• Title/Summary/Keyword: Solid dispersions

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Preparation and Characterization of Solid Dispersions of Eprosartan with Hydrophilic Polymers (친수성 고분자를 이용한 에프로살탄 고체분산체의 제조 및 특성 분석)

  • Hwang, Jun-Seok;Ko, Ji-Eun;Kim, So-Hee;Huh, Kang-Moo
    • Polymer(Korea)
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    • v.36 no.4
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    • pp.500-506
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    • 2012
  • In this study, we developed and optimized hydrophilic polymer based solid dispersion formulations (SDs) for enhancing the aqueous solubility of eprosartan, one of poorly soluble drugs, that has been broadly used for the treatment of high blood pressure. Poly(ethylene glycol) (PEG) and poly(vinyl pyrrolidone) (PVP) based SDs were prepared by hot melting and solvent evaporation methods and the drug/polymer composition varied in the range of 1:1~1:5 with or without poloxamer 407 (P407) as a polymeric surfactant. The SDs prepared by solvent evaporation showed more reduced crystallinity than ones by hot melting, and PVP based SDs showed more enhanced solubility and lower crystallinity than PEG based SDs. Furthermore, it was observed from DSC and PXRD analysis that the SDs with P407 (drug:polymer: P407 = 1:5:1) demonstrated no crystallinity and the most enhanced solubility (more than 3~4 times).

A Study for The Effect of Variation of Resin Content on The Rheological Characteristics of Ink Vehicle (수지의 함량 변화에 따른 잉크 비히클의 유변학적 특성에 관한 연구)

  • Bang, Jong-Gwan;Kim, Sung-Bin;Kim, Tae-Hwan;Lee, Kyu-Il
    • Journal of the Korean Graphic Arts Communication Society
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    • v.23 no.2
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    • pp.117-128
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    • 2005
  • Printing inks are basically dispersions of solid pigment particles in a vehicle. Pigment flocculation and/or colloidal aggregates created by thixotrope additives form a three- dimensional network in the inks. This structure complicates the flow behaviour of inks. However, if the internal structure is formed under control, the printing process will benefit from it because the ink must satify rheological requirements over a very wide range of shear conditions. The presence of internal structure results in the following prominent non-Newtonian rheological properties: viscoelasticity, yield stress, shear thinning and thixotropy. If the components of printing inks were changed, the rheological characteristics such as viscosity, yield stress, viscoelasticity and tack value were considerably varied. Thus, in this paper, the effects of changing the content of rosin modified phenolic resin on rheological properties of the vehicle will be studied. For that, the rheological properties were found by flow, yield stress, creep and oscillation measurements using Bohlin C-VOR Rotational Rheometer. And Emulsion rheology and its microstructure will be investigated.

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Collective Excitations in Thin K Films on Al(111)

  • Kim, Bong-Ok
    • Proceedings of the Korean Vacuum Society Conference
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    • 2000.02a
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    • pp.137-137
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    • 2000
  • The surface collective modes of thin K films deposited on Al(111) have been investigated using frequency dependent photoyield measurements and momentum resolved inelastic electron scattering. Jellium based theoretical calculations have predicted a richer set of features in the thin films than for the surface of a semi-infinite solid because there are th interference between two interfaces (substrate-film and film-vacuum) and heavy damping on the substrate. The use of an optical probe and electron scattering has allowed us to draw a more complete picture of the dynamic screening in thin films. The number, dispersion, damping and optical activity of the collective modes of the thin films have been measured as a function of K film thickness. New overlayer-induced excitations are observed : At qII=0, they correspond to the antisymmetric slab mode and the multipole surface plasmon. At finite qII=0, these modes undergo a transition towards the K multipole and monopole surface plasmons. With increasing coverage, the overlayer excitations turn into the collective modes of semi-infinite K. For a consistent interpretation of photoyield and electron energy loss spectra it is crucial to account for the non-analytic dispersion of the overlayer modes at small parallel wave vectors and for the finite angular resolution of the detector. The observed dispersions confirm predictions based on the time-dependent density functional approach.

