Development of novel itraconazole-loaded solid dispersion without crystalline change with improved bioavailability

Park, Young Joon; Xuan, Jing Ji; Oh, Dong Hoon; Balakrishnan, Pachamuthu; Yang, Haozhe; Yeo, Woo Hyun; Lee, Mi Kyung; Choi, Han Gon; Yong, Chul Soon

doi:10.1007/s12272-010-0812-2

Cited by 24 publications

(8 citation statements)

References 32 publications

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“…8 indicated that SM-SD exhibited faster drug release than the other preparations tested. As previously reported, rapid hydration of hydrophilic polymers promotes the drug wetting process in aqueous surroundings and enlarges the surface area of the solidewater interface, which may contribute to the improved SD dissolution rate [25]. However, SM-SD-SEDS showed a cumulative release of more than 90% in the first 5 min, whereas less than 70% release was observed from SM-SD-SE at 5 min.…”

Section: In Vitro Dissolution Testmentioning

confidence: 56%

Improved dissolution and bioavailability of silymarin delivered by a solid dispersion prepared using supercritical fluids

Yang

Zhao

Feng

et al. 2015

Asian Journal of Pharmaceutical Sciences

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Available online xxxKeywords: Silymarin Solution-enhanced dispersion by supercritical fluids Solid dispersion Dissolution Bioavailability a b s t r a c tThe objective of this study was to improve the dissolution and bioavailability of silymarin (SM). Solid dispersions (SDs) were prepared using solution-enhanced dispersion by supercritical fluids (SEDS) and evaluated in vitro and in vivo, compared with pure SM powder.The particle sizes, stability, and contents of residual solvent of the prepared SM-SDs with SEDS and solvent evaporation (SE) were investigated. Four polymer matrix materials were evaluated for the preparation of SM-SD-SEDS, and the hydrophilic polymer, polyvinyl pyrrolidone K17, was selected with a ratio of 1:5 between SM and the polymer. Physicochemical analyses using X-ray diffraction and differential scanning calorimetry indicated that SM was dispersed in SD in an amorphous state. The optimized SM-SD-SEDS showed no loss of SM after storage for 6 months and negligible residual solvent (ethanol) was detected using gas chromatography. In vitro drug release was increased from the SM-SD-SEDS, as compared with pure SM powder or SM-SD-SE. In vivo, the area under the rat plasma SM concentration-time curve and the maximum plasma SM concentration were 2.4-fold and 1.9-fold higher, respectively, after oral administration of SM-SD-SEDS as compared with an aqueous SM suspension. These results illustrated the potential of using SEDS to prepare SM-SD, further improving the biopharmaceutical properties of this compound. © 2014 Shenyang Pharmaceutical University. Production and hosting by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/ licenses/by-nc-nd/4.0/).

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Section: In Vitro Dissolution Testmentioning

confidence: 56%

Improved dissolution and bioavailability of silymarin delivered by a solid dispersion prepared using supercritical fluids

Yang

Zhao

Feng

et al. 2015

Asian Journal of Pharmaceutical Sciences

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“… 10 , 13 To reinforce the dissolution rate or the physical stability of dispersed drug entities in the carrier matrix, additives such as surfactants or pH modulators can also be used. 8 , 14 , 15 It was reported earlier that the oral bioavailability of ITZ could be enhanced by coadministration with a vitamin C beverage in healthy participants. 16 Vitamin C (L-ascorbic acid, LAA), a highly acidic material, is an essential micronutrient involved in many biological and biochemical functions ( Figure 1 ).…”

Section: Introductionmentioning

confidence: 99%

“…Various techniques have been used to improve the solubility of poorly water-soluble drugs, including using surfactants, 5 inclusion complexation, 6 , 7 and solid dispersion (SD) techniques. 8 For example, the SD technique has been well used to enhance the dissolution rate of ITZ, 4 , 8 – 10 and one of the commercial products of ITZ (Sporanox ® ) is a hard capsule form containing ITZ coated on sugar spheres. Drug was layered onto the sugar pellets by the fluid bed-based SD technique using hydroxypropyl methylcellulose (HPMC) as the hydrophilic dispersing material.…”

Section: Introductionmentioning

confidence: 99%

Itraconazole solid dispersion prepared by a supercritical fluid technique: preparation, in vitro characterization, and bioavailability in beagle dogs

Yin

Daintree²,

Ding³

et al. 2015

DDDT

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This research aimed to develop a supercritical fluid (SCF) technique for preparing a particulate form of itraconazole (ITZ) with good dissolution and bioavailability characteristics. The ITZ particulate solid dispersion was formulated with hydroxypropyl methylcellulose, Pluronic F-127, and L-ascorbic acid. Aggregated particles showed porous structure when examined by scanning electron microscopy. Powder X-ray diffraction and Fourier transform infrared spectra indicated an interaction between ITZ and excipients and showed that ITZ existed in an amorphous state in the composite solid dispersion particles. The solid dispersion obtained by the SCF process improved the dissolution of ITZ in media of pH 1.0, pH 4.5, and pH 6.8, compared with a commercial product (Sporanox®), which could be ascribed to the porous aggregated particle shape and amorphous solid state of ITZ. While the solid dispersion did not show a statistical improvement (P=0.50) in terms of oral bioavailability of ITZ compared with Sporanox®, the Cmax (the maximum plasma concentration of ITZ in a pharmacokinetic curve) of ITZ was raised significantly (P=0.03) after oral administration. Thus, the SCF process has been shown to be an efficient, single step process to form ITZ-containing solid dispersion particles with good dissolution and oral bioavailability characteristics.

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“…Moreover, Mosapride dispersed in carriers may achieve the highest levels of particle size reduction and surface area enhancement [26][27][28] .…”

Section: X-ray Diffraction Analysismentioning

confidence: 99%

Influence of poloxmer on the dissolution properties of mosapride and its pharmaceutical tablet formulation

2017

Egypt. J. Chem.

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T HIS WORK was an attempt to improve therapeutic efficacy and increase patient compliance thereby formulating immediate release of Mosapride citrate's tablets with improved physical and chemical characteristics. The tablet form was prepared by wet granulation of Mosapride with a binder solution of Poloxmer 407 and compressed the dried granules of Mosapride into non-friable, stable tablets. The other objective, the performance of two classes of superdisintegrants as croscarmellose sodium (AcDi-Sol), and sodium starch glycolate (Primojel) in dissolution of Mosapride immediate release and promoting disintegration tablets was evaluated. The post-compression and the pre-compression parameters were characterized which within their respective standards must lie. Chemical composition and crystallinity were investigated via FTIR and XRD, respectively. The post compression parameters such as thickness test, hardness, friability testes and in vitro drug release studies were also performed.

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Development of novel itraconazole-loaded solid dispersion without crystalline change with improved bioavailability

Cited by 24 publications

References 32 publications

Improved dissolution and bioavailability of silymarin delivered by a solid dispersion prepared using supercritical fluids

Improved dissolution and bioavailability of silymarin delivered by a solid dispersion prepared using supercritical fluids

Itraconazole solid dispersion prepared by a supercritical fluid technique: preparation, in vitro characterization, and bioavailability in beagle dogs

Influence of poloxmer on the dissolution properties of mosapride and its pharmaceutical tablet formulation

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