Characterization of ternary solid dispersions of Itraconazole in polyethylene glycol 6000/polyvidone-vinylacetate 64 blends

Janssens, Sandrien; Armas, Héctor Novoa de; D'Autry, Ward; Schepdael, Ann Van; Mooter, Guy Van den

doi:10.1016/j.ejpb.2008.02.007

Cited by 29 publications

(14 citation statements)

References 15 publications

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“…There are also various approaches regarding the method of preparing solid dispersions by the solvent method, including evaporation, spray, and freeze drying (10). A number of carriers can be employed for preparing solid dispersions, including polyethylene glycols (11,12), polyvinylpyrrolidone (13), hydroxypropyl methylcellulose (14,15), and poloxamer (16)(17)(18). The structure of PVP K30, a hydrophilic polymer, is shown in Fig.…”

Section: Introductionmentioning

confidence: 99%

Preparation and Evaluation of Solid Dispersions of A New Antitumor Compound Based on Early-Stage Preparation Discovery Concept

Hou

Cao

et al. 2013

AAPS PharmSciTech

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Ensuring sufficient drug solubility is a crucial problem in pharmaceutical-related research. For water-insoluble drugs, various formulation approaches are employed to enhance the solubility and bioavailability of lead compounds. The goal of this study was to enhance the dissolution and absorption of a new antitumor lead compound, T-OA. Early-stage preparation discovery concept was employed in this study. Based on this concept, a solid dispersion system was chosen as the method of improving drug solubility and bioavailability. Solid dispersions of T-OA in polyvinylpyrrolidone (PVP) K30 were prepared by the solvent evaporation method. Dissolution testing determined that the ideal drug-to-PVP ratio was 1:5. X-ray diffraction, Fourier transform infrared spectroscopy, and differential scanning calorimetry were employed to confirm the formation of solid dispersions. Scanning electron microscopy demonstrated that T-OA was converted into an amorphous form. Both in vitro dissolution testing and the in vivo studies demonstrated that the solubility and bioavailability of T-OA were significantly improved when formulated in a solid dispersion with PVP. The dissolution rate of the T-OA/PVP solid dispersion was greatly enhanced relative to the pure drug, and the relative bioavailability of T-OA solid dispersions was found to be 392.0%, which is 4-fold higher than the pure drug.

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Section: Introductionmentioning

confidence: 99%

Preparation and Evaluation of Solid Dispersions of A New Antitumor Compound Based on Early-Stage Preparation Discovery Concept

Hou

Cao

et al. 2013

AAPS PharmSciTech

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“…The impact of surfactant addition in solid dispersions has been extensively studied by the group of Dr. Van den Mooter (71)(72)(73)(74). In one study, the surfactant TPGS 1000 was incorporated into solid dispersions containing an experimental antiviral compound, UC781, and either PVP VA64 or HPMC 2910 resulting in more rapid dissolution rates as the surfactant concentration was increased in solid dispersion granules (75).…”

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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“…The first SD generation involved the use of crystalline carries (4,5) and sugars (6), while for the second generation several types of hydrophilic polymers such as polyethylene glycols (7,8), polyvinylpyrrolidone (9,10) among others, have been assayed.…”

Section: Introductionmentioning

confidence: 99%

Improved Albendazole Dissolution Rate in Pluronic 188 Solid Dispersions

et al. 2010

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Abstract. Solids dispersions (SDs) have been proposed as an alternative to improve the dissolution rate of low solubility drugs. SDs containing albendazole (ABZ; 5, 10, 25, and 50% w/w) and Pluronic 188 (P 188) as hydrophilic carrier were formulated. The obtained SDs were assessed in comparison to physical mixtures (PMs). Drug-polymer interactions in solid state were investigated using Fouriertransform infrared spectroscopy, scanning electron microscopy, and X-ray diffraction analysis. No chemical interaction was found between ABZ and poloxamer. The dissolution profiles indicated that ABZ incorporated in SDs and PMs was rapidly released, reaching rapidly the steady state. Increased dissolution rates are usually observed at the highest polymer proportions. However, an opposite effect for SDs as well as for PMs was observed in the assays described here. The systems with the lowest P 188 percentages (SD4, SD3; PM4, PM3) tended to be more effective in increasing the ABZ dissolution rate. Such a result can be attributed to the fact that concentrated aqueous solutions of Poloxamer may form thermo-reversible gels. The physical-mechanical properties indicated that SDs possess improved flow and compacting properties compared to PMs. Thus, ABZ SDs would be more convenient for solid dosage form design and manufacture.

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Characterization of ternary solid dispersions of Itraconazole in polyethylene glycol 6000/polyvidone-vinylacetate 64 blends

Cited by 29 publications

References 15 publications

Preparation and Evaluation of Solid Dispersions of A New Antitumor Compound Based on Early-Stage Preparation Discovery Concept

Preparation and Evaluation of Solid Dispersions of A New Antitumor Compound Based on Early-Stage Preparation Discovery Concept

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

Improved Albendazole Dissolution Rate in Pluronic 188 Solid Dispersions

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