Influence of compression at elevated temperature on the compactibility of thermo-mechanically processed polymers

Partheniadis, Ioannis; Karantzalis, A. E.; Shah, Rumit R.; Al-Zoubi, Nizar; Nikolakakis, Ioannis

doi:10.1016/j.cherd.2020.01.035

Cited by 10 publications

(11 citation statements)

References 25 publications

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“…The use of plasticizers is a trend in the production of drug delivery systems by HME and 3D printing, where its addition to the formulation can decrease the T g and the processing temperature of the polymers, helping in the maintenance of drug stability [96]. According to the reports discussed in this review, examples of this type of excipient are triethyl citrate [111,134,146], propylene glycol [109], citric acid monohydrate and Lutrol F127 [115], stearic acid, glyceryl behenate and polyethylene glycol 8000 [103], polyethylene glycol 2000, Poloxamer 188, and Cremophor RH [56].…”

Section: Final Remarks and Challengesmentioning

confidence: 99%

“…In a different approach, Partheniadis et al (2020) compressed extrudates produced with ERS or EL100-55, without any drug, at an ambient (20 °C) or elevated (40 °C) temperature. The use of hot compression was reported as an option to improve the tabletability of the materials after extrusion [ 96 ]. Besides compression, other techniques have been used to prepare tablets from formulations produced by HME.…”

Section: Hot Melt Extrusionmentioning

confidence: 99%

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Eudragit®: A Versatile Family of Polymers for Hot Melt Extrusion and 3D Printing Processes in Pharmaceutics

et al. 2021

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Eudragit® polymers are polymethacrylates highly used in pharmaceutics for the development of modified drug delivery systems. They are widely known due to their versatility with regards to chemical composition, solubility, and swelling properties. Moreover, Eudragit polymers are thermoplastic, and their use has been boosted in some production processes, such as hot melt extrusion (HME) and fused deposition modelling 3D printing, among other 3D printing techniques. Therefore, this review covers the studies using Eudragit polymers in the development of drug delivery systems produced by HME and 3D printing techniques over the last 10 years. Eudragit E has been the most used among them, mostly to formulate immediate release systems or as a taste-masker agent. On the other hand, Eudragit RS and Eudragit L100-55 have mainly been used to produce controlled and delayed release systems, respectively. The use of Eudragit polymers in these processes has frequently been devoted to producing solid dispersions and/or to prepare filaments to be 3D printed in different dosage forms. In this review, we highlight the countless possibilities offered by Eudragit polymers in HME and 3D printing, whether alone or in blends, discussing their prominence in the development of innovative modified drug release systems.

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Section: Final Remarks and Challengesmentioning

confidence: 99%

Section: Hot Melt Extrusionmentioning

confidence: 99%

Eudragit®: A Versatile Family of Polymers for Hot Melt Extrusion and 3D Printing Processes in Pharmaceutics

et al. 2021

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“…32 The addition of 10% ethyl cellulose in F4 instead of PVP K30 in F1 also results in extending the dissolution rate as it's an insoluble polymer and has been used in the formulation of sustained-release dosage forms. 33 Dissolution profile of F4 in the four gastro-floating devices is shown in Figure 5. F4A started the release of the drug after 2 hr from the start of the experiment and this is due to the position of the drug releasing window where it was above the surface of the dissolution media when placed in the dissolution jar at the start of the experiment and after 2 hr the device flipped and the entry of the dissolution media into the hollow section of the device started and thus tablet dissolution started, this fact is considered a disadvantage of this device design although it can be used for altering the release profile into sustained release but it may be associated with an unintended lag time.…”

Section: Discussionmentioning

confidence: 99%

Development of Gastro-floating drug delivery system by 3D Printing: Impact of formulation and design on the release profile of Baclofen

Abdulkhaleq

Ghareeb

2022

J. Contemp. Med. Sci.

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Objectives: Baclofen is a skeletal muscle relaxant with a short half-life and a narrow absorption window in the upper part of the gastrointestinal tract, and this study aims to formulate a sustained-release tablet of baclofen and 3D printing of gastro-floating device and study the effect of various polymers and device design on the release profile of baclofen. Method: Firstly, four formulas were produced through the hot-melt extrusion and direct compression of the extrudate to produce 30 mg baclofen tablets, then four gastro-floating devices (A, B, C, and D) were designed with two air pockets to enable the floating of the device and have drug-releasing windows with total surface area 4, 10, 20, and 40 mm2 respectively, for drug release. 3D printing of the devices was done by an FDM printer and the tablets were inserted into each device and test it for drug release. Results: Decreasing the surface area of the drug releasing windows revealed a significant reduction in the dissolution of baclofen irrespective of the type of polymers and useful for sustained release formulation but may be associated with lag time. Devices with one and two releasing windows (Device B and C respectively) sometimes revealed similar dissolution profiles and this related to the position of the window regarding the surface of the dissolution media. Device D with four windows and a 40 mm2 surface area was found to produce more reliable results. F3 which contains Eudragit RS-100 as the main polymer showed sustained release in device D where the complete dissolution of the drug occurred in 12 hours, and the gastro-floating device remained floating all the time and was assayed for drug content, FT-IR, and DSC study. Conclusion: Hot-melt extrusion was successfully employed to produce sustained release tablets of baclofen. FDM 3D printers are considered a potential tool to produce gastro-floating devices with the required design and release profile.

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“…It is composed of roundish particles with an average diameter between 80 and 100 µm and good flowability (angle of repose < 30 • ) [126]. The glass transition temperature is low (around 40-45 • C) and thus deforms mainly plastically [127,128]. Several studies have demonstrated its suitability as a matrix former for sustaining drug release by direct compression tableting [128][129][130][131][132], and the release is independent of the compression force [131,133].…”

Section: Multifunctional Co-spray Dried Excipientsmentioning

confidence: 99%

Spray Drying for Direct Compression of Pharmaceuticals

et al. 2021

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Tableting by direct compression (DC) is one of the simplest and most cost-effective drug manufacturing approaches. However, most active pharmaceutical ingredients (APIs) and excipients lack the compression and flow properties required to meet the needs of high-speed industrial tablet presses. Therefore, the majority of DC APIs and excipients are modified via processing/co-processing particle engineering techniques to boost their properties. Spray drying is one of the most commonly employed techniques to prepare DC grades of APIs and excipients with prominent advantages. This review aims to present an overview of the commercially marketed and investigationally-prepared DC APIs and excipients produced by spray drying.

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Influence of compression at elevated temperature on the compactibility of thermo-mechanically processed polymers

Cited by 10 publications

References 25 publications

Eudragit®: A Versatile Family of Polymers for Hot Melt Extrusion and 3D Printing Processes in Pharmaceutics

Eudragit®: A Versatile Family of Polymers for Hot Melt Extrusion and 3D Printing Processes in Pharmaceutics

Development of Gastro-floating drug delivery system by 3D Printing: Impact of formulation and design on the release profile of Baclofen

Spray Drying for Direct Compression of Pharmaceuticals

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