• Title/Summary/Keyword: Eudragit E100

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Preparation and Effect of Eudragit E100 Microcapsules Containing Grapefruit Seed Extract on Kimchi (자몽씨 추출물을 함유한 Eudragit E100 미세캡슐의 제조 및 김치에 대한 영향)

  • 김한수;정성기;조성환;구재관;이승철
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.32 no.8
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    • pp.1239-1244
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    • 2003
  • Microcapsules were prepared by coacervation method using acetone/liquid paraffin system to control the ripening of kimchi. Eudragit E100, which was soluble at below pH 5.0 in aqueous solution, was used to make microcapsules to be sensitive to acidity of kimchi. The microcapsules with Eudragit E100 containing grapefruit seed extract (GFSE) showed the highest yield of 92.13%, the size of microcapsules was decreasing as increasing the amount of aluminium stearate, a dispersing agent. Morphology of the microcapsules determined by scanning electron microscopy showed spherical forms. GFSE, encapsulated antimicrobial agents, was quickly released at acidic buffer (pH 4,5,6) within 1 storage day. However, 70% of encapsulated GFSE in Eudragit E100 microcapsules was continuously released at pH 7 till 3 days, and it was sustained till 9 days. Characteristics of kimchi containing microcapsules of GFSE were analysed with ripening period. Decease of pH in kimchi was retarded with the added GFSE microcapsules till 2 days of fermentation, but GFSE did not affect pH in kimchi after 3 days. Total numbers of microorganisms and lactic acid microorganisms in kimchi were decreased with increasing the amount of the added GFSE microcapsules, however, the effect of controlled released GFSE from pH sensitive Eudragit E100 microcapsules was hard to detect. These results suggest the possibility of pH sensitive microcapsules for high qualify of kimchi.

Improved Dissolution and Characterization of Solid Dispersed Atorvastatin Calcium (아토르바스타틴 칼슘 고체분산체의 특성화 및 용출율 개선)

  • Lee, Jun-Hee;Ku, Jeong;Park, Jung-Soo;Park, Jong-Hak;Ahn, Sik-Il;Mo, Jong-Hyun;Kim, Yun-Tae;Rhee, John-M.;Lee, Hai-Bang;Khang, Gil-Son
    • 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.

Evaluation of pH-sensitive Eudragit E100 Microcapsules Containing Nisin for Controlling the Ripening of Kimchi

  • Ko, Sung-Ho;Kim, Han-Soo;Jo, Seong-Chun;Cho, Sung-Hwan;Park, Wan-Soo;Lee, Seung-Cheol
    • Food Science and Biotechnology
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    • v.14 no.3
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    • pp.358-362
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    • 2005
  • Eudragit E100 microcapsules containing nisin were prepared and employed to control the ripening of kimchi. The recovery yields of microcapsules without/with nisin ranged from 93.53 to 94.61 % and 92.85 to 94.09 %, respectively. The particle size of microcapsules decreased (>200 to $100\;{\mu}m$) as the amount of aluminium tristearate increased from 6.0 to 15 %. The microcapsules were morphologically spherical and possessed rough surface. Nisin was completely released from the microcapsules within a day at pH 3.0 and within two days at pH 4.0, 5.0, and 6.0, respectively, whereas half the amount of nisin was released at pH 7.0 within two days. During fermentation of kimchi with microcapsules containing nisin, the pH decrease was retarded which resulted in a constant pH of approximately 4.2. The pH of 4.2 was optimal for ripening of kimchi for a longer period of time when compared with samples without nisin.

Controlled Release of Three Nutrients from Dual-layered Coated Compact Pellets (이중 코팅된 압착 펠렛으로부터 3종 영양소의 방출 제어)

