• Proceedings of the PSK Conference
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• 2002.10a
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• pp.412.1-412.1
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• 2002

Purpose. To prepare PVP-based solid dispersions containing lovastatin (LOS) and solubilizers (sodium lauryl sulfate. Tween80. oleic acid) to enhance dissolution of practically insoluble LOS. Methods. Solid dispersions containing LOS were prepared by dissolving two different organic solvent systems (acetone/ethanol or acetonitrile/ethanol). Results. The stickiness and flowability of solid dispersion powders were dependent on the composition and ratio of the solubilizers. (omitted)

• Polymer(Korea)
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• v.38 no.4
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• pp.434-440
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• 2014

We prepared nanoparticles containing insoluble celecoxib by the method of solid dispersions using a spray dryer to improve solubility of celecoxib. We used PVP K30 and Eudragit EPO as water-soluble carriers for the solid dispersion, and poloxamer 407 as a surfactant. Characterization of celecoxib solid dispersion was performed by scanning electron microscope (SEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FTIR). The results of SEM, DSC and XRD demonstrated that celecoxib is amorphous in solid dispersion. The dissolution rate measured in intestinal juice showed that the method of solid dispersion improved celecoxib solubility as compared with a conventional drug (Celebres$^{(R)}$). In conclusion, solid dispersion formulation prepared by a spray dryer would improve the solubility of celecoxib in oral administration.

• Polymer(Korea)
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• v.33 no.6
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• pp.596-601
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• 2009

We prepared nanoparticles containing insoluble aceclofenac by the method of solid dispersions using spray dryer to improve solubility of aceclofenac. We used PVP-K30 as a water soluble carrier for the solid dispersion and poloxamer as a surfactant. Characterization of aceclofenac solid dispersion was performed by SEM, DSC, XRD and FT-IR. The results of SEM, DSC and XRD demonstrated that aceclofenac is amorphous in solid dispersion. The formation of salt by hydrogen bond between aceclofenac and PVP K-30 was confirmed by FT-IR. The dissolution rate measured in intestinal juice showed the method of solid dispersion improved aceclofenac solubility as compared with a conventional drug($Airtal^{(R)}$). In conclusion, the method of solid dispersion using spray dryer would improve solubility of aceclofenac in oral administration.

• Journal of Pharmaceutical Investigation
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• v.38 no.2
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• pp.111-117
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• 2008

To overcome the solubility of poorly water-soluble drug, the formation of solid dispersion using a spray-dryer with polymeric material, that can potentially enhance the dissolution rate extend of drug absorption was considered in this study. $Eudragit^{(R)}$ E100 as carrier for solid dispersion is acrylate copolymer that soluble in acidic buffer solutions (below pH 5.0). It was used to increase dissolution of atorvastatin calcium as a water-insoluble drug in acidic environments. In this study, a spray-dryer was used to prepare solid dispersion of atorvastatin calcium and $Eudragit^{(R)}$ E100 for purpose of improving the solubility of drug. Atorvastatin calcium and $Eudragit^{(R)}$ E100 were dissolved in ethanol and spray-dryed. DSC and XRD were used to analyze the crystallinity of the sample. It was found that atorvastatin calcium is amorphous in the $Eudragit^{(R)}$ E100 solid dispersion. FT-IR was used to analyze the salt formation by interaction between atorvastatin calcium and $Eudragit^{(R)}$ E100. Comparative dissolution study exhibited better dissolution characteristics than the commercial drug ($Lipitor^{(R)}$) as control. The dissolution rate of atorvastatin calcium was markedly increased in solid dispersion system in simulated gastric juice (pH 1.2). This study proposed that this solid dispersion system improved the bioavailability of poorly water-soluble atorvastatin calcium.

• Journal of Pharmaceutical Investigation
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• v.32 no.3
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• pp.173-179
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• 2002

Solid dispersions of ipriflavone with PVP were prepared by a spray-drying method in order to improve the bioavailability. They were measured with scanning electron microscopy, differential scanning calorimetry, x-ray powder diffraction, and Fourier transform infrared spectroscopy to evaluate the physicochemical interaction between ipriflavone and PVP and study the correlation between these physicochemical characteristics and bioavailability. Ipriflavone exhibited crystallinity, whereas PVP was almost amorphous. The area of the endotherm $({\Delta}H)$ of freezer milled ipriflavone, freezer milled ipriflavone physically mixed with freezer milled PVP, and physically mixed ipriflavone with PVP was almost the same, whereas ${\Delta}H$ of the solid dispersed ipriflavone with PVP was much smaller than that of the other preparation types. Also, the crystallinity and the crystal size of ipriflavone in the solid dispersed ipriflavone with PVP were much smaller than those of the other preparation types. From the in vivo test, the AUC of the solid dispersed ipriflavone with PVP was approximately 10 times higher than that of the physically mixed ipriflavone with PVP. The solid dispersion using the spray-drying method with a water-soluble polymer, PVP, may be effective for the improvement of the bioavailability.

