• YAKHAK HOEJI
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• v.28 no.6
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• pp.371-377
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• 1984

• Journal of Pharmaceutical Investigation
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• v.21 no.3
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• pp.125-132
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• 1991

Using X-ray crystallography powder diffraction, the quantitative representation method of preferred orientation of particles ill tablets was developed. Selected faces of a tablet. the upper surface and faces cut parallel and normal to the upper surface, were presented to an X-ray beam and X-ray diffraction patterns for these faces were measured. The effects of particle size. tableting pressure, and particle form on the preferred orientation were also investigated. It was also recognized that the degree of anisotropy in terms of capping tendency was influenced by the preferred orientation of particles in tablets.

• Journal of Pharmaceutical Investigation
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• v.35 no.4
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• pp.243-247
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• 2005

Although many scientists have used pectin, its feasibility in terms of tablet manufacturability with a high speed machine has never been evaluated. Therefore, compactibility of different pectin types for large scale tableting operation has been evaluated. The compactibility behavior of powder pectins was studied by a compaction simulator. It was found that pectin on its own does not produce tablets of acceptable quality even at a punch velocity as low as 20 rpm (e.g. low tensile strengths, capping and lamination irrespective of applied compression force). Thus, dwell time was introduced and more hard compact was produced as relaxation time in die increases. It was concluded that frequent structural failure observed in both pectin types was due to lack of plastic deformation, poor compactibility and high elastic recovery.

• Journal of Pharmaceutical Investigation
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• v.5 no.3
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• pp.58-65
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• 1975

In the preparation of prednisolone tablets, when microfine cellulose$(Elcema^{\circledR})$ was used as diluents, stability and physical characteristics of prednisolone tablets are as follows; 1. Weight of the plain $Elcema^{\circledR}$ tablets increased by 75% of relative humidity and hardness was weakend, but the temperature $(60^{\circ}C)$ caused no change of thickness and decreased the weight and hardness. 2. In experimental tableting of prednisolone tablets, the addition of $Elcema^{\circledR}$ caused no difficulty in direct compression method, and the shortening of the disintegration time and increase of the hardness were satisfactory. 3. Dissolution rate test exhibited the result similiar to disintegration test. 4. In the comparison test of $Elcema^{\circledR}$ and $Avicel^{\circledR}$ as adjuvants the physical constants of prednisolone tablets showed nearly a similar tendency.

• YAKHAK HOEJI
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• v.29 no.4
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• pp.193-198
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• 1985

In formulation technology, the drugs forming eutectic mixture cause many pharmaceutical problems. In this study, the method to prevent such problems has been investigated. The combined drugs of aspirin and isopropylantipyrine forming eutectic mixtures were granulated by using three kinds of binders (PVP, HPMC, starch) and these granules were made into pellets by compacting them with various compressional forces. It was possible to select optimum conditions in granulating, tableting, etc. Disintegration time and dissolution pattern were investigated about this formulation, too.

• 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.

• Journal of Pharmaceutical Investigation
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• v.32 no.1
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• pp.41-45
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• 2002

The purpose of this study is to microencapsulate a highly hygroscopic drug, pyridostigmine bromide (PB), with a waterproof wall material, in order to increase the flowability of the drug particles. Polyvinylacetaldiethylaminoacetate (AEA), Eugragit E and Eugragit RS were examined as the wall materials. Microcapsules containing PB were prepared by the evaporation technique in an acetone/liquid paraffin system using aluminum tristearate as a core material, and evaluated for drug encapsulation efficiency, surface morphology, particle size and drug dissolution. The encapsulation of PB in the wall material was almost complete. Among the wall materials examined, AEA exhibited the most excellency in shape, surface texture, flowability, size distribution of microcapsules. Above results suggest that AEA would be a potential wall material for microcapsulation of highly hygroscopic drugs, such as PB. Through microencapsulation with AEA, inconvenience of handling of PB powders encountered in the process of weighing and packing the powders to tableting die or capsule body could be greatly improved.

