• Polymer(Korea)
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• v.35 no.6
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• pp.520-525
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• 2011

Superporous hydrogels (SPHs) with fast swelling and superabsorbent properties are useful materials in various biomedical fields, by improving the swelling properties of conventional hydrogels based on their unique porous structure. In this study, Eudragit polymers were used as coating materials to control the swelling properties of poly(acrylic acid-co-acrylamide) based SPHs by environmental pH. The SPHs were coated with Eudragit L100 and S100 that have different pH characteristics as enteric coating materials by a dip coating method, and their pH dependent swelling behaviors were observed in various pH environments. The swelling of SPHs was inhibited at a low pH range, but significantly enhanced above a characteristic pH of Eudragit polymers. This pH dependent swelling behavior of hydrogels could be modulated by the characteristics of the enteric coating polymers.

• Asian-Australasian Journal of Animal Sciences
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• v.26 no.4
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• pp.552-557
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• 2013

Partially purified ${\alpha}$-galactosidase from Bacillus sp. LX-1 was non-covalently immobilized on a reversibly soluble-insoluble polymer, Eudragit L-100, and an immobilization efficiency of 0.93 was obtained. The optimum pH of the free and immobilized enzyme was 6.5 to 7.0 and 7.0, respectively, while there was no change in optimum temperature between the free and immobilized ${\alpha}$-galactosidase. The immobilized ${\alpha}$-galactosidase was reutilized six times without significant loss in activity. The immobilized enzyme showed good storage stability at $37^{\circ}C$, retaining about 50% of its initial activity even after 18 d at this temperature, while the free enzyme was completely inactivated. The immobilization of ${\alpha}$-galactosidase from Bacillus sp. LX-1 on Eudragit L-100 may be a promising strategy for removal of ${\alpha}$-galacto-oligosaccharides such as raffinose and stachyose from soybean meal and other legume in feed industry.

• Korean Chemical Engineering Research
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• v.46 no.2
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• pp.222-226
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• 2008

Nanoparticles have been developed and applied for various applications to intelligently deliver bioactive materials. Herein, lactocin was processed into nanoparticles with methacrylic acid-methyl methacrylate copolymer (1:1) (eudragit L100). The eudragit polymer can protect lactocin from the stomach acid and release lactocin in the intestines. When acetone and pH 7 buffer solution were used as non-solvent and solvent, respectively, the smallest volume-average particle size (290 nm) could be obtained. Freeze drying in presence of carrageenan (dispersant) can process the particles into dried powders with minimum aggregation. SEM observation revealed the primary particles prepared based on lactocin and eudragit were of a few tens of nanometers.

• 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.20 no.1
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• pp.13-18
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• 1990

Hydrocortisone (HC) sustained-release suppositories were prepared by using a solid matrix of methacrylic acid-methacrylic acid methyl ester copolymer $(Eudragit\;L_{100}^{R}:\;EL)$ as a poorly water soluble carrier and polyethylene glycole 1540 (PEG) as an water soluble carrier. HC release rate was controlled by complexation with ${\beta}-cyclodextrin$ $({\beta}-CyD)$ which was confirmed by X-ray diffractometry, IR-spectroscopy and differential scanning calorimetry. Release rate of HC from the EL-PEG matrix suppositories decreased with increase of EL contents. The release rale from $HC-{\beta}-CyD$ complex decreased in the following order: $HC-{\beta}-CyD/PEG$ > HC/PEG > $HC-{\beta}-CyD/EL_{10%}-PEG$ > $HC/EL_{10%}-PEG$ > $HC-{\beta}-CyD/EL_{15%}-PEG$ > $HC/EL_{15%}-PEG$ > $HC-{\beta}-CyD/EL_{20%}-PEG$ > $HC/EL_{20%}-PEG$. The crystallinity of HC in polymer matrix was identified using X-ray diffractometer and the surface of matrix suppositories after release test was examined by scanning electron microscopy. The sustained release of HC from these matrix suppositories was attributed to the network structure of EL.

• 한국생물공학회:학술대회논문집
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• 2003.10a
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• pp.655-659
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• 2003

Solid lipid nanoparticle (SLN) system has been attracted increasing attention during last few years as a potential drug delivery carrier However, the SLN have disadvantage of low encapsulation efficiency for hydrophilic drug. In this study, for increase it's encapsulation efficiency, we prepared the $Eudragit^{\circledR}$ L100-55 (eudragit) coated SLN(E-SLN) based on solvent evaporation method and melt dispersion technique, and analyzed their physicochemical properties in terms of particle size, morphology, and encapsulation efficiency. As a result, they have a ${\pm}150$ nm particle size, spherical shape, and $10^{\sim}25$ % loading efficiency. SLN consists of coconut oil as core material, ascorbic acid and okyong-san as hydrophilic drug.

