The influence of thermal treatment and type of insoluble poly(meth)acrylates on dissolution behavior of very soluble drug from hypromellose matrix tablets evaluated by multivariate data analysis

Kubová, Kateřina; Pěček, Daniel; Hasserová, Kristýna; Doležel, Petr; Pavelková, Miroslava; Vysloužil, Jakub; Muselík, Jan; Vetchý, David

doi:10.1080/10837450.2016.1193191

Cited by 8 publications

(6 citation statements)

References 28 publications

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“…The procedure used proved to be a time- and energy-consuming process. Compared to our previous results, the levetiracetam/microcrystalline cellulose mixture (100g : 50g) was granulated under the same conditions by 27.7 g of all types of Eudragit® WD in 1-step and by 55.7 g of Eudragit® NE or NM in 1-step and RL or RS in 2-step process [30]. Even more Eudragit® NE WD (111.3 g) was applied on the levetiracetam/Neusilin® US2 mixture (100g : 100g) in our experimental study published by Naiserova et al [31].…”

Section: Resultsmentioning

confidence: 92%

“…It was concluded that there is no possibility of applying them directly in one-step process due to the creation of a highly sticky mass unsuitable for consequent processing. This problem was solved by the addition of insoluble filler such as MCC or Neusilin® US2 to create a drug/filler mixture [30, 31]. Nevertheless, the behavior of the highly soluble API directly granulated with water dispersions of insoluble Eudragit® polymers has not been published yet.…”

Section: Introductionmentioning

confidence: 99%

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Highly Soluble Drugs Directly Granulated by Water Dispersions of Insoluble Eudragit® Polymers as a Part of Hypromellose K100M Matrix Systems

Mašková

Naiserová

Kubová

et al. 2019

BioMed Research International

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The aim of the present study was to investigate the suitability of insoluble Eudragit® water dispersions (NE, NM, RL, and RS) for direct high-shear granulation of very soluble levetiracetam in order to decrease its burst effect from HPMC K100M matrices. The process characteristics, ss-NMR analysis, in vitro dissolution behavior, drug release mechanism and kinetics, texture profile analysis of the gel layer, and PCA analysis were explored. An application of water dispersions directly on levetiracetam was feasible only in a multistep process. All prepared formulations exhibited a 12-hour sustained release profile characterized by a reduced burst effect in a concentration-dependent manner. No effect on swelling extent of HPMC K100M was observed in the presence of Eudragit®. Contrary, higher rigidity of formed gel layer was observed using combination of HPMC and Eudragit®. Not only the type and concentration of Eudragit®, but also the presence of the surfactant in water dispersions played a key role in the dissolution characteristics. The dissolution profile close to zero-order kinetic was achieved from the sample containing levetiracetam directly granulated by the water dispersion of Eudragit® NE (5% of solid polymer per tablet) with a relatively high amount of surfactant nonoxynol 100 (1.5%). The initial burst release of drug was reduced to 8.04% in 30 min (a 64.2% decrease) while the total amount of the released drug was retained (97.02%).

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Section: Resultsmentioning

confidence: 92%

Section: Introductionmentioning

confidence: 99%

Highly Soluble Drugs Directly Granulated by Water Dispersions of Insoluble Eudragit® Polymers as a Part of Hypromellose K100M Matrix Systems

Mašková

Naiserová

Kubová

et al. 2019

BioMed Research International

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“…As renaissance, a polymer was modified chemically (Masina et al, 2017;Zayed et al, 2017) or physically (Hong et al, 2016) and blended with an appropriate polymer combination to obtain desired characteristics either physicochemical or physicomechanical properties for controlling the drug release. A novel polymer combination was applied for controlling the drug release by matrix system (Kubova et al, 2017). Drugs are usually incorporated into polymers in the oral controlled release formulations through either physical mixture as a matrix or amorphous solid dispersion (Ali et al, 2017;Ohyagi et al, 2017;Park et al, 2008).…”

Section: Introductionmentioning

confidence: 99%

Characterization of Eudragit types and Kollidon SR inter-polymer complexes and their effects on the drug release

2019

J App Pharm Sci

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A novel of polymer combination promotes an increase of the ability for controlling the drug release. The objective of this research was to characterize the inter-polymer complexes (IPCs) of Eudragit (Eud) types (Eud RS, Eud L, or Eud E) and Kollidon SR (KSR), and elucidate their effects on the drug release kinetics and mechanism. Different preparation techniques were proposed using spray drying and ultrasonic-assisted anti-solvent techniques. The thermal activity, e.g., glass transition temperature (T g ) and Fourier transform infrared spectroscopy were used to characterize the molecular interaction of these IPCs. Theophylline (THP) was selected as a drug model. The effect on the drug release kinetics and mechanism was the main concern of this study. Depending on the results, the hydrogen bonding formation between polymers was observed by a shifting of OH and carbonyl group vibrations. In addition, the van der Waals interaction was identified by an alteration in the vibrational band around the 1,000-1,500 cm −1 . Meanwhile, the change of physicochemical characteristic was identified by the T g of IPCs. Eud E-KSR and Eud E-Eud L IPC were unable to control the THP release. Meanwhile, Eud L-KSR IPC and Eud RS-KSR IPC were success to control the THP release, but it was pH dependent and independent, respectively. This study concluded that the IPCs allowed the THP release in a controlled manner based on the IPC characteristics and their interactions. Either positive or negative interactions on the drug release were observed due to native characteristics of polymers.

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“…The primary mechanism of drug release from hydrophilic matrices occurs when the polymer swells on contact with the aqueous medium to form a gel layer on the surface of the system. The drug then releases by dissolution, diffusion and/or erosion [10][11][12].…”

Section: Introductionmentioning

confidence: 99%

The Role of Matrix Tablet in Drug Delivery System

Mondal

2018

Int J App Pharm

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Matrix tablet is an important tool for controlled and sustained release dosage forms. The oral route remains the most common route for the administration of drugs. Tablets offer the lowest cost approach to sustained and controlled release dosage forms. The hydrophilic polymer matrix is widely used in this dosage form. The use of different polymers in controlling the release of drugs has become the most important tool in the formulation of matrix tablets. The drug releases by both dissolution-controlled as well as diffusion-controlled mechanisms from the matrix. The development of oral controlled release systems has been a challenge to formulation scientists due to their inability to restrain and localize the system at targeted areas of the gastrointestinal tract. There are several advantages of matrix devices including improved patient compliance due to less frequent drug administration, reduction of fluctuation in steady-state drug levels, maximum utilization of the drug, increased safety margin of a potent drug. This review aims on the discussion of different materials used to prepare matrix tablets, different types of matrix tablets and the drug release mechanism from the matrices.

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The influence of thermal treatment and type of insoluble poly(meth)acrylates on dissolution behavior of very soluble drug from hypromellose matrix tablets evaluated by multivariate data analysis

Cited by 8 publications

References 28 publications

Highly Soluble Drugs Directly Granulated by Water Dispersions of Insoluble Eudragit® Polymers as a Part of Hypromellose K100M Matrix Systems

Highly Soluble Drugs Directly Granulated by Water Dispersions of Insoluble Eudragit® Polymers as a Part of Hypromellose K100M Matrix Systems

Characterization of Eudragit types and Kollidon SR inter-polymer complexes and their effects on the drug release

The Role of Matrix Tablet in Drug Delivery System

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