• 약학회지
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• 제45권5호
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• pp.536-544
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• 2001

increase the viability of oral typhoid vaccine during the passage through the castro-intes-tidal tract, numerous attempts have been made including the vaccine coating. However problems such as high death rate during the coating process and its instability in the gastric juice still remain to be solved. In this study, the oral vaccine was made as the micro-enteric beads by adding Salmomella typhi Ty21a cells to sodium alginate solution and spraying onto calcium chloride solution (ionotropic relation method). The vaccine showed more than 90% of its original viability after treating it for 1 hour in the artificial gastric juice (37$^{\circ}C$, 300 rpm). The clearance rate of the Ty21a in the liver and spleen of the mice orally administrated with coated Ty21a was similar to that of the mice intraperitoneally administrated with uncoated Ty21a. The peripheral blood lymphocytes (PBL) isolated from the mice orally administered with this vaccine produced 15.5 fold higher specific IgA antibody titer than that from the control mice administerd with saline solution. furthermore, the mice treated with the coated Ty21a had higher survival rates (50~87%) than the control mice treated with saline solution (0~10%) in the intraperitoneal challenge test with wild type S. typhi Ty21a cells. These results suggest that the alginate-based coating technique is effective to protect live Ty21a from acidic environments, and produces better intestinal immune responses thereby providing a potentially excellent oral typhoid vaccine.

• 폴리머
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• 제35권6호
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• pp.520-525
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• 2011

초다공성 하이드로젤은 다공성 공극구조를 이용하여 기존 수화젤의 팽윤성을 획기적으로 향상시킨 것으로, 빠른 팽윤거동과 높은 흡수율로 다양한 의약용 응용분야에 유용한 재료이다. 본 연구에서는 장용 코팅제인 Eudragit 계열 고분자들을 사용하여 poly(acrylic acid-co-acrylamide)계 초다공성 하이드로젤을 코팅함으로써 pH 의존성 팽윤거동을 보이는 초다공성 하이드로젤을 제조하고자 하였다. 서로 다른 pH 영역에서 작용하는 Eudragit L100과 S100을 이용하여 딥 코팅에 의해 표면을 코팅한 후 SEM을 이용해 공극구조를 관찰하고 pH에 따른 초다공성 하이드로젤의 팽윤거동을 관찰하였다. Eudragit 계열 고분자들로 코팅된 하이드로젤은 낮은 pH 환경하에서는 팽윤이 억제되다가, 특정 pH 이상에서 팽윤성이 향상되는 pH 의존성 팽윤거동을 보였고, 이러한 pH 의존성은 사용한 장용 코팅제용 고분자들의 pH 특성에 의존하였다.

• 한국식품과학회지
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• 제34권5호
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• pp.856-861
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• 2002

유산균의 활용성을 증진시키기 위한 방안으로서 건식 Hybridization system을 이용하여 장용성 피복재로 유산균분말의 표면처리를 실시하였다. 전자현미경 관찰 결과 표면처리는 유산균의 표면을 매끄러운 구형의 모양으로 변화시켰으며 표면처리를 통한 분체복합화 과정에서 유산균의 활력은 유의적인 변화없이 유지되었다. 또한 유산균의 내염성은 처리여부에 따른 유의적 변화를 보이지 않음으로써 표면처리 과정 중 유산균 세포막의 물리적 손상은 일어나지 않은 것으로 판단된다. 표면처리된 유산균의 내산성은 처리전후에 차이를 나타내지 않았으나 이는 균주 자체의 높은 내산성에 기인한 것으로 판단된다. 표면처리 후의 유산균은 유의적으로 높은 열저항성을 보여 표면처리가 유산균의 내열성 향상을 위하여 활용될 수 있는 가능성을 나타냈다. 조사된 장용성 피복재 중 Sureteric은 다른 피복재에 비하여 우수한 표면 처리 효과를 보였으며 유산균분말의 표면처리를 위한 적합한 처리조건은 유산균의 초기입도가 $100{\sim}200\;{\mu}m$, 유산균:피복재의 혼합비율(w/w)은 9 : 1, 처리속도는 15,000 rpm, 3분이었다.

