Coated formulations: New insights into the release mechanism and changes in the film properties with a novel release cell

Marucci, Mariagrazia; Hjärtstam, Johan; Ragnarsson, Gert; Iselau, Frida; Axelsson, Anders

doi:10.1016/j.jconrel.2009.02.017

Cited by 49 publications

(58 citation statements)

References 22 publications

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“…Polymer blends have been used to design controlled-release coatings for solid oral dosage forms. Blending hydrophobic and hydrophilic polymers has proven effective, with the hydrophilic polymer component forming pores upon hydration (30,31,55,85). A similar approach has been demonstrated for topical polymeric films as well, to achieve a wide range of release rates and also, in some cases, a different release mechanism (10,76,77,86,87).…”

Section: Film-forming Polymersmentioning

confidence: 99%

The potential of polymeric film-forming systems as sustained delivery platforms for topical drugs

Frederiksen

Guy

Petersson

2015

Expert Opinion on Drug Delivery

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The promise of polymeric FFS as convenient and aesthetic platforms for sustained topical drug delivery is clear. Manipulation of the formulation allows the delivery profile to be customized and optimized to take advantage of both a rapid, initial input of drug into the skin (likely due to a transient period of supersaturation) and a slower, controlled release over an extended time from the residual film created thereafter.

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Section: Film-forming Polymersmentioning

confidence: 99%

The potential of polymeric film-forming systems as sustained delivery platforms for topical drugs

Frederiksen

Guy

Petersson

2015

Expert Opinion on Drug Delivery

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“…The EC/HPC material has previously been studied experimentally in Marucci et al . (, ); Andersson et al . () and characterized statistically in Häbel et al .…”

Section: Methodsmentioning

confidence: 98%

“…More details about the preparation and imaging of these films can be found in Häbel et al (2017). The EC/HPC material has previously been studied experimentally in Marucci et al (2009Marucci et al ( , 2013; Andersson et al (2013) and characterized statistically in Häbel et al (2016Häbel et al ( , 2017. The mass transport properties of the material have been investigated using numerically calculated diffusion in Gebäck et al (2015).…”

Section: Clsm Images Of Porous Ec/hpc Polymer Filmsmentioning

confidence: 99%

A three‐dimensional statistical model for imaged microstructures of porous polymer films

Barman

Bolin

2017

Journal of Microscopy

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A thresholded Gaussian random field model is developed for the microstructure of porous materials. Defining the random field as a solution to stochastic partial differential equation allows for flexible modelling of nonstationarities in the material and facilitates computationally efficient methods for simulation and model fitting. A Markov Chain Monte Carlo algorithm is developed and used to fit the model to three-dimensional confocal laser scanning microscopy images. The methods are applied to study a porous ethylcellulose/hydroxypropylcellulose polymer blend that is used as a coating to control drug release from pharmaceutical tablets. The aim is to investigate how mass transport through the material depends on the microstructure. We derive a number of goodness-of-fit measures based on numerically calculated diffusion through the material. These are used in combination with measures that characterize the geometry of the pore structure to assess model fit. The model is found to fit stationary parts of the material well.

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“…The lag phase was more than 1 h at the 37.5~50% coating levels. The films were initially not permeable to the drug investigated, indicating that the lag phase was determined by the time of pore forming in the film due to HPC leaching and that the drug was released mainly through the water-filled pores (43).…”

Section: Effect Of Pore Former Types On Drug Release (Hpc Vs Ms)mentioning

confidence: 99%

Model Drug as Pore Former for Controlled Release of Water-Soluble Metoprolol Succinate from Ethylcellulose-Coated Pellets Without Lag Phase: Opportunities and Challenges

Wang¹,

Dai²,

Chang

et al. 2014

AAPS PharmSciTech

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Abstract. The objective of the present study was to evaluate the feasibility of using model drug metoprolol succinate (MS) as a pore former to modify the initial lag phase (i.e., a slow or non-release phase in the first 1-2 h) associated with the drug release from coated pellets. MS-layered cores with high drug-layering efficiency (97% w/w) were first prepared by spraying a highly concentrated drug aqueous solution (60% w/w, 70°C) on non-pareils without using other binders. The presence of MS in ethylcellulose (EC) coating solution significantly improved the coating process by reducing pellets sticking, which often occurs during organic coating. There may be a maximum physical compatibility of MS with EC, and the physical state of the drug in the functional coating layer of EC/MS (80:20) was simultaneously crystalline and noncrystalline (amorphous or solid molecule solution). The lag phase associated with hydroxypropylcellulose (HPC) as a pore former was not observed when MS was used as a pore former. The drug release from EC/ MS-coated pellets was pH independent, inversely proportional to the coating levels, and directly related to the pore former levels. The functional coating layer with MS as a pore former was not completely stabilized without curing. Curing at 60°C for 1 day could substantially improve the stability of EC/MScoated pellets. The physical state of the drug in the free film of EC/MS (85:15) changed partially from amorphous to crystal when cured at 60°C for 1 day, which should be attributed to the incompatibility of the drug with EC.

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Coated formulations: New insights into the release mechanism and changes in the film properties with a novel release cell

Cited by 49 publications

References 22 publications

The potential of polymeric film-forming systems as sustained delivery platforms for topical drugs

The potential of polymeric film-forming systems as sustained delivery platforms for topical drugs

A three‐dimensional statistical model for imaged microstructures of porous polymer films

Model Drug as Pore Former for Controlled Release of Water-Soluble Metoprolol Succinate from Ethylcellulose-Coated Pellets Without Lag Phase: Opportunities and Challenges

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