Tableting of hot-melt coated paracetamol granules: Material tableting properties and quality characteristics of the obtained tablets

Milanovic, Ana; Aleksić, Ivana; Ibrić, Svetlana; Parojčić, Jelena; Cvijić, Sandra

doi:10.1016/j.ejps.2019.105121

Cited by 12 publications

(12 citation statements)

References 20 publications

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“…Examined tablets of all investigated formulations were characterized with very low ejection stress (0.09 to 0.26 MPa) in the considered compression pressure range. According to the literature, ejection stress should be lower than 3 MPa to prevent failure during tablet produc-tion [18,42]. Consequently, this result indicated that there was no need for the addition of a lubricant in any of the investigated formulations.…”

Section: Mechanical Propertiesmentioning

confidence: 69%

“…No lubricant was added before or during compression. For each phase of the tableting process (compression, detachment, and ejection) a force-displacement curve was generated by the instrument software, and the data were used to calculate the tensile strength, Equation (5); detachment stress, Equation (6); ejection stress, Equation ( 7) [18]. Tablet hardness and diameter were measured by using a hardness tester (Erweka ® TBH 125D, Erweka, Heusenstamm, Germany).…”

Section: Tablets Preparation and Determination Of Mechanical Propertiesmentioning

confidence: 99%

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Development of Lipid-Based Gastroretentive Delivery System for Gentian Extract by Double Emulsion–Melt Dispersion Technique

et al. 2021

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Gentian (Gentiana lutea L., Gentianaceae) root extract (GRE) is used for the treatment of gastrointestinal disorders. However, its bioactive potential is limited in conventional forms due to the low bioavailability and short elimination half-life of the dominant bioactive compound, gentiopicroside. The aim of study was to encapsulate GRE in the lipid-based gastroretentive delivery system that could provide high yield and encapsulation efficiency, as well as the biphasic release of gentiopicroside from the tablets obtained by direct compression. Solid lipid microparticles (SLM) loaded with GRE were prepared by freeze-drying double (W/O/W) emulsions, which were obtained by a multiple emulsion–melt dispersion technique, with GRE as the inner water phase, Gelucire® 39/01 or 43/01, as lipid components, with or without the addition of porous silica (Sylysia® 350) in the outer water phase. Formulated SLM powders were examined by SEM and mercury intrusion porosimetry, as well as by determination of yield, encapsulation efficiency, and flow properties. Furthermore, in vitro dissolution of gentiopicroside, the size of the dispersed systems, mechanical properties, and mucoadhesion of tablets obtained by direct compression were investigated. The results have revealed that SLM with the macroporous structure were formulated, and, consequently, the powders floated immediately in the acidic medium. Formulation with porous silica (Sylysia® 350) and Gelucire® 43/01 as a solid lipid was characterized with the high yield end encapsulation efficiency. Furthermore, the mucoadhesive properties of tablets obtained by direct compression of that formulation, as well as the biphasic release of gentiopicroside, presence of nanoassociates in dissolution medium, and optimal mechanical properties indicated that a promising lipid-based gastroretentive system for GRE was developed.

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Section: Mechanical Propertiesmentioning

confidence: 69%

Section: Tablets Preparation and Determination Of Mechanical Propertiesmentioning

confidence: 99%

Development of Lipid-Based Gastroretentive Delivery System for Gentian Extract by Double Emulsion–Melt Dispersion Technique

et al. 2021

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“…Use of meltable materials of controlled properties makes the HMC process well controllable 41 . The melt pelletization and melt granulation processes desires meltable materials having a high viscosity and a reduced particle size 42,43 .…”

Section: Hmc Using Fluid-bed Processormentioning

confidence: 99%

“…The melt pelletization and melt granulation processes desires meltable materials having a high viscosity and a reduced particle size 42,43 . High viscosity materials are desirous to improve mechanical strength of the coating but reduced particle size desirous to prevent rough surface of coating 2,3,41 .…”

