Design space and critical points in solid dosage forms

Aguilar-de-Leyva, Ángela; Campiñez, María Dolores; Casas, Marta; Caraballo, Isidoro

doi:10.1016/j.jddst.2017.06.004

Cited by 8 publications

(5 citation statements)

References 54 publications

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“…On the basis of percolation theory, pharmaceutical systems can be described as randomly distributed materials where geometrical phase transitions can occur [22,23]. When a component reaches its percolation threshold, it starts to extend over the whole sample, having much greater influence on the properties of the system.…”

Section: Resultsmentioning

confidence: 99%

Achieving High Excipient Efficiency with Elastic Thermoplastic Polyurethane by Ultrasound Assisted Direct Compression

2019

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Ultrasound assisted compression (USAC) is a manufacturing technique which applies thermal and mechanical energy to the powder bed, producing tablets with improved characteristics compared to the direct compression process. This technology is ideal for thermoplastic materials, as polyurethanes, whose particles usually undergo a sintering process. Thermoplastic polyurethanes are widely used in sustained drug release systems but rarely seen in tablets due to their elastic properties. The aim of this work is to investigate the ability of USAC to manufacture sustained release matrix tablets based on elastic thermoplastic polyurethanes (TPU), overcoming the limitations of direct compression. The technological and biopharmaceutical characteristics of the TPU matrices have been evaluated, with special focus on the porous structure due to the implications on drug release. For the first time, USAC has been successfully employed for manufacturing elastic thermoplastic polyurethanes-based matrices. TPU tablets show an inert character with a sustained drug release governed by a diffusional mechanism. Initial porosity of matrices was similar in all batches studied, with no influence of drug particle size, and a fractal nature of the pore network has been observed. SEM microphotographs show the continuum medium created by the sintering of the polymer, responsible for the high excipient efficiency.

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Section: Resultsmentioning

confidence: 99%

Achieving High Excipient Efficiency with Elastic Thermoplastic Polyurethane by Ultrasound Assisted Direct Compression

2019

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“…Critical points related to properties such as drug release and mechanical characteristics, among others, have been found in solid dosage forms [36][37][38][39]. To evaluate the behaviour, critical points, and thresholds of the blends in the extrusion process, some parameters summarized in Tables 3 and 4 have been studied.…”

Section: Blend Behaviour In the Extrusion Processmentioning

confidence: 99%

Assessment of the Extrusion Process and Printability of Suspension-Type Drug-Loaded AffinisolTM Filaments for 3D Printing

et al. 2022

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Three-dimensional (3D) printing technology enables the design of new drug delivery systems for personalised medicine. Polymers that can be molten are needed to obtain extruded filaments for Fused Deposition Modelling (FDM), one of the most frequently employed techniques for 3D printing. The aim of this work was to evaluate the extrusion process and the physical appearance of filaments made of a hydrophilic polymer and a non-molten model drug. Metformin was used as model drug and Affinisol™ 15LV as the main carrier. Drug-loaded filaments were obtained by using a single-screw extruder and, subsequently, their printability was tested. Blends containing up to a 60% and 50% drug load with 5% and 7.5% of auxiliary excipients, respectively, were successfully extruded. Between the obtained filaments, those containing up to 50% of the drug were suitable for use in FDM 3D printing. The studied parameters, including residence time, flow speed, brittleness, and fractal dimension, reflect a critical point in the extrusion process at between 30–40% drug load. This finding could be essential for understanding the behaviour of filaments containing a non-molten component.

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“…Hydrophilic matrices are monolithic systems of a matrix containing one or more hydrophilic excipients and an active pharmaceutical ingredient [1]. From a practical aspect, a direct compression hydrophilic matrix tablet is one of the simplest ways of developing an oral extended-release dosage form.…”

Section: Introductionmentioning

confidence: 99%

“…This phenomenon corresponds to the combined effect of diffusion with polymer relaxation and/or matrix erosion [9]. In combination with the expansion of the gel layer, other phenomena and characteristics such as matrix erosion, the internal structure of the matrix, and matrix porosity determine the release behavior of the drug from the hydrophilic matrix [1,4,10]. The interplay of hydration, gelling, swelling, erosion, and maybe even the final breakup of the dosage form (Scheme 1) can cause drug release from a hydrophilic matrix tablet [11].…”

Section: Introductionmentioning

confidence: 99%

“…In the development of drug delivery technology, the study of hydrophilic polymers has received considerable attention. The hydrophilic matrix's performance depends on the polymer type and viscosity grade, the presence of certain excipients, and even on factors associated with the material manufacturing, such as porosity [1,2,15]. Numerous researchers have studied the effects of different viscosity grades and degrees of substitution of HPMC on the compaction properties and drug release behavior of matrices [15][16][17][18].…”

Section: Introductionmentioning

confidence: 99%

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Drug-Polymers Composite Matrix Tablets: Effect of Hydroxypropyl Methylcellulose (HPMC) K-Series on Porosity, Compatibility, and Release Behavior of the Tablet Containing a BCS Class I Drug

Hirun

Kraisit

2022

Polymers

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The purpose of this research was to see how the physicochemical properties and porosity of matrix tablets containing various types of hydroxypropyl methylcellulose (HPMC) K series affected the release of propranolol hydrochloride (PNL). PNL is a class I drug (high solubility and permeability) according to the Biopharmaceutics Classification System (BCS), making it an excellent model drug used for studying extended-release drug products. The direct compression method was used to prepare the HPMC-based matrix tablets. PNL and the excipients were found to be compatible using Fourier transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), and differential scanning calorimetry (DSC). The surfaces of all the compressed HPMC-based matrix tablets were rough, with accumulated particles and small holes. The compressed HPMC-based matrix tablet porosity was also determined by using mercury porosimetry. The compressed HPMC-based matrix tablets made of low viscosity HPMC had tiny pores (diameter < 0.01 μm). The shorter polymeric chains are more prone to deformation, resulting in a small pore proportion. The compressed HPMC-based matrix tablets sustained the release of PNL for over 12 h. The release exponent values (n), which reflect the release mechanism of the drug from the tablets, ranged from 0.476 to 0.497. These values indicated that the release was governed by anomalous transport. The compressed HPMC-based matrix tablets have the potential for a sustained release of PNL.

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Design space and critical points in solid dosage forms

Cited by 8 publications

References 54 publications

Achieving High Excipient Efficiency with Elastic Thermoplastic Polyurethane by Ultrasound Assisted Direct Compression

Achieving High Excipient Efficiency with Elastic Thermoplastic Polyurethane by Ultrasound Assisted Direct Compression

Assessment of the Extrusion Process and Printability of Suspension-Type Drug-Loaded AffinisolTM Filaments for 3D Printing

Drug-Polymers Composite Matrix Tablets: Effect of Hydroxypropyl Methylcellulose (HPMC) K-Series on Porosity, Compatibility, and Release Behavior of the Tablet Containing a BCS Class I Drug

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