Kim, Myoung-Jin;Choi, Hye-Min;Nam, Won-Hee;Kim, Se-Jin;Son, Su-Mi;Kim, Jung-Ok
Journal of Physiology & Pathology in Korean Medicine
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v.35
no.6
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pp.235-241
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2021
Sogunjung-tang (SGJT) is traditional herbal prescriptions used to treat abdominal pain. In this study, we evaluated the effect on inflammation and gastritis through SGJT formulation development. SGJT composition herbal medicine was boiled in water at 95~100℃ for 3 hours and then concentrated. Sogunjung-tang mix soft extract (STM) was prepared using pharmaceutical excipients such as purified water, sodium benzoate, β-cyclodextrin and CMC-Na. Anti-inflammatory experiment was conducted using STM and lipopolysaccharide (LPS) in RAW 264.7 cells. Cell survival was measured by MTT method. Nitric oxide (NO) was measured using griess reagents, and pro inflammatory cytokines were measured by enzyme-linked immunosorbent assay and RT-PCR. Also, we verified STM validity in acute gastritis using the ICR mouse. STM was administered oral for three days. And 150 mM HCl in 60% ethanol was oral administered 0.5 mL one hour after the last drug administration. Mice were sacrificed 1 hour after 150 mM HCl in 60% ethanol administration. The gastric mucosa was visually observed. STM were not toxic in RAW 264.7 cells. Treatment of STM inhibited the production of NO and inflammatory cytokine at the protein and mRNA levels. Also, in the acute gastritis model with the mouse, the treatment of STM improved gastric mucosal bleeding and edema. In summary, it was confirmed that the treatment of STM exerts anti-inflammatory and anti-gastritis effects. Therefore, we suggest that STM may provide a preclinical evidence for the prevention and treatment of inflammatory and gastritis diseases.
The formation of inclusion complexes between ${\beta}$-cyclodextrin and diethylenetriamine substituted-pyridine copper(II) perchlorate; [Cu(dien)(sub-py)] $(ClO_4)_2$, were studied by spectrophotometric methods. On account of charge-transfer band(MLCT) and $^2T_2{\rightarrow}^2E$, the two high peaks were observed as an inclusion complex for the [${\beta}$-CD]$[Cu(dien)(p-Cl-py)]^{2+}$ in the ultraviolet region of the spectrum. The ${\beta}$-CD and $[Cu(dien)(sub-py)]^{2+}$ ion formed a 1:1 complex, and the formation constants were decreased with the increasing temperatures, due to weak binding energy between ${\beta}$-CD and $[Cu(dien)(sub-py)]^{2+}$ ion. This reaction was controlled by enthalpy. In a correlation of the Hammett substituent constants and formation constants for the reaction, formation constants were increased by strong binding energy in the inclusion complexes when electron donating groups were substituted in pyridine ring.
The evaluation of malocclusion has to be done quantitatively and qualitatively. This will be lead toward an analysis of malocclusion severity as well as treatment difficulty. The method of proper evaluation of malocclusion severity and treatment difficulty is necessary to assess treatment effect and efficiency for the orthodontists and to establish fundamentals for planning and executing the health-related policies in private and public institutions. The purposes of this study as the first part of the objective and quantitative analysis of malocclusion were 1) to measure treatment difficulty based on the opinions of several orthodontists. and 2) to investigate the relationships between objective malocclusion severity and subjective treatment difficulty 100 pairs of dental casts that had various types and severity of malocclusion were selected from the orthodontic departments of Kyurghee University and Samsung Medical Center The objective malocclusion severity was measured with the PAR (Peer Assessment Rating) index and the subjective treatment difficulty was evaluated by 8 experienced orthodontists. The relationships between objective malocclusion severity and subjective treatment difficulty were statistically evaluated. There were significant relationships between objective malocclusion severity and subjective treatment difficulty especially in the measurements of the upper anterior alignment, the buccal occlusion. the overjet, the overbite and the midline discrepancy en the malocclusion components. The results of this study can provide the background knowledge to develop a new occlusal index. which contains both the malocclusion severity and treatment difficulty for Korean orthodontists.
