The effect of pressurized carbon dioxide as a temporary plasticizer and foaming agent on the hot stage extrusion process and extrudate properties of solid dispersions of itraconazole with PVP-VA 64

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

doi:10.1016/j.ejps.2005.07.006

Cited by 87 publications

(51 citation statements)

References 15 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: 51%

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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: 51%

“…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. It was further observed that the extrudates were foamy in nature which subsequently improved milling (15).…”

Section: Effect Of Plasticizers On Hme Of Kldmentioning

confidence: 94%

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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show abstract

“…[38,39] The application window of hot-stage extrusion has been broadened by using sub-or supercritical carbon dioxide as a temporary plasticizer, allowing thermolabile drug-polymer blends to be extruded at lower temperatures. [40][41][42][43] A detailed review on the pharmaceutical applications of techniques using supercritical fluids is given by Pasquali et al [44] Classification A physicochemical classification of solid dispersions was first introduced by Chiou and Riegelman. [5] This classification included simple eutectic mixtures, solid solutions and glass solutions.…”

Section: Non-conventional Methods For Solid Dispersion Manufacturingmentioning

confidence: 99%

Review: physical chemistry of solid dispersions

2009

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Objectives With poorly soluble drug candidates emerging in the drug discovery pipeline, the importance of the solid dispersion formulation approach is increasing. This strategy includes complete removal of drug crystallinity, and molecular dispersion of the poorly soluble compound in a hydrophilic polymeric carrier. The potential of this technique to increase oral absorption and hence bioavailability is enormous. Nevertheless, some issues have to be considered regarding thermodynamic instability, as well in supersaturated solutions that are formed upon dissolution as in the solid state. Key findings After a brief discussion on the historical background of solid dispersions and their current role in formulation, an overview will be given on the physical chemistry and stability of glass solutions as they form supersaturated solutions, and during their shelf life. Conclusions Thorough understanding of these aspects will elicit conscious evaluation of carrier properties and eventually facilitate rational excipient selection. Thus, full exploitation of the solid dispersion strategy may provide an appropriate answer to drug attrition due to low aqueous solubility in later stages of development.

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“…The resulting product is then collected after cooling at room temperature and milled 46,47 . A reduction in processing temperature can be achieved by the association of hot-stage extrusion with the use of carbon dioxide as a plasticizer 48,49 which broadens the application of hot-stage extrusion to thermally labile compounds 48 . Solid dispersions of para-amino salicylic acid/ethylcellulose, itraconazole/ PVP 50 and itraconazole/ethylcellulose were successfully prepared by this technique.…”

Section: Fig 4: Manufacturing Processes Used To Produce Solid Dispermentioning

confidence: 99%

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2010

IJPSR

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The solubility behavior of drugs remains one of the most challenging aspects in the formulation development. Although there was a great interest in solid dispersion systems during the past four decades to increase solubility by improving dissolution rate and bioavailability of poorly soluble drugs; there commercial use has been very limited, primarily because of manufacturing difficulties and various stability problems. It can be carried out by reducing drug particle size to the absolute minimum, and hence improving drug wet-ability, bioavailability may be significantly improved. Solid dispersion of drugs was generally produced by melt or solvent evaporation methods. Recently, surfactants have been included to stabilize the formulations, thus avoiding drug recrystallization and potentiating their solubility. New manufacturing processes to obtain solid dispersions have also been developed to reduce the drawbacks of the initial process. In this review, it is intended to discuss the eminent approach to improve the solubility or the dissolution rate and recent revival has been discussed.

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The effect of pressurized carbon dioxide as a temporary plasticizer and foaming agent on the hot stage extrusion process and extrudate properties of solid dispersions of itraconazole with PVP-VA 64

Cited by 87 publications

References 15 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

Review: physical chemistry of solid dispersions

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