  • Piao, Zong-Zhu;Lee, Eung-Seok;Choi, Yun-Jaie;Lee, Beom-Jin
    • Journal of Pharmaceutical Investigation
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    • v.38 no.3
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    • pp.177-182
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    • 2008
  • The purposes of this study were to prepare dual-layered coated compact pellets containing three nutrients Glucose, Chromium picolinate, Vitamin C) for rumen bypass. The core compact pellets were prepared by an extrusionspheronization method and then double layered coated with pH independent EC (ethyl cellulose) and pH-dependent polymers ($Eudragit^{(R)}$ E100) using a fluid-bed spray coater. Depending on the coating levels of EC and $Eudragit^{(R)}$ E100, release profiles were variable in simulated rumen (pH 6.8) and abomasums (pH 2.0) fluid using USP apparatus I (basket method). When compact pellets were coated with EC (about 10% level in inner layer) and then $Eudragit^{(R)}$ E100 (20% level in outer layer) in a dual-layered manner, rumen-bypass delivery resisting rumen fluid followed by release in abomasums fluid could possible. The friability was also satisfactory based on chewing behavior of ruminants. The dual-layered coated compact pellets showed smooth surface and distinct inner/outer layers using scanning electron microscopy (SEM). The current rumen bypass delivery system can be also applicable to deliver other nutrients in ruminants.

Preparation of Eudragit coated solid lipid nanoparticles (SLN) for hydrophilic drug delivery

  • Han, Sung-Chul;Yoon, Hee-Sun;Lee, Ki-Young;Kim, Yeon-Zu;Kim, Dong-Woon
    • 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.

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Preparation and Application of Wnitening Ingredient Entrapped in Solid Lipid Nanoparticle [SLN] (미백성분이 포함된 나노입자의 제조와 응용)

  • 한성철;김연주;이기영;김동운
    • 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.

The Microsponge Delivery System of Itraconazole: Preparation, Characterization and Release Studies (이트라코나졸 마이크로스폰지의 약물 전달 시스템: 제조, 특성 및 방출 연구)

  • Cho, Young-Ho;Lee, Jong-Hwa;Kim, Hak-Hyung;Lee, Gye-Won
    • KSBB Journal
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    • v.26 no.3
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    • pp.217-222
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    • 2011
  • Itraconazole is a triazole antifungal agent to inhibit most fungal pathogens. To improve the oral absorption and dissolution of poorly water-soluble itraconazole, microsponge system composed of $Eudragit^{(R)}$ E100 and polyvinyl alcohol(PVA) formulated by quasi-emulsion solvent diffusion method, and its physicochemical properties and pharmacokinetic parameters of itraconazole were studied. The microsponge of itraconazole were discrete free flowing micro sized particles with perforated orange peel like morphology as visualized by scanning electron microscope (SEM). Results showed that the drug loading efficiency, production yield, and particle size of itraconazole microsponge were affected by drug to polymer ratio, the volume of internal phase containing methylene chloride, stirring rate and the concentration of PVA used. Also, the results showed that the dissolution rate of itraconazole from the microsponges was affected by drug to polymer ratio. In other words, the release rate of itraconazole from microsponges was increased from at least 27.43% to 64.72% after 2 h. The kinetics of dissolution mechanism showed that the dissolution data followed Korsmeyer-Peppas model. Therefore, these results suggest that microsponge system can be useful for the oral delivery of itraconazole by manipulating the release profile.

Pharmacokinetic Evaluation of Ketorolac Tromethamine Sustained-Release Pellets after Oral Administration in Rabbits (케토롤락트로메타민 서방성 펠렛의 약물속도론적 평가)

