Translocation of drug particles in HPMC matrix gel layer: effect of drug solubility and influence on release rate

Bettini, Ruggero; Catellani, P. L.; Massimo, Gina; Peppas, Nicholas A.; Colombo, Paolo

doi:10.1016/s0168-3659(00)00366-7

Cited by 215 publications

(119 citation statements)

References 15 publications

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“…Dashed lines in Fig. 7 are the fronts observed in VIS photography (figure 3), The rates of all three visible fronts are consistent with earlier studies, in which a similar tablet composition was used, [6] which indicates that analyses of the newly developed tablet cell can well be compared to analyses focussing only on macro-photography. The solid lines in Fig.…”

Section: Ftir Imagingsupporting

confidence: 84%

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Simultaneous FTIR Spectroscopic Imaging and Visible Photography to Monitor Tablet Dissolution and Drug Release

Kazarian

Weerd

2007

Pharm Res

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A method to study tablet dissolution simultaneously by Fourier transform infraredattenuated total reflection (FTIR-ATR) imaging and macro-photography is described. Such a combined approach appeared important as the results of macro-photography, which have been provided by a number of authors, led to contradictory interpretations. The macro-photographs of a pharmaceutical tablet during exposure to water show a number of 'fronts' moving into the tablet. These fronts are obviously related to water penetration into and dissolution of the tablet, but the exact nature can not be derived from photographic evidence. Therefore, the combination of macro-photography and FTIR-ATR imaging was developed and used to interpret the physical changes leading to the observed fronts. The quantitative results obtained by FTIR-ATR imaging enabled the attribution of the three observed fronts (inside to outside) to: 1. True water penetration, possibly combined with (partial) dissolution of buflomedyl pyridoxal phosphate (BPP) 2. Total gellification of hydroxypropyl-methylcellulose (HPMC) 3. Erosion front IntroductionIn recent years, a number of new approaches has been reported to study the behaviour of pharmaceutical tablets during dissolution. These studies aim to generate an understanding of the processes in a dissolving tablet. This is a welcome addition to the standard dissolution tests, which obtain the amount of dissolved active ingredient as a function of time, but do not provide indications on the underlying mechanisms of tablet dissolution.

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Section: Ftir Imagingsupporting

confidence: 84%

“…The experimental set-ups, applied samples, and information content of the results are normally dissimilar, and some aspects will be described below. [5][6][7][8][9] Fluorescence imaging…”

Section: Introductionmentioning

confidence: 99%

Simultaneous FTIR Spectroscopic Imaging and Visible Photography to Monitor Tablet Dissolution and Drug Release

Kazarian

Weerd

2007

Pharm Res

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“…Other factors which may also affect the rate at which a drug is released from its hydrophilic gel matrix may include the formulation composition [105-108], the physiochemical properties of the drug and polymer [109][110][111][112][113][114] and the processing and compaction conditions [115][116][117]. All these factors can influence the choice of the polymer viscosity and chemistry used.…”

Section: Effect Of Food On Drug Relelasementioning

confidence: 99%

“…Factors that can affect the properties of the gel layer include the physiochemical properties of the drug and polymer, formulation composition, processing conditions and the environmental variables such as the characteristics of the GI fluids [106][107][108][109][110]114,115,165,166]. Two major properties of the GI fluids are ionic strength and pH [91,95,166].…”

Section: Numerous Other In-vitromentioning

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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“…During hydration of HPMC a gel layer is formed around the dry core of polymer and swelling of polymer occurs. Drug is then released via pure diffusion or a diffusion-erosion controlled mechanism, where the ratio and properties of the active drug, HPMC and other excipients as well as the composition of fluids and the hydrodynamics in the gastrointestinal tract will determine the detailed release profile [7][8][9][10] . Figure 4 shows the intragastric release behavior of two commercially available HPMC-based tablet formulations containing an anti-asthmatic drug.…”

Section: Cellulose Ethersmentioning

confidence: 99%

Polysaccharides in Oral Drug Delivery — Recent Applications and Future Perspectives

Klein

2009

Polysaccharide Materials: Performance by Design

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Translocation of drug particles in HPMC matrix gel layer: effect of drug solubility and influence on release rate

Cited by 215 publications

References 15 publications

Simultaneous FTIR Spectroscopic Imaging and Visible Photography to Monitor Tablet Dissolution and Drug Release

Simultaneous FTIR Spectroscopic Imaging and Visible Photography to Monitor Tablet Dissolution and Drug Release

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

Polysaccharides in Oral Drug Delivery — Recent Applications and Future Perspectives

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