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A Study of Dexibuprofen Loaded Solid Dispersion Using Rotary Hot-melt Granulation (회전식 고온용융과립법을 이용한 덱시부프로펜 함유 고체분산체 연구)

  • Kim, Dong-Wook
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.21 no.2
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    • pp.595-600
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    • 2020
  • The purpose of this paper was to prepare and evaluate solid dispersions (SD) that can increase the dissolution rate of dexibuprofen as a model drug with low solubility in water using saccharides and sugar alcohols as dispersion materials. DSC, XRD, content and content uniformity test, dissolution test, and disintegration test were conducted for physicochemical evaluation of the prepared SD. For the results, it was confirmed using differential scanning calorimetry that fructose, which has a melting point around 120 ℃ of the device operating temperature range, is a suitable excipient for the preparation of SD by the rotary hot-melt granulation (RHMG) method. X-ray diffraction analysis was conducted to confirm that the crystallinity of dexibuprofen was reduced. Disintegration test of the prepared tablet using SD-containing dexibuprofen and fructose confirmed a very fast disintegration time within 1~2 seconds and also showed that the dissolution rate was about 20% faster than that of the dexibuprofen raw material. Dexibuprofen with reduced crystallinity by SD confirmed through the RHMG method can be used to increase the dissolution rate of the drug and increase the disintegration time of the tablet. Thus, it can be used in the manufacturing of various solid preparations.

Effect of Solubilizing and Microemulsifying Excipients in Polyethylene Glycol 6000 Solid Dispersion on Enhanced Dissolution and Bioavailability of Ketoconazole

  • Heo, Min-Young;Piao, Zong-Zhu;Kim, Tae-Wan;Cao, Qing-Ri;Kim, Ae-Ra;Lee, Beom-Jin
    • Archives of Pharmacal Research
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    • v.28 no.5
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    • pp.604-611
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    • 2005
  • Polyethylene glycol (PEG) 6000-based solid dispersions (SDs), by incorporating various pharmaceutical excipients or microemulsion systems, were prepared using a fusion method, t o compare the dissolution rates and bioavailabilities in rats. The amorphous structure of the drug in SDs was also characterized by powder X-ray diffractometry (XRD) and differential scanning calorimetry (DSC). The ketoconazole (KT), as an antifungal agent, was selected as a model drug. The dissolution rate of KT increased when solubilizing excipients were incorporated into the PEG-based SDs. When hydrophilic and lipophilic excipients were combined and incorporated into PEG-based SDs, a remarkable enhancement of the dissolution rate was observed. The PEG-based SDs, incorporating a self microemulsifying drug delivery system (SMEDDS) or microemulsion (ME), were also useful at improving the dissolution rate by forming a microemulsion or dispersible particles within the aqueous medium. However, due to the limited solubilization capacity, these PEG-based SDs showed dissolution rates, below 50% in this study, under sink conditions. The PEG-based SD, with no pharmaceutical excipients incorporated, increased the maximum plasma concentration (C$_{max}$) and area under the plasma concentration curve (AUC$_{0-6h}$) two-fold compared to the drug only. The bioavailability was more pronounced in the cases of solubilizing and microemulsifying PEG-based SDs. The thermograms of the PEG-based SDs showed the characteristic peak of the carrier matrix around 60$^{\circ}C$, without a drug peak, indicating that the drug had changed into an amorphous structure. The diffraction pattern of the pure drug showed the drug to be highly crystalline in nature, as indicated by numerous distinctive peaks. The lack of the numerous distinctive peaks of the drug in the PEG-based SDs demonstrated that a high concentration of the drug molecules was dissolved in the solid-state carrier matrix of the amorphous structure. The utilization of oils, fatty acid and surfactant, or their mixtures, in PEG-based SD could be a useful tool to enhance the dissolution and bioavailability of poorly water-soluble drugs by forming solubilizing and microemulsifying systems when exposed to gastrointestinal fluid.

