• YAKHAK HOEJI
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• v.45 no.5
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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.

• 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.

• Korean Journal of Food Science and Technology
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• v.34 no.5
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• pp.856-861
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• 2002

Surface-modified powders were produced by hybridization system using core freeze-dried lactic acid bacteria (Lactobacillus acidophilus ATCC 43121) and enteric coating materials. Scanning electron microscopy showed that the surface of freeze-dried lactic acid bacteria changed to smooth round shape during surface reforming process, although no significant physical damages affecting the activity of the lactic acid bacteria were observed based on viability and salt-tolerance tests. Signigicant difference was not found in acid tolerance test probably due to the inherent acid tolerance of L. acidophilus ATCC 43121. Significantly improved heat tolerance was obtained by surface modification process. Among the tested coating materials, Sureteric showed a higher surface- reforming ability than Eudragit S100 and L100-55. Core : coating ratio agent of 9 : 1 (w/w) with rotor speed of 15,000 rpm for 3 min were determined to be optimum conditions for the process.

• Archives of Pharmacal Research
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• v.27 no.1
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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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• 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.

• 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.

• Proceedings of the PSK Conference
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• 2003.04a
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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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• v.30 no.1
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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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• 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.

• Korean Journal of Food Science and Technology
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• v.40 no.6
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• pp.621-625
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• 2008

Squid oil is an abundant source of polyunsaturated fatty acids. This is particularly true for eicosapentaenoic acid and docosahexaenoic acid. The principal objective of this study was to extend the stability and improve the process aptitude of squid liver oil. Fluidized bed coatings were employed for coating with microencapsulated oil. The efficiency of the fluidized bed coating of the microencapsulated powder was over 90%. The apparent density with zein-DP was 0.6 g/mL, thereby indicating that flow ability had been improved as the result of an increase in specific gravity. The solubility of artificial gastric and enteric fluids with HPMC-FCC was 59.9 and 0%, respectively, whereas with zein-DP solubility was 0 and 31.0%, respectively. Polyunsaturated fatty acid retention results demonstrated that zein-DP coating was higher than HPMC-FCC, followed by the microencapsulated squid liver oil method. These results demonstrated that the application of microencapsulation and fluidized bed micro-coating techniques improved the stability and processing compatibility of squid liver oil.