• Title/Summary/Keyword: Water-soluble Polymer

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Radiation Technology in the Preparation of Polyethylene Oxide Hydrophilic Gels and Immobilization of Proteases for Use in Medical Practice

  • E.I.Vereschagin;Han, Do-Hung;A.W.Troitsky;O.V.Grishin;S.E.Petrov;E.P.Gulyaeva;L.A.Bogdanova;M.V.Korobeinikov;V.L.Auslender
    • Archives of Pharmacal Research
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    • v.24 no.3
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    • pp.229-233
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    • 2001
  • This Paper deals with the development of a technology for making a hydrophilic gel of Polyethylene oxide reception in which radiating ability is employed to cause cross-linking of Polymers in a water solution. The gel of polyethylene oxide was shown to be nontoxic contain 5-50% of polymer and be useful in composite medicinal forms along with biologically active substances including Bac. subtilis proteases. Proteases immobilized in the gel possess high thermal stability and proteolytic activity and are readily applied in medicine. The effect of immobilized proteolytic and glucolytic enzymes of Bac. subtillis (Immozimase) on the warm ischemia-reperfusion (I/R) which can cause hepatic and jejunum injury was also studied. These enzymes were immobilized on water-soluble polymer polyethylene glycol by means of an electron beam. The number of degraanulated mast cells as well as serum ALT after I/R in the group with Immozimase was decreased to almost half as compared with the control group. Pretreatment with Immozimase resulted in significant reduction of hepatic and gut neutrophil accumulation as compared with control animals. It was concluded that Immozimase has a protective effect for hepatic and gut ischemia/reperfusion, and this effect seems to be associated with prevention of leukocyte accumulation .

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Preparation of Lipid Nanoparticles Containing Paclitaxel and their in vitro Gastrointestinal Stability (파클리탁셀을 함유한 지질나노입자의 제조와 인공 소화액에서의 안정성 평가)

  • Kim, Eun-Hye;Lee, Jung-Eun;Lim, Deok-Hwi;Jung, Suk-Hyun;Seong, Ha-Soo;Park, Eun-Seok;Shin, Byung-Cheol
    • Journal of Pharmaceutical Investigation
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    • v.38 no.2
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    • pp.127-134
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    • 2008
  • Peroral administration is the most convenient one for the administration of pharmaceutically active compounds. Most of poorly water-soluble drugs administered via the oral route, however, remain poorly available due to their precipitation in the gastrointestinal (GI) tract and low permeability through intestinal mucosa. In this study, one of drug delivery carriers, lipid nanoparticles (LNPs) were designed in order to reduce side effects and improve solubility and stability in GI tract of the poorly water soluble drugs. However, plain LNPs are generally unstable in the GI tract and susceptible to the action of acids, bile salts and enzymes. Accordingly, the surface of LNPs was modified with polyethylene glycol (PEG) for the purpose of improving solubility and GI stability of paclitaxel (PTX) in vitro. PEG-modified LNPs containing PTX was prepared by spontaneous emulsification and solvent evaporation (SESE) method and characterized for mean particle diameter, entrapping efficiency, zeta potential value and in vitro GI stability. Mean particle diameter and zeta potential value of PEG-modified LNP containing PTX showed approximately 86.9 nm and -22.9 mV, respectively. PTX entrapping efficiency was about 70.5% determined by UV/VIS spectrophotometer. Futhermore, change of particle diameter of PTX-loaded PEG-LNPs in simulated GI fluids and bile fluid was evaluated as a criteria of GI stability. Particle diameter of PTX-loaded PEG-LNPs were preserved under 200 nm for 6 hrs in simulated GI fluids and bile fluid at $37^{\circ}C$ when DSPE-mPEG2000 was added to formulation of LNPs above 4 mole ratio. As a result, PEG-modified LNPs improved stability of plain LNPs that would aggregate in simulated GI fluids and bile solution. These results indicate that LNPs modified with biocompatible and nontoxic polymer such as PEG might be useful for enhancement of GI stability of poorly water-soluble drugs and they might affect PTX absorption affirmatively in gastrointestinal mucosa.