• Archives of Pharmacal Research
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• v.26 no.7
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• pp.569-574
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• 2003

Controlled-release amitriptyline pellets (ATP) were formulated and its oral bioavailability was assessed in human volunteers after oral administration under fasting conditions. Core pellets were prepared using a CF granulator by two different methods (powder layering and solvent spraying) and coated with Eudragit RS or RL 100. Physical characteristics and dissolution rates of core pellets and coated pellets were evaluated to optimize the formulation. Powder layering method resulted in a better surface morphology than solvent spraying method. However, physical properties of the products were poorer when prepared by powder layering method with respect to hardness, friability and density. The dissolution profile of amitriptyline coated with Eudragit RS 100 was comparable to that of commercially available amitriptyline enteric-coated pellets ($Saroten^{\circledR}$ retard). After the oral administration of both products at the dose of 50 mg, the mean maximum concentrations ($C_{max}$) were 36.4 and 29.7 ng/mL, and the mean areas under the concentration-time curve ($AUC_{0-96}$) were 1180.2 and 1010.7 ng.h/mL for ATP and Saroten retard, respectively. The time to reach the maximum concentrations ($T_{max}$) was 6 h for both formulations. Statistical evaluation suggested that ATP was bioequivalent to Saroten retard.

• Journal of Pharmaceutical Investigation
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• v.35 no.6
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• pp.453-460
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• 2005

4-Aminopyridine (AP) is a potassium channel blocker used in the treatment of neurological disorders such as multiple sclerosis and Alzheimer disease. AP‘s window of therapeutic effect appears to correlate with its plasma halflife (3.5 hours). It demonstrates pH-dependent solubility because of a weakly basic drug. In addition, the resulting release from conventional matrix tablets decreases with increasing pH-milieu of the gastrointestinal tract. The aim of this study is to design sustained release matrix tablet containing AP, overcoming this problem. $Eudragit^{\circledR}$ L 100 (EuL) and sodium alginate were used in an effort to achieve pH independent drug release. The effect of sodium alginate and EuL on drug release from matrix tablet was investigated. The drug release behavior from the different tablets was analyzed by $t_{20%},\;t_{40%},\;t_{60%}$, The exponential diffusion coefficient n, kinetic constant K were calculated according to the Korsmeyer-Peppas equation. The drug release from matrix tablets prepared with sodium alginate was decreased with increasing the content of sodium alginate in pH 7.4 while there is no significant difference in pH 1.2. The exponent n values were determined to be approximately 0.5 and 0.8 respectively, in both pH 1.2 and 7.4. These values indicate diffusion-based anomalous mechanism and erosion-based anomalous mechanism, respectively. The drug release from sodium alginate matrix tablets prepared with solid dispersion of EuL containing drug showed a slow drug release in an acidic medium and a more fast drug release in phosphate medium, compared with sodium alginate matrix tablets prepared with physical mixture. These results may be attributed to the gel forming ability of sodium alginate and pH dependent solubility of EuL. Therefore, sustained-release AP matrix tablets using sodium alginate and EuL were successfully prepared.

• Archives of Pharmacal Research
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• v.28 no.6
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• pp.736-742
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• 2005

Xyloglucan (XG), which exhibits thermal sol to gel transition, non-toxicity, and low gelation concentration, is of interest in the development of sustained release carriers for drug delivery. Drug-loaded XG beads were prepared by extruding dropwise a dispersion of indomethacin in aqueous XG solution (2 wt.-$\%$) through a syringe into corn oil. Enteric coating of XG bead was performed using Eudragit L 100 to improve the stability of XG bead in gastrointestinal (GI) track and to achieve gastroresistant drug release. Release behavior of indomethacin from XG beads in vitro was investigated as a function of loading content of drug, pH of release medium, and concentration of coating agent. Adhesive force of XG was also measured using the tensile test. Uniform-sized spherical beads with particle diameters ranging from 692 $\pm$ 30 to 819 $\pm$ 50 $\mu$m were obtained. The effect of drug content on the release of indomethacin from XG beads depended on the medium pH. Release of indomethacin from XG beads was retarded by coating with Eudragit and increased rapidly with the change in medium pH from 1.2 to 7.4. Adhesive force of XG was stronger than that of Carbopol 943 P, a well-known commercial mucoadhesive polymer, in wet state. Results indicate the enteric-coated XG beads may be suitable as a carrier for oral drug delivery of irritant drug in the stomach.

• KSBB Journal
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• v.19 no.3
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• pp.178-186
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• 2004

The aim of this study was to investigate the skin-whitening effect of okyong-san and to develop new drug delivery carrier The extracts of okyong-san were found to have the whitening effect and Eudragit$\^$ⓡ/ L 100-55 (EUD) coated solid lipid nanoparticle (E-SLN) was prepared by solvent evaporation method and melt dispersion technique. As a result, E-SLN have a 144-170 nm of particle size, spherical shape, and 33-41% encapsulation efficiency, After release test in vitro, release profile of E-SLN depended on pH and temperature. Lastly, closed patch test and skin-whitening test was peformed clinically. In conclusion, test sample had non-stimulation and high % whiteness. The results suggest that okyong-san and E-SLN is useful as cosmeceuticals for whitening cosmetics.