• Archives of Pharmacal Research
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• 제27권1호
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• pp.118-126
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• 2004

The aqueous extract of European mistletoe (Viscum album, L.) has been used in cancer therapy. The purified mistletoe lectins, main components of mistletoe, have demonstrated cytotoxic and immune-system-stimulating activities. Korean mistletoe (Viscum album L. coloratum), a subspecies of European mistletoe, has also been reported to possess anticancer and immunological activities. A galactose- and N-acetyl-D-galactosamine-specific lectin (Viscum album L. coloratum agglutinin, VCA) with Mr 60 kDa was isolated from Korean mistletoe. Mistletoe preparations have been given subcutaneously due to the low stability of lectin in the gastrointestinal (GI) tract. In the present study, we investigated the possibility of alginate/chitosan microcapsules as a tool for oral delivery of mistletoe lectin. In addition, our strategy has been to develop a system composed of stabilizing cores (granules), which contain mistletoe lectin, extract or powder, coated by a biodegradable polymer wall. Our results indicated that successful incorporation of VCA into alginate/chitosan microcapsules has been achieved and that the alginate/chitosan microcapsule protected the VCA from degradation at acidic pH values. And coating the VCA with polyacrylic polymers, Eudragit, produced outstanding results with ideal release profiles and only minimal losses of cytotoxicity after manufacturing step. The granules prepared with extract or whole plant produced the best results due to the stability in the extract or whole plant during manufacturing process.

• Journal of Pharmaceutical Investigation
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• 제33권3호
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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.

• Archives of Pharmacal Research
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• 제28권6호
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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.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.297.1-297.1
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• 2003

Organic solvent-based enteric coating technology using hydroxypropyl methylcellulose phthalate (HPMCP) has been developed for many years due to low water solubility of HPMCP. In this work, aqueous HPMCP nanoparticles (HPMCP-NPs) were prepared by neutralization emulsification method using HPMCP powder and ammonium hydroxide (NH40H) in the absence of any organic solvent and emulsifier. (omitted)

• Journal of Pharmaceutical Investigation
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• 제30권1호
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• pp.47-50
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• 2000

A new technique has been developed for the preparation of Lactobacillus microcapsules to enhance the stability against high temperature, humidity, gastric acid and bile acid. Employing fluidized bed coating, primary sub-coating was processed in non-organic solvent system, so that Lactobacillus did not directly contact with organic solvent. Secondary enteric-coating was processed in organic solvent with low temperature $(below\;33^{\circ}C)$ technique, which minimized the heat labilability of Lactobacillus. Survival rate of Lactobacillus within microcapsule was not less than 95% and acid tolerance was above 30% in the artificial gastric acid. Further more it was dissolved in the artificial intestine juice within 2-3 hr. Average size of Lactobacillus microcapsules was $450\;{\mu}m$(25-50 mesh) and its viability was above 90% in the direct tableting.

• Archives of Pharmacal Research
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• 제26권7호
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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.

• 한국식품과학회지
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• 제40권6호
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• pp.621-625
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• 2008

오징어 간유 미세캡슐화 분말을 HPMC-FCC, zein-DP로 코팅하여 유동층 코팅 특성을 살펴본 결과, 유동층 코팅 효율은 HPMC-FCC, zein-DP 모두 90%의 효율을 나타내었다. 겉보기 밀도는 zein-DP 코팅분말이 0.6 g/mL로 높게 나타나 코팅 분말의 비중이 커져 흐름성이 개선되었음을 확인할 수 있었다. 인공위액과 인공장액에 대한 용해성을 살펴본 결과, HPMC-FCC는 각각 59.9%와 0%를 나타내었고 zein-DP는 각각 0%와 31.0%를 나타내어 코팅재료에 따라 용해성을 조절할 수 있었다. 저장 안정성은 zein-DP나 HPMC-FCC로 코팅한 분말이 미세캡슐화 분말보다 높은 PUFA/SFA 잔존율을 보여, 유동층 코팅 기술이 유지식품의 안정성을 확보할 수 있는 새로운 기술이 될 수 있음을 확인할 수 있었다.