Controlled Ondansetron Release Based on Hydroxyethyl Starch Hydroxyethyl Methacrylate

  • Tahir, Muhammad Nazir;Adnan, Ahmad;Cho, Eunae;Jung, Seunho
    • Bulletin of the Korean Chemical Society
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    • v.33 no.12
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    • pp.4035-4040
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    • 2012
  • Presented study describes the synthesis of photo cross-linkable and water soluble hydroxyethyl starch hydroxyethyl methacrylate (HESHEMA) samples with different degree of substitution (DS) by functionalization of hydroxyethyl starch (HES) with hydroxyethyl methacrylate (HEMA) or hydroxyethyl methacrylate carbonylimidazole (HEMACI) in DMSO using two different routes. It was revealed that the reaction time for HESHEMA synthesis can be reduced from 5 days to 24 h by conducting the reaction at $80^{\circ}C$ instead of at room temperature. Solubility of HESHEMA was found to be dependent on DS which in turn was dependent on ratio between HES and HEMA or HEMACI. HESHEMA samples with DS > 0.24 depicted insoluble in water, whereas the samples with DS < 0.05 did not form appreciable gel. HESHEMA samples with appropriate DS were converted into hydrogels by cross-linking polymer chains under UV radiations and resulting HESHEMA hydrogels showed swelling up to 1200%. Application of HESHEMA in controlled drug delivery was investigated by diffusion based encapsulation of Ondansetron, a serotonin 5-$HT_3$ receptor antagonist drug, mainly used for nausea and vomiting treatment.

Filling System Analysis for Cavity in Ground using DEM (개별요소해석을 이용한 지반공동부 주입시스템 분석)

  • Han, Jung-Geun;Kim, Young-Ho;You, Seung-Kyong;Chung, Da-Som
    • Journal of the Korean Geosynthetics Society
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    • v.17 no.1
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    • pp.119-126
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    • 2018
  • The ground cavity occurring in the downtown area is on the increase. However, when ground subsidence is occurred or a cavity that causes it to occur is found, time and economic difficulties are follwed in recovery. In advance, this study conducted to develop filling system for reinforcement material which is consist of polymer pouch and admixture as a new filler material. We developed a polymer pouch that is water soluble in the precedent study. Since the filling system is trenchless method and don't need any plant, it has time and economic benefits. This system uses air pressure to filling out cavity in a short time. We estimate this system with respect to filling speed and filling ratio by model experiment. In addition, we could confirm various filling condition using DEM Analysis. So, we could develop filling system and analysis it.

Oxidative Decomposition of 2, 4, 6-Trichlorophenol Catalyzed by Polymer Supported Metalloporphyins (고분자결합 금속포르피린을 촉매로 한 2, 4, 6-트리클로로페놀의 산화 분해반응)

  • Park, Hye-Ok;Lee, Bo-Young;Rhee Paeng, Insook
    • Analytical Science and Technology
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    • v.14 no.1
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    • pp.72-79
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    • 2001
  • Oxidative decomposition of 2, 4, 6-trichlorophenol(TCP) was studied in aqueous solution. Iron and manganese protoporphyrin [or tetrakis(p-carboxyphenylporphyrin)] and their polymer supported derivatives were used as catalysts, and $KHSO_5$ and tert-butyldroperoxide(TBHP) as oxidants. Metalloporphyrin itself shows very poor catalytic activity in oxidative decomposition of TCP with oxidant. However, very high catalytic activity was observed when metalloporphyrin was chemically bound to newly synthesized polymers or XAD2 resin. Additionally, it revealed much higher catalytic activity in the presence of water-soluble polymers having a electron-donating axial ligand such as pyridine and immidazole. Maleic acid and chloromaleic acid were found in the resulting solution by ESI-MS. Especially, XAD2-supported metalloporphyrins can be reused as catalysts due to insolubility to solvent, and stability against oxidant.