• Journal of Pharmaceutical Investigation
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• v.19 no.2
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• pp.109-116
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• 1989

Solid dispersion of fenticonazole nitrate (FN) with poloxamer 407, polyethylene glycol 6000, povidone (K-90) were prepared by the solvent method. To characterize the state of the drug in solid dispersions, the x-ray diffractometry and differential scanning calorimetry were carried out. The identification of these systems suggested that FN in the poloxamer 407 system remained in crystalline state, and the drug in the PVP system was amorphous. A marked increase in the dissolution rate of FN was attained by dispersing the drug in the hydrophilic polymers used, and the dispersion with poloxamer 407 was superior to the other two carriers in releasing the drug into solution.

• YAKHAK HOEJI
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• v.54 no.4
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• pp.316-321
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• 2010

Adefovir dipivoxil which was originally developed by Gilead Sciences has been used as treatments of HIV and HBV, especially a therapeutics for HBeAg positive and negative chronic patients. We developed highly efficient purification method using reverse phase column chromatography for mass production and a stable amorphous Adefovir dipivoxil using solid dispersion method. Reverse phase column chromatography led to highly pure product, more than 99.7% by HPLC and can be used for mass production compared with normal column chromatography. Solid dispersion method containing watersoluble polymer and Isomalt showed improved stability of amorphous Adefovir dipivoxil against heat and moisture.

• Journal of Pharmaceutical Investigation
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• v.28 no.4
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• pp.267-274
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• 1998

Biphenyl dimethyl dicarboxylate (DDB) has been used for the treatment of acute and chronic hepatitis. However, its poor solubility in water, $2.5\;{\mu}g/ml$, caused low bioavailability of the drug after its oral administration. In order to increase the dissolution of DDB in gastrointestinal tracts, consequently to increase the bioavailability of the drug, DDB tablet was prepared with solid dispersion of DDB with poloxamer 338 or 407 using a direct compression method. To improve the flowability of the solid dispersion, Aerosil was used as an adsorbent. The effect of formulation variables (poloxamer and Aerosil contents) on the dissolution rate of DDB from tablets was investigated using an analysis of variance. The dissolution rate of DDB from tablets was evaluated with KP II (paddle) method. The dissolution patterns of the drug from the tablet prepared with poloxamer 407 were affected significantly by the contents of poloxamers and Aerosil over the range employed, but those of the drug from the tablet prepared with poloxamer 338 were not. The optimum formulation of the DDB tablet, showed the same dissolution pattern as that of the reference, was obtained after polynomial equations of drug dissolution profiles for each formula were fitted to contour plots. The optimum formulation ratios of DDB:poloxamer 407:Aerosil were 1:2.5:2.5 and 1:5:5.

• Journal of Convergence for Information Technology
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• v.10 no.12
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• pp.236-244
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• 2020

In this research a suspended solid transport experiment was conducted in the river experiment center to find the characteristics and dispersion of the material. Modeling by the particle dispersion model was also executed to reproduce the suspended solid transport. The suspended solid was consisted of a mixture of silica and water using a mixing equipment, which was then introduced into a real-scale flume and measured with the laser-diffraction based particle size analyzer(LISST) to find the concentration of the material. The comparison between the measured suspended solid concentration using drone images and particle size analyzers, with the model showed a good match overall, which proved the applicability of the model. Along with finding the model applicability, the research showed the potential for suspended solid estimation in high flow situations with high rainfall.

• Journal of Pharmaceutical Investigation
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• v.38 no.4
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• pp.241-247
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• 2008

Paclitaxel is a taxane diterpene amide, which was first extracted from the stem bark of the western yew, Taxus brevifolia. This natural product has proven to be useful in the treatment of a variety of human neoplastic disorders, including ovarian cancer, breast and lung cancer. Paclitaxel is a highly hydrophobic drug that is poorly soluble in water. It is mainly given by intravenous administration. Therefore, The pharmaceutical formulation of paclitaxel ($Taxol^{(R)}$; Bristol-Myers Squibb) contains 50% $Cremophor^{(R)}$ EL and 50% dehydrated ethanol. However the ethanol/Cremophor EL vehicle required to solubilize paclitaxel in $Taxol^{(R)}$ has a pharmacological and pharmaceutical problems. To overcome these problems, new formulations for paclitaxel that do not require solubilization by $Cremophor^{(R)}$ EL are currently being developed. Therefore this study utilized a supercritical fluid antisolvent (SAS) process for cremophor-free formulation. To select hydrophilic polymers that require solubilization for paclitaxel, we evaluated polymers and the ratio of paclitaxel/polymers. HP-${\beta}$-CD was used as a hydrophilic polymer in the preparation of the paclitaxel solid dispersion. Although solubility of paclitaxel by polymers was increased, physical stability of solution after paclitaxel/polymer powder soluble in saline was unstable. To overcome this problem, we investigated the use of surfactants. At 1/20/40 of paclitaxel/hydrophilic polymer/ surfactant weight ratio, about 10 mg/mL of paclitaxel can be solubilized in this system. Compared with the solubility of paclitaxel in water ($1\;{\mu}g/mL$), the paclitaxel solid dispersion prepared by SAS process increased the solubility of paclitaxel by near 10,000 folds. The physicochemical properties was also evaluated. The particle size distribution, melting point and amophorization and shape of the powder particles were fully characterized by particle size distribution analyzer, DSC, SEM and XRD. In summary, through the SAS process, uniform nano-scale paclitaxel solid dispersion powders were obtained with excellent results compared with $Taxol^{(R)}$ for the physicochemical properties, solubility and pharmacokinetic behavior.