• Journal of Adhesion and Interface
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• v.2 no.4
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• pp.10-23
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• 2001

In order to increase the lower values of % grafting and monomer conversion in the emulsion graft polymerization of methylmethacrylate(MMA) onto sodium alginate (SA; a polymer electrolyte) with alginic acid-g-PMMA, the graft polymerization with water soluble (methanol and acetone) and insoluble solvents was carried out using a varity of solvent amounts and agitating rates. And some physical properties of the graft polymer were also investigated. In the polymerizations with water insoluble solvent, there were pronounced improvements in both % grafting and MMA conversion by the promotion of MMA diffusion from the core to the SA adsorpted on the outer layer of particle and that of MMA complex formation with SA. And the effect was larger for the solvents (cyclohexane, decalin) which do not dissolve PMMA. On the other hand, in the polymerization with water soluble solvent, there was an significant increase in MMA conversion and a considerable increase in the % grafting by the destruction of electrical double layer around the SA chains, abstracting the hydrated water in the layer and the effect was more potential in the case of methanol which is a precipitant of PMMA.

• Journal of Pharmaceutical Investigation
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• v.38 no.4
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• pp.249-254
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• 2008

Solid dispersions of poorly water-soluble drug, atorvastatin, were prepared with Eudragit L100 to improve the solubility by spray dryer. To investigate the correlation between physicochemical properties and dissolution rate of solid dispersions, the samples were characterized by scanning electron microscopy (SEM), differential scanning calorimeter (DSC) and fourier transform infrared spectroscopy (FT-IR). SEM and DSC were found that atorvastatin is amorphous in the Eudragit L100 solid dispersion. FT-IR was used to analyze the salt formation by interaction between atorvastatin and Eudragit L100. The dissolution rate of solid dispersed atorvastatin was markedly increased compared to drug powder in stimulated intestinal juice (pH 6.8). Thus, the solid dispersed atorvastatin using the spray drying method with Eudragit L100 may be effective for the bioavailability.

• Journal of Pharmaceutical Investigation
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• v.37 no.6
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• pp.339-347
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• 2007

SMEDDS is mixture of oils, surfactants, and cosurfactants, which are emulsified in aqueous media under conditions of gentle agitation and digestive motility that would be encountered in the gastro-intestinal(GI) tract. The main purpose of this work is to prepare self-microemulsifying drug delivery system(SMEDDS) for oral bioavailability enhancement of a poorly water soluble drug, atorvastatin calcium. Solubility of atorvastatin calcium was determined in various vehicles. Pseudo-ternary phase diagrams were constructed to identity the efficient self-emulsification region and particle size distributions of the resultant micro emulsions were determined using a laser diffraction sizer. Optimized formulations for in vitro dissolution and bioavailability assessment were $Capryol^{(R)}$ 90(50%), Tetraglycol(16%), and $Cremophor^{(R)}$ EL(32%). The release rate of atorvastatin from SMEDDS was significantly higher than the conventional tablet ($Lipitor^{(R)}$), 2-fold. Our studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as atorvastatin calcium by the oral route.

• Polymer(Korea)
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• v.34 no.6
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• pp.501-506
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• 2010

Natural chitosan has high molecular weight and the poor solubility in water. Water-soluble chitosan with low molecular weight was prepared by the hydrolysis method. In order to develop an efficient gene delivery carrier, chitosan was conjugated with lipoic acid to form the comb-type copolymer. The copolymer with the amphiphilic property formed the self-assembled nanoparticles in the aqueous solution. The average size of nanoparticles was 217.6 nm and the average size of nanoparticles/DNA complex was 170 nm. New chitosan-lipoic acid copolymer showed the low cytotoxicity and 10 times higher transfection efficiency than that of the pure chitosan.

• Journal of Pharmaceutical Investigation
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• v.22 no.2
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• pp.105-113
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• 1992

To improve the solubility and dissolution rate of trimethoprim (TMP), which is slightly soluble drug, its inclusion complexes were prepared and studied in this experiment. Inclusion complexes of TMP with ${\beta}-cyclodextrin$ and ${\beta}-cyclodextrin$ polymer (CDPS) were prepared according to Fenyvesi method. These were compared with TMP and its physical mixture with CDPS. Water, diluted hydrochloric acid and phosphate buffer solution were used as dissolution media. And accelerated stability test was studied at $50,\;70\;and \;80^{\circ}C$. It was found that solubility and dissolution rate of inclusion complexes were increased in water. Especially, the solubility and dissolution rate of TMP was found to be markedly increased by inclusion complexation with CDPS. In stability test, ${\beta}-cyclodextrin$ inclusion complexes were more or less stable than TMP alone. This tendency was not led in CDPS. Consequently, CDPS was useful in increasing dissolution rate and stability of TMP.

