Use of Surfactants as Plasticizers in Preparing Solid Dispersions of Poorly Soluble API: Stability Testing of Selected Solid Dispersions

Ghebremeskel, Alazar N.; Vemavarapu, Chandra; Lodaya, Mayur

doi:10.1007/s11095-006-9034-1

Cited by 109 publications

(68 citation statements)

References 11 publications

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“…Plasticizers can be divided into different classes such as traditional, non-traditional, and special plasticizers. The most commonly used traditional plasticizers are triacetin (48), citrate ester (41,49), vitamin E D-alpha tocopheryl PEG 1000 succinate (TPGS) (50), surfactants (51), and lowmolecular-weight polyethylene glycols (31). Non-traditional plasticizers are included in formulations to serve other critical functions and are often low-molecular-weight materials such as the active substance itself (52)(53)(54)(55).…”

Section: Plasticizersmentioning

confidence: 99%

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

2015

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Abstract. Hot-melt extrusion (HME) is a promising technology for the production of new chemical entities in the developmental pipeline and for improving products already on the market. In drug discovery and development, industry estimates that more than 50% of active pharmaceutical ingredients currently used belong to the biopharmaceutical classification system II (BCS class II), which are characterized as poorly water-soluble compounds and result in formulations with low bioavailability. Therefore, there is a critical need for the pharmaceutical industry to develop formulations that will enhance the solubility and ultimately the bioavailability of these compounds. HME technology also offers an opportunity to earn intellectual property, which is evident from an increasing number of patents and publications that have included it as a novel pharmaceutical formulation technology over the past decades. This review had a threefold objective. First, it sought to provide an overview of HME principles and present detailed engineered extrusion equipment designs. Second, it included a number of published reports on the application of HME techniques that covered the fields of solid dispersions, microencapsulation, taste masking, targeted drug delivery systems, sustained release, films, nanotechnology, floating drug delivery systems, implants, and continuous manufacturing using the wet granulation process. Lastly, this review discussed the importance of using the quality by design approach in drug development, evaluated the process analytical technology used in pharmaceutical HME monitoring and control, discussed techniques used in HME, and emphasized the potential for monitoring and controlling hot-melt technology.

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Section: Plasticizersmentioning

confidence: 99%

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

2015

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“…The other surfactants were not very effective as plasticizers. In a stability study of solid dispersions containing surfactants by the same group, the influence of the surfactant on physical stability was investigated (70). The addition of surfactant in HPMC E5 compositions resulted in crystallization when stored at 30°C/65% RH, but no difference was observed between samples with and without surfactant in PVP or PVP VA64 compositions.…”

Section: Thermal Processing Strategies Incorporation Of Plasticizers mentioning

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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“…65-80 (Crowley et al, 2002;McGinity et al, 1997;Repka et al, 1999a;Repka et al, 2000a;Repka et al, 2002b;Zhang, 1999) Poly(ethylene glycol) Carbowax ® -20 37-63 (Cuff et al, 1998;Forster et al, 2001c;Hamaura et al, 1999;Koleng et al, 1997;Perissutti et al, 2002;Repka et al, 2001c) Poly(vinyl pyrrolidone) Kollidon ® 168 - (Follonier et al, 1995;Forster et al, 2001a;Forster et al, 2001c;Hamaura et al, 1999;Hulsmann et al, 2001;Keleb et al, 2001) Poly ( (Miyagawa et al, 1996;Miyagawa et al, 1999;Sato et al, 1997) Ethylene-vinyl acetate copolymer plasticizers in producing solid dispersions by HME in addition to acting as solubilizers (Ghebremeskel et al, 2006). Additionally, several drug substances have been repo...…”

Section: Plasticizersmentioning

confidence: 99%

Pharmaceutical Applications of Hot-Melt Extrusion: Part I

Crowley¹,

Zhang²,

Repka

et al. 2007

Drug Development and Industrial Pharmacy

640

365

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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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Use of Surfactants as Plasticizers in Preparing Solid Dispersions of Poorly Soluble API: Stability Testing of Selected Solid Dispersions

Cited by 109 publications

References 11 publications

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

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

Pharmaceutical Applications of Hot-Melt Extrusion: Part I

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