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Phospholipid polymer can reduce cytotoxicity of poly (lactic acid) nanoparticles in a high-content screening assay

  • Kim, Hyung Il;Ishihara, Kazuhiko
    • Biomaterials and Biomechanics in Bioengineering
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    • v.1 no.2
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    • pp.95-104
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    • 2014
  • The objective of this study was to evaluate the cytotoxicity of poly (lactic acid) (PLA) nanoparticles. We used a water-soluble, amphiphilic phospholipid polymer, poly (2-methacryloyloxyethyl phosphorylcholine-co-n-butyl methacrylate) (PMB30W), as a stabilizer for the PLA nanoparticles. The PLA nanoparticles and PMB30W-modified PLA (PLA/PMB30W) nanoparticles were prepared by evaporating tetrahydrofuran (THF) from its aqueous solution. Precipitation of the polymers from the aqueous solution produced PLA and PLA/PMB30W nanoparticles with a size distribution of $0.4-0.5{\mu}m$. The partial coverage of PMB30W on the surface of the PLA/PMB30W nanoparticles was confirmed by X-ray photoelectron spectroscopy (XPS) and dynamic light-scattering (DLS). A high-content automated screening assay (240 random fields per group) revealed that the PLA nanoparticles induced apoptosis in a mouse macrophage-like cell line (apoptotic population: 73.9% in 0.8 mg PLA/mL), while the PLA/PMB30W nanoparticles remained relatively non-hazardous in vitro (apoptotic population: 13.8% in 0.8 mg PLA/mL). The reduction of the apoptotic population was attributed to the phosphorylcholine groups in the PMB30W bound to the surface of the nanoparticle. In conclusion, precipitation of PLA in THF aqueous solution enabled the preparation of PLA nanoparticles with similar shapes and size distribution but different surface characteristics. PMB30W was an effective stabilizer and surface modifier, which reduced the cytotoxicity of PLA nanoparticles by enabling their avoidance of the mononuclear phagocyte system.

BCNU Release Behaviour from BCNU/PLGA Wafer Prepared by Vacuum Drying Method (진공 건조법에 의해 제조된 BCNU/PLGA웨이퍼의 BCNU 방출거동)

  • Park, Jung-Soo;Shin, Joon-Hyun;Lee, Doo-Hee;Rhee, John-M.;Kim, Moon-Suk;Lee, Hai-Bang;Khang, Gil-Son
    • Polymer(Korea)
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    • v.31 no.3
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    • pp.201-205
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    • 2007
  • Biodegradable polymers such as polylactide, polyglycolide and poly (lactide- co-glycolide) (PLGA) have been extensively investigated because of easily controlled drug release rate, completely degradable materials without the toxic by-product, and good biocompatibility. But, according to the bulk erosion property of PLGA in vitro test, it had the disadvantage that first-order release reduced releasing amount slowly after excessive initial burst. In this study we used PLGA powder obtained through recrystallization to revise bulk erosion property of PLGA. The PLGA used in this study was prepared by vacuum drying method and to estimate release profiles of BCNU loaded PLGA wafer. We also evaluated the release profile of drug with the water soluble additive. It was found that the drug loaded PLGA recrystallized by vacuum drying method exhibited the initial burst and the constant rate of drug release compared to that prepared by a conventional method.

Debittering of Citrus Products Using ${\beta}-Cyclodextrin$ Polymer and Ultrafiltration Process (${\beta}-Cyclodextrin$ 중합체와 한외여과 공정을 이용한 감귤류의 쓴맛 성분 제거)