• Polymer(Korea)
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• v.27 no.5
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• pp.405-412
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• 2003

Poly(vinyl alcohol) (PVA) and N-(2-hydroxy)propyl-3-trimethylammonium chitosan chloride (HTCC), a water soluble chitosan derivative synthesized by the reaction of quaternary ammonium compound with chitosan, were blended using water as a solvent and the PVA/HTCC blend films with various compositions were prepared by solution casting method. The miscibility between the two polymers and the thermal properties of the blend films were investigated using FT-IR, DSC, DMA, and TGA. Single glass transition temperatures and single melting temperatures of the blend films along with the strong and clear film state for the whole composition of blending ratios suggest the miscibility between PVA and HTCC. The PVA/HTCC blend films with HTCC content of 1% and greater showed excellent antimicrobial activity.

• Polymer(Korea)
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• v.27 no.4
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• pp.370-376
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• 2003

Poly(DL-lactide-co-glycolide) nanoparticles were prepared by the modified spontaneous emulsification solvent diffusion method. Polymer solution was prepared by two water-soluble organic solvents, such as ethanol and acetone. Because of its biocompatible nature, PEG-PPG diblock copolymer was used as surfactant and stabilizer. The influence of several preparative variables on the nanoparticle formation, such as type and concentration of stabilizing agent, stirring methods, water/oil phase ratio and polymer concentration were investigated in order to control and optimize the process. After preparation of nanoparticles, particle size and distribution were evaluated by the light scattering particle analyzer. As results, the particle size was 50-200 nm and dispersibility was monodisperse. It was found that the appropriate selections of binary solvent mixtures and polymeric concentrations in both organic and aqueous phases could provide a good yield and favorable physical properties of PLGA nanoparticles.

• Journal of the Korean Chemical Society
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• v.53 no.5
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• pp.547-552
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• 2009

Chitosan, a natural polymer, has been importantly considered as biomedical materials due to its good biocompatibility and various bio-active characteristes. Water soluble chitosan was then copolymerized EGDMA(ethylene glycol dimethacrylate; used as a cross-linking agent for the free-radical copolymerization), MMA (methylmethacrylate), MA (methacrylic acid) in the presence of AIBN (azobisisobutyronitrile) as a radical initiator. The water content and visible transmissibility, ultimate strength of copolymerized ophthalmic polymer were measured to be 24$\sim$59%, 88$\sim$89% and 0.1$\sim$2.4 Kgf, respectively. And also, we tested for antimicrobial activities against staphylococcus aureus, Pseudomonas aeruginosa. They showed that in case of antimicrobial activities, the values including chitosan were much higher than that of the polymers of no including chitosan, suggesting that the copolymer can be used as a novel ophthalmic material of high performance.

• Polymer(Korea)
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• v.39 no.3
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• pp.403-411
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• 2015

A series of hydrophobically associating fluorinated amphiphilic polyacrylamide copolymers with remarkably high heat resistance and salt tolerance were synthesized by free radical micellar copolymerization, using acrylamide (AM) and sodium 2-acrylamido-tetradecane sulfonate ($AMC_{14}S$) as amphiphilic monomers, and 2-(perfluorooctyl) ethyl acrylate (PFHEA) as hydrophobic monomer. The structure of the terpolymer was characterized by FTIR, $^1H$ NMR and $^{19}F$ NMR. The solution properties of the terpolymers were investigated in details, and the results showed that the terpolymer solution had strong intermolecular hydrophobic association as the concentration exceeded the critical association concentration 1.5 g/L. The terpolymer solution possessed high surface activity, viscoelasticity, excellent heat resistance, salt tolerance and shearing resistance. The viscosity retention rate of copolymer solution was as high as 59.9% under the condition of fresh wastewater, $85^{\circ}C$ and a 60-days aging test.

• Bulletin of the Korean Chemical Society
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• v.32 no.5
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• pp.1587-1592
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• 2011

The aim of the present study was to improve the solubility and bioavailability of a poorly water-soluble drug in human body, using a solid dispersion technique (hot melt extrusion). The solid dispersion was prepared by cooling the hot melt of the drug in the carrier (Vitamin E TPGS and PVP). The dissolution rate of formulation 1 from a novel formulation prepared by solid dispersion technique was equal to release of formulation 6 (40% of eprosartan mesylate is in contrast to teveten$^{(R)}$) within 60 min (Table 1). The oral bioavailability of new eprosartan mesylate tablet having vitamin E TPGS and PVP K29 was tested on rats and dogs. Of the absorption enhancer and polymer tested, vitamin E TPGS and PVP K29, resulted in the greatest increases of AUC in animals (about 2.5-fold increase in rat and dog). When eprosartan mesylate was mixed with the absorption enhancer and polymer in a ratio of 2.94:2:1, vitamin E TPGS and PVP K29 improved eprosartan mesylate bioavailability significantly compared with the conventional immediate release (IR) tablet Teveten$^{(R)}$ (formulation 7). These results show that solid dispersion using vitamin E TPGS and PVP K29 is a promising approach for developing eprosartan mesylate drug products.