• Journal of Pharmaceutical Investigation
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• v.25 no.3
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• pp.205-211
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• 1995

To increase the solubility of iodine and iodine releasing agents, which are used widely as a topical broad spectrum antiseptics and disinfectant sanitizers, its inclusion complexes were prepared and studied. Inclusion complexes of iodine with ${\beta}-cyclodextrin$ were prepared by coprecipitation method and complex formation was acertained by differential scanning calorimetry and microscopic observation. Iodine content of inclusion complex was determined by means of iodometry. Tablets containing inclusion complex were manufactured with sugar, citric acid, magnesium stearate, dextrose. Stability of inclusion complexes and tablets was evaluated by accelerated stability test, and comparing with PVP-iodine. During preparation, use of 50% ethanol solution is preferable to water as the medium because the former resulted in more stable complex for a month under accelerated storage conditions. Solubility of iodine in KI aqueous solution was 0.048 g/ml and lower than in 50% ethanol solution. Inclusion complex and its tablets were very stable at severe condition for one month, and comparable to PVP-iodine in the aspect of stability. Inclusion complex tabletswere not affected with citric acid, sugar, dextrose, and direct tableting method was recommendable because wet granulation using ethanol gave some release of included iodine during process.

• Archives of Pharmacal Research
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• v.28 no.4
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• pp.493-501
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• 2005

Effect of solvents on physical characteristics and release characteristics of monolithic acetaminophen (APAP) hydroxypropylmethylcellulose (HPMC) matrix granules and tablets were examined. Various types and amounts of solvents were employed for granulation and coating. APAP and other excipients were mixed and were then wet-granulated in a high-speed mixer. The dried granules were then directly compressed and film-coated with low viscosity grade HPMC. As the amount of water increased, the size of granules also increased, showing more spherical and regular shape. However, manufacturing problems such as capping and lamination in tableting occurred when water was used alone as a granulating solvent. The physical properties of HPMC matrix granules were not affected by the batch size. The initial release rate as well as the amount of APAP dissolved had a tendency to decrease as the water level increased. Addition of nonaqueous solvent like ethanol to water resulted in good physical properties of granules. When compared to water/ethanol as a coating solvent, the release rate of film-coated HPMC matrix tablets was more sensitive to the conditions of coating and drying in methylene chloride/ethanol. Most of all, monolithic HPMC matrix tablet when granulated in ethanol/water showed dual release with about $50\%$ drug release immediately within few minutes followed by extended release. It was evident that the type and amount of solvents (mainly water and ethanol) were very important for wet granulation and film-coating of monolithic HPMC matrix tablet, because the plastic deforming and fragmenting properties of material were changed by the different strengths of the different solvents.

• Journal of Microbiology and Biotechnology
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• v.29 no.2
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• pp.200-208
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• 2019

Probiotics show low cell viability after oral administration because they have difficulty surviving in the stomach due to low pH and enzymes. For the oral delivery of probiotics, developing a formula that protects the probiotic bacteria from gastric acidity while providing living cells is mandatory. In this study, we developed tablets using a new pH-sensitive phthalyl inulin (PI) to protect probiotics from gastric conditions and investigated the effects of different compression forces on cell survival. We made three different tablets under different compression forces and measured survivability, disintegration time, and kinetics in simulated gastric-intestinal fluid. During tableting, there were no significant differences in probiotic viability among the different compression forces although disintegration time was affected by the compression force. A higher compression force resulted in higher viability in simulated gastric fluid. The swelling degree of the PI tablets in simulated intestinal fluid was higher than that of the tablets in simulated gastric fluid due to the pH sensitivity of the PI. The probiotic viability formulated in the tablets was also higher in acidic gastric conditions than that for probiotics in solution. Rapid release of the probiotics from the tablet occurred in the simulated intestinal fluid due to the pH sensitivity. After 6 months of refrigeration, the viability of the PI probiotics was kept. Overall, this is the first study to show the pH-sensitive properties of PI and one that may be useful for oral delivery of the probiotics.