation speeds in a single run. In this paper, a brief history and a description of this system are presented, along with its applications in the development of immediate and modified release products and in the simulation of fasted and fed states using biorelevant media. Furthermore, a comparison is made with the basket and paddle apparatus, especially highlighting the superior hydrodynamics of USP apparatus 3, since the results are not sensitive to factors such as the presence of sample collection probes or air bubbles in the dissolution medium.Uniterms: Solid dosage forms/in vitro release. Solid dosage forms/dissolution. Apparatus 3/use/evaluation of solid dosage forms. Reciprocating cylinders.USP aparato 3 (cilindros recíprocos) é um equipamento bastante versátil para a avaliação das características de liberação in vitro de formas farmacêuticas sólidas orais, pois permite que o produto seja submetido a diferentes meios de dissolução e condições de agitação, em um único ensaio. Neste trabalho, são apresentados um breve histórico e a descrição desse sistema, suas aplicações no desenvolvimento de produtos de liberação imediata e modificada, assim como sua utilização na simulação dos estados não alimentado e alimentado com o emprego de meios biorrelevantes. Além disso, uma comparação é estabelecida com o cesto e a pá, com destaque para a hidrodinâmica superior do USP aparato 3, que faz com que os resultados não sejam influenciados por fatores como o uso de sondas de coleta de amostras ou presença de bolhas de ar no meio de dissolução.Unitermos: Formas farmacêuticas sólidas/liberação in vitro. Formas farmacêuticas sólidas/dissolução. USP Aparato 3/uso/avaliação de formas farmacêuticas sólidas. Cilindros recíprocos.

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“…[49] In this study the flat faced 4 mm mini tablets with a target weight of 20 mg were compacted at 2000 psi (7.65 kN). Due to the poor compactability of psyllium's mini tablets, a mixture of 50 % psyllium and 50 % HPMC was utilised.…”

Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 99%

Psyllium: a promising polymer for sustained release formulations in combination with HPMC polymers

Kaialy

Emami

Asare-Addo

et al. 2013

Pharmaceutical Development and Technology

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Psyllium has a mucilaginous property that makes it a good candidate to be utilized as an excipient in the preparation of controlled release systems. Various formulations were prepared using theophylline as a model drug and investigated with view to achieve an ideal slow drug release profile. The addition of HPMC to psyllium significantly reduced burst release however the percentage of drug release within a 12 h period was too slow and thereby inadequate. This was overcome by the addition of lactose as hydrophilic filler which enabled a slow release with roughly 80% drug release in 12 h. The inclusion of HPMC within psyllium formulations changed the drug release kinetics from Fickian diffusion to anomalous transport. Granulated formulations demonstrated slower drug release than ungranulated or physical mixture and caused a change in dissolution kinetics from Fickian diffusion to anomalous transport. Milled granules showed more efficient controlled drug release with no burst release. Milling of the granules also changed the drug release kinetics to anomalous transport. Although, psyllium was proved to be a promising polymer to control the drug release, a combination of psyllium-HPMC and formulation processes should be considered in an attempt to achieve a zero-order release.

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Effect of ionic strength and pH of dissolution media on theophylline release from hypromellose matrix tablets—Apparatus USP III, simulated fasted and fed conditions

Cited by 47 publications

References 33 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

Applications of USP apparatus 3 in assessing the in vitro release of solid oral dosage forms

Psyllium: a promising polymer for sustained release formulations in combination with HPMC polymers

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