Dissolution Characteristics of Hydrophobic Drug-Soluble Carrier Coprecipitate (I)-Enhanced Dissolution Rates of Furosemide from Furosemide Polymer Coprecipitates-

  • Shin, Sang-Chull;Lee, Min-Hwa;Woo, Jong-Hak
    • Journal of Pharmaceutical Investigation
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    • v.6 no.3
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    • pp.48-57
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    • 1976
  • An enhancement in the dissolution rate of the drug should facilitate its GI absorption if the absorption process is dissolution rate limited. One of the need for the techniques that can potentially enhance the dissolution rate and extent of absorption of hydrophobic drugs is the formation of coprecipitates with pharmacologically inert, polymeric materials. The physicochemical modification offers the advantage of possibly enabling one to administer the drug orally in a form from which it is most available for GI absorption. Several $investigation^{1-15)}$ demonstrated that the formation of solid dispersions or coprecipitates of relatively water-insoluble drugs with various pharmacologically inert carriers can increase singnificantly their in vitro dissolution rates. However, little information is available in the literature related to the dissolution rate patterns of furosemide, a water-insoluble diurectices, with respect to the sort of copolymer and the ratio of coprecipitates as a function of time, respectively. The purpose of the present investigation was to ascertain, the general applicability of the copolymers to use fore more fast, enhanced dissolution techniques of furosemide. To accomplish the need for enhancement in the dissolution rate of furosemide, varying ratio coprecipitates with different water-soluble polymers, such as polyvinylpyrrolidone (PVP), polyethylene glycol 4000(PEG 4000), and polyethylene glycol 6000 (PEG 6000), were quantitatively studied by comparing their dissolution characteristics of furosemide. The dissolution patterns of pure furosemide, varying ratio furosemide-PVP coprecipitates, (1:2, 1:5, and 1:9(w/w)), furosemide-PEG 4000 coprecipitates (1:4, 1:9, and 1:19(w/w), furosemide-PEG 6000 coprecipitates(1:4, 1:9, and 1:19(w/w)), and the same ratio physical mixtures, respectively, were compared by the amount dissolved as a function of time.

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Solubilization of Quercetin , and Permeability Study of Quercetin and Rutin to Rabbit Duodenal Mucosa (퀘르세틴의 가용화 , 퀘르세틴 및 루틴의 토끼 십이지장 점막 투과성)

  • Chun, In-Koo;Seo, Eun-Ha
    • YAKHAK HOEJI
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    • v.42 no.1
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    • pp.59-69
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    • 1998
  • To increase the solubility of quercetin, which is a practically insoluble flavonoid of Ginkgo biloba leaf, the effects of nonaqueous vehicles. Their cosolvents, water-sol uble polymers and modified cyclodextrins (CDs) were observed. Polyethylene glycols, diethyleneglycol monoethyl ether, and their cosolvents with water showed a good solvency toward quercetin. Also the aqueous solutions of povidone, copolyvidone and Cremophor RH 40 was effective in solubilizing quercetin. Complex formation of quercetin with ${\beta}$-cyclodextrin (${\beta}$-CD), dimethyl-${\beta}$-cyclodextiin (DMCD), 2-hydroxypropyl-${\beta}$-cyclodextrin (HPCD) and ${\beta}$-cyclodextrin sulfobutyl ether (SBCD) in water was investigated by solubility method at $37^{\circ}C$. The addition of CDs in water markedly increased the solubility of quercetin with increasing the concentration. AL type phase solubility diagrams were obtained with CDs studied. Solubilizaton efficiency by CDs was in the order of SBCD >> DMCD > HPCD > ${\beta}$-CD. The dissolution rates of quercetin from solid dispersions with copolyvidone, povidone and HPCD were much faster than those of drug alone and corresponding physical mixtures, and exceeded the equilibrium solubility (3.03${\pm}1.72{\mu}$g/ml). The permeation of quercetin through duodenal mucosa did not occur even in the presence of enhancers such as bile salts, but the permeation was observed when the mucus layer was scraped off. This was due to the fact that quercetin had a strong binding to mucin ($58.5{\mu}$g/mg mucin). However rutin was permeable to the duodenal mucosa. The addition of enhancer significantly increased the permeation of rutin in the order of sodium glycocholate.