Upon development of information super-highway and multimedia-related technoiogies in recent years, more efficient technologies to transmit, store and retrieve the multimedia data are required. Among such technologies, firstly, it is common that the semantic-based image retrieval is annotated separately in order to give certain meanings to the image data and the low-level property information that include information about color, texture, and shape Despite the fact that the semantic-based information retrieval has been made by utilizing such vocabulary dictionary as the key words that given, however it brings about a problem that has not yet freed from the limit of the existing keyword-based text information retrieval. The second problem is that it reveals a decreased retrieval performance in the content-based image retrieval system, and is difficult to separate the object from the image that has complex background, and also is difficult to extract an area due to excessive division of those regions. Further, it is difficult to separate the objects from the image that possesses multiple objects in complex scene. To solve the problems, in this paper, I established a content-based retrieval system that can be processed in 5 different steps. The most critical process of those 5 steps is that among RGB images, the one that has the largest and the smallest background are to be extracted. Particularly. I propose the method that extracts the subject as well as the background by using an Image, which has the largest background. Also, to solve the second problem, I propose the method in which multiple objects are separated using RGB channel selection techniques having optimized the excessive division of area by utilizing Watermerge's threshold value with the object separation using the method of RGB channels separation. The tests proved that the methods proposed by me were superior to the existing methods in terms of retrieval performances insomuch as to replace those methods that developed for the purpose of retrieving those complex objects that used to be difficult to retrieve up until now.
Shanmugam, Srinivasan;Im, Ho Taek;Sohn, Young Taek;Kim, Kyung Soo;Kim, Yong-Il;Yong, Chul Soon;Kim, Jong Oh;Choi, Han-Gon;Woo, Jong Soo
Biomolecules & Therapeutics
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v.21
no.2
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pp.161-169
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2013
The objective of this study was to enhance the oral bioavailability (BA) of zanamivir (ZMR) by increasing its intestinal permeability using permeation enhancers (PE). Four different classes of PEs (Labrasol$^{(R)}$, sodium cholate, sodium caprate, hydroxypropyl ${\beta}$-cyclodextrin) were investigated for their ability to enhance the permeation of ZMR across Caco-2 cell monolayers. The flux and $P_{app}$ of ZMR in the presence of sodium caprate (SC) was significantly higher than other PEs in comparison to control, and was selected for further investigation. All concentrations of SC (10-200 mM) demonstrated enhanced flux of ZMR in comparison to control. The highest flux (13 folds higher than control) was achieved for the formulation with highest SC concentration (200 mM). The relative BA of ZMR formulation containing SC (PO-SC) in plasma at a dose of 10 mg/kg following oral administration in rats was 317.65% in comparison to control formulation (PO-C). Besides, the $AUC_{0-24\;h}$ of ZMR in the lungs following oral administration of PO-SC was $125.22{\pm}27.25$ ng hr $ml^{-1}$ with a $C_{max}$ of $156.00{\pm}24.00$ ng/ml reached at $0.50{\pm}0.00$ h. But, there was no ZMR detected in the lungs following administration of control formulation (PO-C). The findings of this study indicated that the oral formulation PO-SC containing ZMR and SC was able to enhance the BA of ZMR in plasma to an appropriate amount that would make ZMR available in lungs at a concentration higher (>10 ng/ml) than the $IC_{50}$ concentration of influenza virus (0.64-7.9 ng/ml) to exert its therapeutic effect.
Fourier Transform Infrared Spectroscopy and in-situ Position Annihilation Lifetime Spectroscopy(PALS) analysis of hybrid film, which consist of silsesquioxane(SSQ) and 4-tert-butyl calix[4]arene-O,O',O",O'"-tetraacetic acid tetraethyl ester(CA[4]) have been investigated in order to understand initial formation of nanopore in the next generation porous low-k dielectrics(k < 2.0). SSQ/CA[4] can provide effective homogeneous thin film having porous structure. The porogen decomposition behavior were completely different in the two kinds of SSQ/CA[4] based hybrid film (i.e. SSQ/CA[4] 10 and SSQ/CA[4] 20%). Relatively small pores(1.5 nm) come from dispersion of uni-molecular CA[4] in the SSQ matrix have been generated at $300^{\circ}C$, while mesopores(2.5~3.0 nm) induced from self assembled CA[4] have been generated at $250^{\circ}C$. It might be due to highly interconnected structure of SSQ/CA[4] 20% hybrid thin film resulting in facile evacuating of decomposed fragment of CA[4] molecule.
