Clinical study of solid dispersions of itraconazole prepared by hot-stage extrusion

Six, K.; Daems, Tinne; Hoon, Jan de; Hecken, Anne Van; Depré, Marleen; Bouche, Marie-Paule; Prinsen, Paul; Verreck, Geert; Peeters, Jef; Brewster, Marcus E.; Mooter, Guy Van den

doi:10.1016/j.ejps.2004.10.005

Cited by 149 publications

(94 citation statements)

References 21 publications

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“…Over the last five years HME has been used largely to manufacture granules, pellets, immediate and modified release tablets, transmucosal/ transdermal films and implantable reservoir devices [3, 4,9,35]. For instance, with respect to drug administration through the oral route, molecular solid dispersions of nifedipine [38] , nimodipine [29] and itraconazole [39,40,41] have been successfully produced using HME technology. Amorphous indomethacin dispersions have been manufactured using pharmaceutically acceptable hydrophilic polymers by using HME technology [26,42,43].…”

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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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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“…Polymers that are able to form H-bonds with the API can usually prolong the supersaturated state realizing a higher bioavailability. 15 Vandecruys et al 19 screened some formulation excipients (with 25 drug candidates) that affect supersaturation by various mechanisms. Surfactants and hydroxypropyl-ß-cyclodextrin were found to be the best at augmenting the extent of supersaturation (enhancing the solubility), while pharmaceutical polymers (e.g., hydroxypropyl methylcellulose and polyvinylpyrrolidone) were more useful at maintaining the stability of supersaturated state but did not create a high supersaturation extent.…”

Section: Introductionmentioning

confidence: 99%

“…13 Therefore, amorphous solid dispersions with slower dissolution rates are sometimes more useful as they can prolong the time of supersaturation at a lower level. 14,15 In order to predict supersaturation and precipitation phenomena under in vivo circumstances, some in vitro models have been developed. 14,16,17 Tableting can enable adjusting the dissolution rate through appropriate compression force and composition, thus maximizing bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Lubricant-Induced Crystallization of Itraconazole From Tablets Made of Electrospun Amorphous Solid Dispersion

Démuth

Farkas

Balogh

et al. 2016

Journal of Pharmaceutical Sciences

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Keywords:oral drug delivery amorphous solid dispersion dissolution crystallization nanotechnology tableting chemical stability Raman spectroscopy a b s t r a c t Investigation of downstream processing of nanofibrous amorphous solid dispersions to generate tablet formulation is in a quite early phase. Development of high speed electrospinning opened up the possibility to study tableting of electrospun solid dispersions (containing polyvinylpyrrolidone-vinyl acetate and itraconazole [ITR] in this case). This work was conducted to investigate the influence of excipients on dissolution properties and the feasibility of scaled-up rotary press tableting. The dissolution rates from tablets proved to be mainly composition dependent. Magnesium stearate acted as a nucleation promoting agent (providing an active hydrophobic environment for crystallization of ITR) hindering the total dissolution of ITR. This crystallization process proved to be temperature dependent as well. However, the extent of dissolution of more than 95% was realizable when a less hydrophobic lubricant, sodium stearyl fumarate (soluble in the medium), was applied. Magnesium stearate induced crystallization even if it was put in the dissolution medium next to proper tablets. After optimization of the composition, scaled-up tableting on a rotary press was carried out. Appropriate dissolution of ITR from tablets was maintained for 3 months at 25 C/60% relative humidity. HPLC measurements confirmed that ITR was chemically stable both in the course of downstream processing and storage.

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“…Moreover, solid dispersions may improve the bioavailability of poorly water soluble drugs by increasing the drug dissolution rate and their saturation solubility in the gastrointestinal fluids. [10][11][12][13] The purpose of this study was to develop the solid dispersion of sibutramine freebase having high dissolution characteristics. For the formulation study, a suitable solubilizing agent and excipients were selected and a finalized formulation containing sibutramine freebase was taken for an pharmacokinetic study with the commercial product in beagle dogs.…”

Section: Introductionmentioning

confidence: 99%

Biopharmaceutical Evaluation of a Solid Dispersion System Containing Sibutramine Freebase

2008

Bulletin of the Korean Chemical Society

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To increase the solubility of sibutramine freebase, the solid dispersion was prepared using a fluid-bed granulator. The solid dispersion containing sibutramine freebase was characterized by differential scanning calorimetry (DSC) and powder X-ray diffraction (XRD). After filling the sibutramine solid dispersion in the gelatin hard capsule, we performed in vitro dissolution test, the stability test under accelerated conditions and pharmacokinetic study in beagle dogs. The DSC and XRD data showed that sibutramine solid dispersion would be amorphous state. The dissolution rate of sibutramine solid dispersion was significantly increased about 70% than sibutramine freebase. The stability of sibutramine solid dispersion capsules was equivalent or above to commercial product of sibutramine. In beagle dogs, the sibutramine solid dispersion showed equivalent pharmacokinetic behavior with commercial product of sibutramine hydrochloride. In conclusion, the solid dispersion system provided a possible way to overcome the low solubility of sibutramine freebase, and the sibutramine solid dispersion can be a bioequivalent with the commercial product in humans.

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Clinical study of solid dispersions of itraconazole prepared by hot-stage extrusion

Cited by 149 publications

References 21 publications

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

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

Lubricant-Induced Crystallization of Itraconazole From Tablets Made of Electrospun Amorphous Solid Dispersion

Biopharmaceutical Evaluation of a Solid Dispersion System Containing Sibutramine Freebase

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