  • Kwak, Son-Hyok;Hwang, Sung-Joo;Jiang, Ge;Nam, Kyung-Wan;Moon, Young-Girl;Lee, Hai-Bang;Cho, Sun-Hang;Yuk, Soon-Hong;Lee, Han-Koo;Jeong, Sang-Young;Lee, Young-Won
    • Journal of Pharmaceutical Investigation
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    • v.30 no.4
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    • pp.241-246
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    • 2000
  • To develop a sustained-release preparation containing ketorolac tromethamine, two sustained-release pellet formulations were evaluated with a pharmacokinetic study as compared with a conventional commercial tablets (10 mg $Tarasyn^{TM}$, Roche Korea Ltd.). Two sustained-release formulations were as follows; formulation A was composed of an inner layer containing 75% of drug coated with $Eudragit^{TM}$ RS 100 membrane and an outer layer containing 25% of drug mixed with $Eudragit^{TM}$ NE30D, and formulation B was composed of only an inner layer containing 100% of drug coated with $Eudragit^{TM}$ RS 100 membrane. The dissolution test was performed for two formulations. In case of conventional tablets, 2.5 mg of drug per a dose was administered orally into male Albino rabbit (2.0-2.3 kg of body weight) 3 times at intervals of 4 hours. In case of two sustained formulations, 7.5 mg of drug was administered once orally. Blood samples were withdrawn periodically after the administration, and the blood concentration was determined by HPLC. The conventional tablets showed very high peak-trough fluctuation between administered doses, but two sustained formulations showed less fluctuation. Formulation A with the loading dose showed the time to reach minimum effective concentration (MEC) i.e. the onset time was less than 20 min, while Formulation B had more than 1 hr of the onset time. Formulation A had the more constant plasma level than formulation B. However, formulation B had a time lag, so the plasma level was less than MEC for an initial period of 1 hr. In formulation A, the plasma level was maintained within the therapeutic window $(0.3-5\;{\mu}g/ml)$ for a long period. Formulation A was thought to be an ideal sustained-release formulation for ketorolac tromethamine oral delivery system.

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Release and Characterization of Multiple Coated Pellets Containing Melatonin (멜라토닌이 함유된 다층 코팅 펠렛의 방출 및 특성분석)

  • Kang, Bok-Ki;Khang, Gil-Son;Kim, Jong-Min;Jeung, Sang-Young;Lee, Hai-Bang;Cho, Sun-Hang
    • Journal of Pharmaceutical Investigation
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    • v.33 no.3
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    • pp.179-185
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    • 2003
  • Melatonin (MT) is an indole amide pineal hormone. It has not only very short half-life but also pH-sensitive property. The sustained release dosage form which delivers MT in a circadian fashion over 8 h is clinical value. The purpose of this study is to prepare sugar beads using multiple coating methods and enteric-coated in a sustained release to evaluate in vitro release characteristics in simulated gastric and intestinal fluids. The $Eudragit^{\circledR}$ as a polymer, sustained release membrane, and triethylcitrate (TEC) as a plasticzer were used. Multi-coated melatonin delivery system was composed of sugar, various excipients, $Eudragit^{\circledR}$ and enteric materials (e.g. hydroxy propyl methyl cellulose phthalate, HPMCP), and prepared by fluid bed coater. The dissolution test was carried out using the basket method at a stirring speed of 100 rpm at $37^{\circ}C$ in simulated gastric (pH 1.2) and intestinal fluid (pH 7.4). The released amount of MT was determined by High performance liquid chromatography method. The morhologies of surface and cross section of multi-coated beads were observed by scanning electron microscope. Size of multi-coated sugar beads was ranged over $1000{\sim}1300\;{\mu}m$. The release rate of MT from coated beads was limited in simulated gastric fluid (pH 1.2), but it was sustained in intestinal fluid (pH 7.4) during $3{\sim}8$ hours. The MT beads may provide small-intestine-targeted device for oral delivery. Studies on animal and relative experiment are in process.

An Electrochemical Enzyme Immunochip Based on Capacitance Measurement for the Detection of IgG

  • Yi, Seung-Jae;Choi, Ji-Hye;Kim, Hwa-Jung;Chang, Seung-Cheol;Park, Deog-Su;Kim, Kyung-Chun;Chang, Chulhun L.
    • Bulletin of the Korean Chemical Society
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    • v.32 no.4
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    • pp.1298-1302
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    • 2011
  • This study describes the development of an electrochemical array immunochip for the detection of IgG. Interdigitated immunochip platforms were fabricated by sputtering gold on a glass wafer by using MEMS process and then were coated with Eudragit S100, an enteric polymer, forming an insulating layer over the working area of immunochips. The breakdown of the polymer layer was exemplified by the catalytic action of urease which, in the presence of urea, caused an alkaline pH change. This subsequently caused an increase of the double layer capacitance of the underlying electrode. Used in conjunction with a competitive immunoassay format, this allowed the ratio of initial to final electrode capacitance to be directly linked with the concentration of analyte, i.e. IgG. Responses to IgG could be detected at IgG concentration as low as $250\;ngmL^{-1}$ and showed good linearity up to IgG concentration as high as $20\;{\mu}gmL^{-1}$.