• 한국식품영양과학회지
• /
• 제32권8호
• /
• pp.1239-1244
• /
• 2003

김치의 과숙성을 조절한 고품질화를 위하여 pH 5.0이하의 산성에서 용해되는 Eudragit E100으로 자몽씨 추출물(GFSE)을 함유한 미세 캡슐을 아세톤/액체 파라핀 방법으로 제조하였다. 분산제로 첨가한 aluminium tristearate의 함량에 따라 89.39∼92.13%의 수율을 나타내었으며, aluminium tristearate의 양에 따라 큰 차이를 보이지 않았다. 첨가한 aluminium tristearate함량이 증가할수록 미세캡슐의 크기는 작아지는 경향을 보였는데, 12%의 aluminium tristearate가 존재할 때, GFSE를 함유한 Eudragit E100 미세캡슐은 200 $\mu\textrm{m}$이상이 50.42%, 150∼200 $\mu\textrm{m}$의 범위 내의 것이 36.11%, 100∼150 $\mu\textrm{m}$ 범위의 것이 11.28%, 100 $\mu\textrm{m}$ 이하의 것이 0.17%의 입자 분포를 나타내었다. Eudragit E100 미세 캡슐은 전자현미경으로 구형으로 관찰되었다. Eudragit E100을 pH를 달리한 완충용액에 저장하였을 때, 함유된 GFSE는 pH 3, 4, 5, 6의 조건에서는 1일 만에 내부의 GFSE가 모두 용출되었고 pH 7에서는 9일 후에 약 70%의 GFSE가 용출되었다. 또한, 김치에 첨가하여 저장하였을 때, GFSE 함유 Eudragit E100 미세캡슐의 양이 증가할수록 저장 기간 2일까지는 김치의 pH 저하를 완화시켰으나, 3일 이후에는 큰 영향을 주지 못하였다. 총균수와 젖산균의 경우에서도 GFSE의 첨가량이 증가할수록 각각 감소하는 경향을 나타내었으나 pH에 의한 엄밀한 방출은 관찰되지는 않았다.

• Journal of Pharmaceutical Investigation
• /
• 제38권2호
• /
• pp.111-117
• /
• 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.

• Food Science and Biotechnology
• /
• 제14권3호
• /
• pp.358-362
• /
• 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.

• Journal of Pharmaceutical Investigation
• /
• 제38권3호
• /
• pp.177-182
• /
• 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.

• 한국생물공학회:학술대회논문집
• /
• 한국생물공학회 2003년도 생물공학의 동향(XIII)
• /
• pp.655-659
• /
• 2003

수용성 약물의 캡슐화 효율을 높이기 위하여 eudragit이 코팅된 SLN을 제조하였고 TEM을 이용하여 그 형태가 양호하게 형성된 것을 확인하였다. DLS를 이용하여 형성된 입자의 분포와 크기를 확인하였으며 옥용산을 포함하는 E-SLN은 ${\pm}180$ nm, ascorbic acid는 ${\pm}150$ nm의 크기를 가지는 것으로 확인되었다. 캡슐화 효율은 옥용산을 경우 41%, ascorbic acid는 33%로 나타났으며, 이는 E-SLN이 수용성 약물을 캡슐화하는 데 유용함을 보여준다.

• KSBB Journal
• /
• 제19권3호
• /
• pp.178-186
• /
• 2004

복합한방 재료인 옥용산에 대해 UV 흡수능, tyrosinase 저해활성 그리고 free radical 소거활성을 측정함으로서 미백활성을 검정하고 비교 시험군으로서 비타민C와 함께 Eudragit 이 코팅된 coconut oil을 이용한 SLN을 제조할 수 있었다. 실험 결과, 옥용산은 UV 영역에서 흡수능을 가지며 tyrosinase 저해 활성과 free radical 소거활성을 가진 것으로 확인되었다. 제조된 E-SLN을 TEM을 이용하여 관찰한 결과 크기 50∼300 nm인 구형의 양호한 입자를 형성하고 있음을 확인하였다. 또한 그 크기분포와 캡슐화 효율 분석을 통해 EUD의 농도가 2.0% (w/v), w/o 비율은 1 ： 9, emulsion과 pour solution의 비율은 1 : 10, 그리고 실온에서 제조한 E-SLN의 캡슐화 효율이 가장 높고 크기의 분포가 가장 양호한 것을 알 수 있었다. E-SLN을 이용하여 in vitro 방출시험을 실시한 결과 E-SLN은 pH와 온도 의존적으로 약물을 방출하는 경향을 나타냈다. 결과적으로 제조된 E-SLN은 pH와 온도 의존적으로 약물을 전달할 필요가 있는 계에 대한 약물전달 시스템으로 적합할 것으로 보인다. 폐쇄 첩포시험과 자외선 조사에 의한 인공색소침착과 시료도포에 의한 미백효능 판정에 의한 임상시험 결과 옥용산과 비타민C, 그리고 이를 포함하는 E-SLN은 대조군의 경우와 비교하여 미백효과를 가지는 것으로 확인되었으며 이는 기능성화장품에의 응용 가능성을 높여주었다.

• KSBB Journal
• /
• 제26권3호
• /
• pp.217-222
• /
• 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.

• Journal of Pharmaceutical Investigation
• /
• 제30권4호
• /
• pp.241-246
• /
• 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.

• Journal of Pharmaceutical Investigation
• /
• 제33권3호
• /
• pp.179-185
• /
• 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.

• Bulletin of the Korean Chemical Society
• /
• 제32권4호
• /
• pp.1298-1302
• /
• 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 $20\;{\mu}gmL^{-1}$.