Polymeric systems for amorphous Δ9-tetrahydrocannabinol produced by a hot-melt method. Part I: Chemical and thermal stability during processing

Munjal, Manish; Stodghill, Steven P.; ElSohly, Mahmoud A.; Repka, Michael A.

doi:10.1002/jps.20667

Cited by 24 publications

(14 citation statements)

References 25 publications

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“…The materials must meet the same levels of purity and safety as those prepared by traditional techniques. Most of the raw materials used in hot-melt extruded pharmaceuticals have been used in the production of other solid dosage forms such as tablets, pellets, granules, transdermal, and transmucosal systems (Aitken-Nichol et al, 1996;Munjal et al, 2006;Prodduturi et al, 2005;Repka et al, 1999aRepka et al, , 2000aRepka et al, , 2000bRepka et al, , 2001aRepka et al, , 2001bRepka et al, , 2002bRepka et al, , 2002cRepka et al, , 2006. Thermal stability of the individual compounds is a prerequisite for the process, although the short processing times encountered in this process may not limit all thermolabile compounds.…”

Section: Materials Used In Hot-melt Extrusionmentioning

confidence: 99%

“…Several research groups have demonstrated HME processes as a viable method to prepare pharmaceutical drug delivery systems, including granules (Follonier et al, 1995), pellets (Follonier et al, 1994;Young et al, 2002), sustained release tablets (Crowley et al, 2004b;Crowley et al, 2002;McGinity et al, 1997;Zhang, 1999;Zhang et al, 2000), transdermal and transmucosal drug delivery systems (Aitken-Nichol et al, 1996;Munjal et al, 2006;Prodduturi et al, 2005;Repka et al, 1999aRepka et al, , 2000bRepka et al, , 2001aRepka et al, , 2001bRepka et al, , 2002bRepka et al, , 2002d and implants (Bhardwaj et al, 1997(Bhardwaj et al, , 1998Rothen-Weinhold et al, 2000;Sam, 1992). The HME technique is an attractive alternative to traditional processing methods.…”

Section: Introductionmentioning

confidence: 99%

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Pharmaceutical Applications of Hot-Melt Extrusion: Part I

Crowley¹,

Zhang²,

Repka

et al. 2007

Drug Development and Industrial Pharmacy

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Interest in hot-melt extrusion techniques for pharmaceutical applications is growing rapidly with well over 100 papers published in the pharmaceutical scientific literature in the last 12 years. Hot-melt extrusion (HME) has been a widely applied technique in the plastics industry and has been demonstrated recently to be a viable method to prepare several types of dosage forms and drug delivery systems. Hot-melt extruded dosage forms are complex mixtures of active medicaments, functional excipients, and processing aids. HME also offers several advantages over traditional pharmaceutical processing techniques including the absence of solvents, few processing steps, continuous operation, and the possibility of the formation of solid dispersions and improved bioavailability. This article, Part I, reviews the pharmaceutical applications of hot-melt extrusion, including equipment, principles of operation, and process technology. The raw materials processed using this technique are also detailed and the physicochemical properties of the resultant dosage forms are described. Part II of this review will focus on various applications of HME in drug delivery such as granules, pellets, immediate and modified release tablets, transmucosal and transdermal systems, and implants.

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Section: Materials Used In Hot-melt Extrusionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Pharmaceutical Applications of Hot-Melt Extrusion: Part I

Crowley¹,

Zhang²,

Repka

et al. 2007

Drug Development and Industrial Pharmacy

Self Cite

646

365

View full text Add to dashboard Cite

show abstract

“…For both methods, the melting temperature must be high enough to ensure that the drug is completely melted and transformed to amorphous state. But at high temperature, both drug and polymer carriers face the risk of thermal degradation, especially for heat sensitive drugs (7,8). Therefore, how to decrease the processing temperature of MM and HME is a big challenge for pharmaceutical scientists.…”

Section: Introductionmentioning

confidence: 99%

Improving the Chemical Stability of Amorphous Solid Dispersion with Cocrystal Technique by Hot Melt Extrusion

et al. 2011

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“…HME possesses several advantages over traditional solvent casting methods for the preparation of patches, including continuous processing and avoidance of residual solvent [1][2][3][4]. Similarly, the transdermal route offers potential advantages of improved drug pharmacokinetics, elimination of gastrointestinal absorption problems and the hepatic first pass effect, reduction of dosing and improved patient compliance [5,6].…”

Section: Introductionmentioning

confidence: 99%

Hot melt extruded transdermal films based on amorphous solid dispersions in Eudragit RS PO: The inclusion of hydrophilic additives to develop moisture-activated release systems

Albarahmieh

Craig

2016

International Journal of Pharmaceutics

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A series of Eudragit RS PO-based hot melt extruded films were evaluated as potential transdermal systems, with particular emphasis on the inclusion of hydrophilic excipients to allow water sorption, which in turn would allow drug release on application to the skin. More specifically, sucrose, methyl cellulose, xanthan gum (Xantural®75), poloxamer (Pluronic®F127), Gelucire 44/14 were added to Eudragit RS PO and assessed in terms of physical structure (modulated temperature DSC (MTDSC), thermogravimetric analysis (TGA), powder XRD (PXRD), scanning electron microscopy(SEM)) and in vitro drug release and permeation properties. In addition, the effect of prior hydration on drug permeation was studied for selected systems. Phase separation was noted for sucrose, methylcellulose (high loading), xanthan gum (high loading), poloxamer and Gelucire 44/14 (high loading) using both visual observation and MTDSC. PXRD studies indicated drug crystallization within the phase separated systems. SEM studies broadly followed the same pattern. Dissolution studies indicated that the hydrophilic excipients considerably enhanced the release rate, while Franz diffusion cell studies showed a much greater variability in effectiveness, which we ascribe to the paucity of water of hydration present which would not allow swellable additives such as xanthan to release the drug. However, films containing Gelucire 44/14 emerged as the most satisfactory systems, despite the higher additive loaded systems showing drug phase separation. This may be related to emulsification rather than swelling on contact with water, as noted for the permeation studies involving prehydration. This strategy therefore presents a promising approach for triggered transdermal drug delivery, activated by hydration from the skin itself.

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Polymeric systems for amorphous Δ9-tetrahydrocannabinol produced by a hot-melt method. Part I: Chemical and thermal stability during processing

Cited by 24 publications

References 25 publications

Pharmaceutical Applications of Hot-Melt Extrusion: Part I

Pharmaceutical Applications of Hot-Melt Extrusion: Part I

Improving the Chemical Stability of Amorphous Solid Dispersion with Cocrystal Technique by Hot Melt Extrusion

Hot melt extruded transdermal films based on amorphous solid dispersions in Eudragit RS PO: The inclusion of hydrophilic additives to develop moisture-activated release systems

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