  • Woo, Gun-Jo;Ha, Seung-Mi
    • Korean Journal of Food Science and Technology
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    • v.29 no.2
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    • pp.302-308
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    • 1997
  • ${\beta}-Cyclodextrin\;({\beta}-CD)$ polymers were prepared using epichlorohydrin as a cross linking agent. The polymers were separated into ${\beta}-CD$ soluble polymer $({\beta}-CD\;SP)$ and ${\beta}-CD$ insoluble polymer $({\beta}-CD\;ISP)$ on a 10,000 molecular weight cut-off membrane (YM 10). Optimum separation conditions in the YM 10 were: transmembrane pressure 51.7 kPa, separation temperature $35^{\circ}C$, and volume concentration ratio 10. The flux was $0.025\;mL/cm^{2}/min$ under the optimum conditions. Gel permeation chromatography indicated that ${\beta}-CD\;SP\;and\;{\beta}-CD\;ISP$ had a degree of polymerization of $2{\sim}8$ and over 10, respectively. The formation of an inclusion complex with hydrophobic compounds such as 4-dimethylaminoazobenzene, methyl red, and naringin was compared among ${\beta}-CD,\;{\beta}-CD\;SP\;and\;{\beta}-CD\;ISP$. The molar absorptivity for the two chromatic compounds was increased and the absorption peak was shifted in the presence of ${\beta}-CD$ polymers. Naringin, the principal flavonoid bitter tasting component of citrus fruit, had a low water solubility. The solubility of naringin was increased through the formation of an inclusion complex with ${\beta}-CD$ polymers. There was no significant difference in the formation of an inclusion complex between ${\beta}-CD\;SP\;and\;{\beta}-CD\;ISP$. Reduction of the bitter components from citrus products was shown to be possible when employing ${\beta}-CD\;SP$, while the usage of ${\beta}-CD$ monomer has been limited due to the low water solubility.

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The Effects of Osmogant and Binder in Membrane on Nifedipine Release from Osmotic Granule (니페디핀의 삼투성 과립에서 삼투염과 반투막내의 결합제 종류가 약물방출에 미치는 영향)

  • Jeong Sung-Chan;Cho Young-Ho;Kim Moon-Suk;Lee Bong;Khang Gil-Son;Rhee John-M.;Lee Hai-Bang
    • Polymer(Korea)
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    • v.30 no.2
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    • pp.112-117
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    • 2006
  • To improve the type error of osmotic tablet which is one of the drug delivery system, osmotic granule could be manufactured by fluidized bed coating. It has drug layer containing different amount of osmogant and is coated with membrane including different types of binder. We confirmed that the morphology of osmotic granule was different at each coating step. The more mont of osmotic agent, the faster drug release was observed due to increasing the driving force for drug release from osmotic granule. And drug release from osmotic granule coated with membrane using different types of binder was differed by solubility of binders to water. The formation of pore in membrane was confirmed by SEM and DSC Membrane using water soluble binder released more amount of drug. From these results, we assured that difference of osmotic pressure between the inside and the outside of granule and porosity of membrane have an effect on drug release from osmotic granule.

Suspension Polymerization with Hydrophobic Silica as a Stabilizer II. Preparation of Polystyrene Composite Particles Containing Carbon Black (소수성 실리카를 안정제로 하는 현탁중합 II. 카본블랙을 함유하는 폴리스티렌 복합체 입자의 합성)

  • Park, Moon-Soo
    • Polymer(Korea)
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    • v.30 no.6
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    • pp.505-511
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    • 2006
  • We tried to prepare polystyrene composite particles containing carbon black by suspension polymerization with water as a reaction medium. Hydrophobic silica was selected as a stabilizer and oil-soluble azobisisobutyronitrile (AIBN), as an initiator. All polymerization reactions were carried out at a fixed temperature of $75^{\circ}C$. Stabilizer concentration was varied from $0.17{\sim}3.33wt%$ compared to water, where particles with $7.96{\mu}m$ in average diameter were obtained at 1.57 wt% of stabilizer. Increase in divinylbenzene concentration, as a crosslinking agent, from $0.1{\sim}1.0 wt%$ compared to monomer exhibited a large increase in average particle diameter Incorporation of 1wt% of carbon black compared to monomer produced an increase in average diameter It is speculated that viscosity lower than that necessary to induce even dispersion of carbon black particles led to poor dispersion, and as a result, large particles. For a styrene mixture containing 3 wt% carton black compared to monomer, enhanced dispersion due to an increase in carbon black concentration reduced average particle diameters. For styrene mixtures containing 1 and 3 wt% carbon black compared to monomer, preparticles before polymerization and polymer composite particles after polymerization showed a similar tendency towards particle formation. When carbon black concentration compared to monomer was increased to 5 and 7 wt%, styrene mixtures exhibited a large increase in viscosity and thus better dispersion of carbon black particles, which led to a decrease in preparticle diameters. However, these particles experienced agglomeration in the polymerization process, and polystyrene composite particles increased in average diameter.