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Adhesive Strength in Tension of SBR-Modified Cement Mortar with Self-Flowability Material for Floor-Finishing (자기 평활성 바닥 마감용 SBR 시멘트 모르타르의 인장부착강도)

  • Do, Jeong-Yun;Soh, Yang-Seob
    • Journal of the Korea Concrete Institute
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    • v.15 no.4
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    • pp.549-556
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    • 2003
  • Various researches on the application of polymer dispersions to the cement mortar and concrete have been practised in many countries like America, Japan and Germany and so on because of high performance and good modification effect of these. In this study, SBR, Polymer dispersion that widely used in situ is employed that the self-flowability may be induced in the cemen mortar. In order to comprehend and investigate the modification of cement mortar with self-flowability by SBR and properties and fracture mode of adhesive strength in tension of that, experimental parameter was set as SBR solid-Cement ratio(S/C) and Cement:Fine aggregate(C:F) and the experiments such as Unit weight, Flow, Consistency change, Crack resistance and Segregation that inform on the general properties have been done. In addition of that, Adhesion in tension is measured with a view to comprehending the properties and fracture mode in tensile load. Consistency change of cement mortar modified by SBR did grow better as the ratio of SBR solid-Cement increased and was much superior to that of resin based flooring such as polyurethane and epoxy which recorded the loss of consistency in 90min. after mixing. Adhesive strength in tension increased with continuity in the curing age and showed the maximum in case of C:F=1:1 and S/C=20%. As the increase of curing age, the fracture mainly happened in the concrete substrate and the interface between the specimen and concrete substrate.

The Effect of Carbide Precipitation on the High Temperature Deformation of Ni3Al and TiAl

  • Han, Chang-Suk;Kim, Jang-Woo;Kim, Young-Woo
    • Korean Journal of Metals and Materials
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    • v.47 no.3
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    • pp.147-154
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    • 2009
  • The effect of carbon addition on the microstructures and mechanical properties of $Ni_3Al$ and TiAl intermetallic alloys have been characterized. It is shown that carbon is not only an efficient solid solution strengthener in $Ni_3Al$ and TiAl, it is also an efficient precipitation strengthener by fine dispersion of carbide. Transmission electron microscope investigation has been performed on the particle-dislocation interactions in $Ni_3Al$ and TiAl intermetallics containing various types of fine precipitates. In an $L1_2$-ordered $Ni_3Al$ alloy with 4 mol.% of chromium and 0.2~3.0 mol.% of carbon, fine octahedral precipitates of $M_{23}C_6$ type carbide, which has the cube-cube orientation relationship with the matrix, appear during aging. Typical Orowan loops are formed in $Ni_3Al$ containing fine dispersions of $M_{23}C_6$ particles. In the L10-ordered TiAl containing 0.1~2.0 mol.% carbon, TEM observations revealed that needle-like precipitates, which lie only in one direction parallel to the [001] axis of the $L1_0$ matrix, appear in the matrix and preferentially at dislocations. Selected area electron diffraction (SAED) patterns analyses have shown that the needle-shaped precipitate is $Ti_3AlC$ of perovskite type. The orientation relationship between the $Ti_3AlC$ and the $L1_0$ matrix is found to be $(001)_{Ti3AlC}//(001)_{L10\;matrix}$ and $[010]_{Ti3AlC}//[010]_{L10\;matrix}$. By aging at higher temperatures or for longer period at 1073 K, plate-like precipitates of $Ti_2AlC$ with a hexagonal structure are formed on the {111} planes of the $L1_0$ matrix. The orientation relationship between the $(0001)_{Ti2AlC}//(111)_{L10\;matrix}$ is and $[1120]_{Ti2AlC}//[101]_{L10\;matrix}$. High temperature strength of TiAl increases appreciably by the precipitation of fine carbide. Dislocations bypass the carbide needles at further higher temperatures.