Section: Hmc Using Fluid-bed Processormentioning

confidence: 99%

Dry-Coating of Powder Particles is Current Trend in Pharmaceutical Field

Alli¹

2021

J. Drug Delivery Ther.

608

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Modification of surface attributes of particles, usually accomplished by coating, is desirous to enhance and maintain their usability. Coating is a multi-step process involves application of the coating material (CoM) onto the substrate, herein powder particles, where the process along with device/ equipment monitors surface attributes of the applied coating. Nowadays competitive market calls for cost cutting to survive product(s). Thus saving of energy and time, minimising number and quantity of additives, reducing and shortening process steps; consequently minimising the coating process cost are main goals while developing coating process for powder particle. Innovation of processes for dry-powder coating (DPC) along with their further development and refinement finds solution to said issues. Further, DPC process does not calls for liquid solvent or solution thus are viewed as cost-effective and environmentally safe, DPC process uses thermo-mechanical methods like mechanofusion, magnetic assisted impaction coating (MAIC), hybridization, rotating fluid-bed process, theta-composer, hot-melt coating (HMC), and many others. Besides these available are non-thermo-mechanical methods namely electrostatic coating; supercritical fluids (SCF) based methods like rapid expansion of supercritical fluid (RESF), gas anti-solvent (GAS), SCF anti-solvent, gas-saturated solution (GSS); vapour coating; and others. Basing on said thermo-mechanical and non-thermo-mechanical principle several DPC methods/ process had been reported in scientific literatures and patents. Said DPC method founds multidisciplinary applications like drug delivery and drug development. Diverse devices are there for the DPC process; their method of working, principle, limitations and benefits along with their applicability in pharmaceutical field are discussed and presented in this article. Keywords: Dry, particle, coating, pharmaceutical, process

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“…Hot-melt blending has been widely used in the pharmaceutical industry to produce drug delivery systems, by virtue of the advantages such as solvent-free, continuous, and efficient processing [1][2][3]. Due to the easily tailored processing, different dosage forms including granules [4], pellets [5], tablets [6], and films [7] have been manufactured to meet various drug delivery requirements [8,9]. With the development of clinical medicine, a drug delivery system is often required to achieve controlled drug release in order to maintain a stable blood drug concentration, reduce the side effects of drugs, and achieve a high therapeutic effect.…”

Section: Introductionmentioning

confidence: 99%

Heat Treatment Induced Specified Aggregation Morphology of Metoprolol Tartrate in Poly(ε-caprolactone) Matrix and the Drug Release Variation

et al. 2021

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Hot-melt blending has been widely used in the pharmaceutical industry to produce drug delivery systems, however, realizing the controlled drug release behavior of a hot-melt blended medicament it is still a tough challenge. In this study, we developed a simple and effective heat treatment method to adjust the drug release behavior, without the addition of any release modifiers. Thin metoprolol tartrate (MPT)/poly(ε-caprolactone) (PCL) tablets were prepared through hot-melt processing, and different morphologies of MPT were obtained by altering processing temperatures and the following heat treatment. MPT particles with different particle sizes were obtained under different processing temperatures, and fibrous crystals of MPT were fabricated during the following heat treatment. Different morphological structures of MPT adjusted the drug diffusion channel when immersed in phosphate-buffered saline (PBS), and various drug release behaviors were approached. After being immersed for 24 h, 7% of the MPT was released from the blend processed at 130 °C, while more than 95% of the MPT were released after the following heat treatment of the same sample. Thus, flexible drug release behaviors were achieved using this simple and effective processing manufacture, which is demonstrated to be of profound importance for biomedical applications.

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Tableting of hot-melt coated paracetamol granules: Material tableting properties and quality characteristics of the obtained tablets

Cited by 12 publications

References 20 publications

Development of Lipid-Based Gastroretentive Delivery System for Gentian Extract by Double Emulsion–Melt Dispersion Technique

Development of Lipid-Based Gastroretentive Delivery System for Gentian Extract by Double Emulsion–Melt Dispersion Technique

Dry-Coating of Powder Particles is Current Trend in Pharmaceutical Field

Heat Treatment Induced Specified Aggregation Morphology of Metoprolol Tartrate in Poly(ε-caprolactone) Matrix and the Drug Release Variation

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