Ball milling and hot-melt extrusion of indomethacin–L-arginine–vinylpyrrolidone-vinyl acetate copolymer: Solid-state properties and dissolution performance

2021 ◽  
pp. 121424
Author(s):  
Anton Iemtsev ◽  
Alžběta Zemánková ◽  
Fatima Hassouna ◽  
Alex Mathers ◽  
Martin Klajmon ◽  
...  
Keyword(s):  
Solid State ◽  
Ball Milling ◽  
Vinyl Acetate ◽  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
Hot Melt ◽  
Acetate Copolymer

Ethylene vinyl acetate as matrix for oral sustained release dosage forms produced via hot-melt extrusion

2011 ◽  
Vol 77 (2) ◽  
pp. 297-305 ◽  
Author(s):  
A. Almeida ◽  
S. Possemiers ◽  
M.N. Boone ◽  
T. De Beer ◽  
T. Quinten ◽  
...  
Keyword(s):  
Sustained Release ◽  
Vinyl Acetate ◽  
Ethylene Vinyl Acetate ◽  
Hot Melt Extrusion ◽  
Dosage Forms ◽  
Melt Extrusion ◽  
Hot Melt

scholarly journals Miscibility and thermal properties of poly(vinylpyrrolidone-vinyl acetate)/lamivudine and tenofovir binary blends prepared by hot melt extrusion

2021 ◽  
Vol 10 (3) ◽  
pp. 109-116
Author(s):  
Marcos L Dias ◽  
Lucyenne S Barbosa ◽  
Rodrigo B Anjos ◽  
Adriana PD Baptista ◽  
Fabio ML Dantas
Keyword(s):  
Vinyl Acetate ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
High Concentration ◽  
Binary Blends ◽  
Pharmaceutical Ingredients ◽  
Immunodeficiency Syndrome ◽  
Hot Melt

Preparation of amorphous solid dispersions (ASD) by hot melt extrusion (HME) of poly(vinylpyrrolidone-vinyl acetate) (Kollidon) and the active pharmaceutical ingredients (API) Lamivudine (3TC) and Tenofovir Disoproxyl Fumarate (TDF) was investigated aiming to study their miscibility and thermal behavior. These two drugs are currently used as drugs in first line treatment of patients with Acquired Immunodeficiency Syndrome (AIDS). In order to predetermine parameters for extrusion and the maximum concentration of API to be used without any recrystallization, binary blends were first processed in the mixing chamber at 130°C using a roller type rotor at 10, 20 and 30 rpm for 7 min, giving rise to ASD of both API, at least up to 20 wt% of the drug. Both 3TC and TDF were then extruded individually with Kollidon in a single screw extruder. HME produced ASD with high concentration of both Kollidon/API combinations, being part of the API soluble in the polymer matrix. From HME, Kollidon/3TC forms ASD in concentration up to 50 wt%, but from 30 wt% 3TC, the ASD has no time stability, showing recrystallization in less than 5 months, while the Kollidon/TDF system forms ASD up to 30 wt% of TDF, but it has aging stability inferior to 4 months.

scholarly journals Enhanced solid-state stability of amorphous ibrutinib formulations prepared by hot-melt extrusion

2020 ◽  
Vol 579 ◽  
pp. 119156 ◽  
Author(s):  
Marta F. Simões ◽  
Bernardo A. Nogueira ◽  
Andreia M. Tabanez ◽  
Rui Fausto ◽  
Rui M.A. Pinto ◽  
...  
Keyword(s):  
Solid State ◽  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
Solid State Stability ◽  
Hot Melt

Selection of Solid-State Plasticizers as Processing Aids for Hot-Melt Extrusion

2018 ◽  
Vol 107 (1) ◽  
pp. 372-379 ◽  
Author(s):  
Dipen Desai ◽  
Harpreet Sandhu ◽  
Navnit Shah ◽  
Waseem Malick ◽  
Hossein Zia ◽  
...  
Keyword(s):  
Solid State ◽  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
Hot Melt ◽  
Processing Aids ◽  
Selection Of

scholarly journals Opportunities for Successful Stabilization of Poor Glass-Forming Drugs: A Stability-Based Comparison of Mesoporous Silica Versus Hot Melt Extrusion Technologies

Pharmaceutics ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 577 ◽  
Author(s):  
Felix Ditzinger ◽  
Daniel J. Price ◽  
Anita Nair ◽  
Johanna Becker-Baldus ◽  
Clemens Glaubitz ◽  
...  
Keyword(s):  
Solid State ◽  
Mesoporous Silica ◽  
Oral Absorption ◽  
Hot Melt Extrusion ◽  
Resonance Spectroscopy ◽  
Melt Extrusion ◽  
Pharmaceutical Ingredients ◽  
Poorly Soluble ◽  
Co Precipitation ◽  
Hot Melt

Amorphous formulation technologies to improve oral absorption of poorly soluble active pharmaceutical ingredients (APIs) have become increasingly prevalent. Currently, polymer-based amorphous formulations manufactured by spray drying, hot melt extrusion (HME), or co-precipitation are most common. However, these technologies have challenges in terms of the successful stabilization of poor glass former compounds in the amorphous form. An alternative approach is mesoporous silica, which stabilizes APIs in non-crystalline form via molecular adsorption inside nano-scale pores. In line with these considerations, two poor glass formers, haloperidol and carbamazepine, were formulated as polymer-based solid dispersion via HME and with mesoporous silica, and their stability was compared under accelerated conditions. Changes were monitored over three months with respect to solid-state form and dissolution. The results were supported by solid-state nuclear magnetic resonance spectroscopy (SS-NMR) and scanning electron microscopy (SEM). It was demonstrated that mesoporous silica was more successful than HME in the stabilization of the selected poor glass formers. While both drugs remained non-crystalline during the study using mesoporous silica, polymer-based HME formulations showed recrystallization after one week. Thus, mesoporous silica represents an attractive technology to extend the formulation toolbox to poorly soluble poor glass formers.

scholarly journals Solid state thermomechanical engineering of high-quality pharmaceutical salts via solvent free continuous processing

2020 ◽  
Vol 22 (2) ◽  
pp. 540-549 ◽  
Author(s):  
Md Sadeque Hossain Mithu ◽  
Steven A. Ross ◽  
Bruce D. Alexander ◽  
Dennis Douroumis
Keyword(s):  
Solid State ◽  
Hot Melt Extrusion ◽  
Solvent Free ◽  
Continuous Processing ◽  
Melt Extrusion ◽  
High Quality ◽  
Pharmaceutical Salts ◽  
Hot Melt

Solvent-free, continuous processing of high-quality pharmaceutical salts through via hot-melt extrusion as an alternative to solvent based approaches.

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