Hot stage extrusion of p-amino salicylic acid with EC using CO2 as a temporary plasticizer

Verreck, Geert; Decorte, Annelies; Heymans, Koen; Adriaensen, Jef; Liu, Dehua; Tomasko, David L.; Ariën, Albertina; Peeters, Jef; Mooter, Guy Van den; Brewster, Marcus E.

doi:10.1016/j.ijpharm.2006.07.024

Cited by 85 publications

(41 citation statements)

References 13 publications

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“…The property of porous structure extrudates has a very significant impact in drug release and milling process resulting in a very high milling efficiency compared to non-porous extrudates. Similar porous nature of the extrudates was observed by other research groups by using super critical CO 2 as plasticizer (14,15). In a study by Verreck and co-workers, super critical CO 2 was used as plasticizer in extruding Eudragit® E100, PVPVA 64, and ethyl cellulose which reduced the extrusion temperature by 15, 30, and 65°C.…”

Section: Effect Of Plasticizers On Hme Of Kldsupporting

confidence: 73%

Taste Masking of Griseofulvin and Caffeine Anhydrous Using Kleptose Linecaps DE17 by Hot Melt Extrusion

Juluri

Popescu²,

Zhou³

et al. 2015

AAPS PharmSciTech

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Abstract. The objective of this project was to investigate the potential of Kleptose Linecaps DE17 (KLD) in masking the unpleasant/bitter taste of therapeutic agents by hot melt extrusion (HME). Griseofulvin (GRI) and caffeine anhydrous (CA) were used as a bitter active pharmaceutical ingredient (API) model drugs. Thermogravimetric studies confirmed the stability of GRI, CA, and KLD at the employed extrusion temperatures. The differential scanning calorimetry (DSC) studies revealed a characteristic melting endotherm of GRI at 218-220°C and CA at 230-232°C in the physical mixtures as well as in all extrudates over the period of study, indicating the crystalline nature of drug. HME of KLD was achieved only in the presence of plasticizer. Among the several plasticizers investigated, xylitol showed improved processability of KLD at 15% w/w concentration. Dissolution studies of HME extrudates using simulated salivary medium exhibited ∼threefold less release compared to physical mixture at the end of 5 min (the lesser drug release, better the taste masking efficiency). Furthermore, the results from the sensory evaluation of products in human panel demonstrated strong bitter taste in the case of physical mixture compared to the HME formulation, suggesting the potential of Kleptose Linecaps DE17 as taste masking polymer in melt extruded form.

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Section: Effect Of Plasticizers On Hme Of Kldsupporting

confidence: 73%

Taste Masking of Griseofulvin and Caffeine Anhydrous Using Kleptose Linecaps DE17 by Hot Melt Extrusion

Juluri

Popescu²,

Zhou³

et al. 2015

AAPS PharmSciTech

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“…In both polymer systems, an increase in surface area and porosity was observed with CO 2 injection, resulting in an increased milling efficiency of the extrudate intermediate. The benefits of sc-CO 2 injection were further demonstrated in the extrusion of EC 20 cps with a thermally labile API, p-amino salicylic acid (p-ASA) (92). p-ASA substantially degrades above 120°C but is stable for at least 10 min at atmospheric conditions below 110°C.…”

Section: Temporary Plasticizers and Supercritical Technologymentioning

confidence: 99%

Challenges and Strategies in Thermal Processing of Amorphous Solid Dispersions: A Review

2015

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Abstract. Thermal processing of amorphous solid dispersions continues to gain interest in the pharmaceutical industry, as evident by several recently approved commercial products. Still, a number of pharmaceutical polymer carriers exhibit thermal or viscoelastic limitations in thermal processing, especially at smaller scales. Additionally, active pharmaceutical ingredients with high melting points and/or that are thermally labile present their own specific challenges. This review will outline a number of formulation and process-driven strategies to enable thermal processing of challenging compositions. These include the use of traditional plasticizers and surfactants, temporary plasticizers utilizing sub-or supercritical carbon dioxide, designer polymers tailored for hot-melt extrusion processing, and KinetiSol® Dispersing technology. Recent case studies of each strategy will be described along with potential benefits and limitations.

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“…Miller et al (2007) have demonstrated the ability of HME to act as an efficient dispersive process for aggregated, fine engineering particles to improve dissolution rate properties by enhancing particles' wettability [46]. A very interesting investigation of Verreck and co-workers (2006) [47] determined the use of supercritical carbon dioxide (scCO2) as a temporary plasticiser during the manufacture of ethylcellulose through HME. A significant reduction in the processing temperature was achieved using scCO2 without any disadvantageous effects on the extrudate.…”

Section: Formulation Research and Developments To Datesmentioning

confidence: 99%

Hot-Melt Extrusion (HME): From Process to Pharmaceutical Applications

Maniruzzaman¹,

Douroumis²,

Boateng³

et al. 2012

Recent Advances in Novel Drug Carrier Systems

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Hot stage extrusion of p-amino salicylic acid with EC using CO2 as a temporary plasticizer

Cited by 85 publications

References 13 publications

Taste Masking of Griseofulvin and Caffeine Anhydrous Using Kleptose Linecaps DE17 by Hot Melt Extrusion

Taste Masking of Griseofulvin and Caffeine Anhydrous Using Kleptose Linecaps DE17 by Hot Melt Extrusion

Challenges and Strategies in Thermal Processing of Amorphous Solid Dispersions: A Review

Hot-Melt Extrusion (HME): From Process to Pharmaceutical Applications

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