Journal of Fisheries and Marine Sciences Education
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v.27
no.5
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pp.1334-1342
/
2015
The aim of this study was to investigate the quality characterization of salmon oil microencapsulated with maltodextrin (MD), cyclodextrin (CD), sodium caseinate (SC), arabic gum (AG) and WPI. After spray drying to ambient temperature, the salmon oil powders were packed (single package) and placed at room temperature ($25^{\circ}C$) for 30 day. The quality characterization of salmon oil powder including total oil (%), extractable oil (%), encapsulation efficiency (%), fatty acid, SEM, pH, acid value (AV), peroxide value(POV) were investigated. Salmon oil was microencapsulated with a high power yield (> 80%); including the formulation MD/SC and MD/SC/WPI. The microencapsules of MD/SC/WPI presented spherical shapes, smooth texture and non-porous surfaces. The pH of MD/SC/WPI varied from 6.11 to 5.99 (p>0.05). The AV of MD/SC/WPI varied from 4.74 to 4.61 (p>0.05). The pH and AV were not significantly different. The POV of MD/SC/WPI increased with storage day (p<0.05). It was concluded that MD/SC/WPI could delay lipid oxidation and high yield (82.55%) of salmon oil powder.
This study was aimed to design and formulate the moisture-activated patches containing ofloxacin and lidocaine for antibacterial and local anesthetic action. The solubility of lidocaine at $32^{\circ}C$ in various vehicles decreased in the rank order of PG $759.5{\pm}44.5\;mg/mL$ > PGL > IPM > PEG 300 > PEG 400 > Ethanol > PGMC > DGME > PGML > OA > $Captex^{\circledR}\;300$ > $Captex^{\circledR}\;200$ > water $(4.0{\pm}0.1\;mg/mL)$. Ofloxacin revealed very low solubility, which the highest solubility was obtained from PEG 400 $(18.7{\pm}6.3\;mg/mL)$ among the vehicles used. The addition of lactic acid increased the solubility of ofloxacin dramatically; the solubility at 5% lactic acid was $133.7{\pm}9.7\;mg/mL$. As $2-hydroxypropyl-{\beta}-cyclodextrin$ was added at the concentrations of 40, 80, 120, 160 and 200 mM, the solubilities of lidocaine and ofloxacin were enhanced up to three and two times, respectively, with concentration-dependent pattern. Gel intermediates for filmtype patches were prepared with mucoadhesive polymer, viscosity builders, lidocaine or ofloxacin at pH values from 5 to 7. Gels were cast onto a release liner and dried at room temperature. Dried patch was attached onto an adhesive backing layer, thus forming a patch system. Patches containing a single drug component were characterized by in vitro measurement of drug release rates through a cellulose barrier membrane. The release study was carried out at $37^{\circ}C$ using a Franz-type cell. Receptor solutions were isotonic phosphate buffers (pH 7.4). Samples $(100\;{\mu}L)$ were taken over 24 hours and quantitated by a verified HPLC method. The releases from all tested were proportional to the square root of time. The release rates were 0.9, 157.3 and $281.7\;{\mu}g/cm^{2}/min^{1/2}$ for the lidocaine patches and 19.8,37.2 and $50.7\;{\mu}g/cm^{2}/min^{1/2}$ for the ofloxacin patches at the concentrations of 0.3, 0.5 and 1 %, respectively. The release rates were dose dependent in both drug patches $(R^{2}\;=\;0.9077\;for\;lidocaine;\;R^{2}\;=\;0.9949\;for\;ofloxacin)$ and those were also thickness-dependent $(R^{2}\;=\;0.9246\;for\;lidocaine;\;R^{2}\;=\;0.9512\;for\;ofloxacin)$.
The purpose of this study is to investigate the interaction of progesterone with various cyclodextrins (CDs) in the aqueous solution and in solid state, and finally to formulate a parenteral aqueous formulation. CDs used were ${\alpha}-$, ${\beta}-$, and ${\gamma}-CD$, $2-hydroxypropyl-{\beta}-CD$ (HPCD), sulfobutyl $ether-{\beta}-CD$ (SBCD), $dimethyl-{\beta}-CD$ (DMCD) and $trimethyl-{\beta}-CD$ (TMCD). The solubility studies of progesterone were performed in the presence of various CDs as a function of concentration or temperature. The solubility of progesterone increased in the rank order of ${\alpha}-CD$ < ${\beta}-CD$ < ${\gamma}-CD$ < TMCD$ < HPCD < DMCD < SBCD. Addition of SBCD (200 mg/ml) in water increased the aqueous solubility $(9.36\;{\mu}g/ml)$ about 3,200 times, and lowering the temperature facilitated the solubilization of progesterone. However, the addition of HPCD and SBCD in 20:80 (v/v) polyethylene glycol 300-water and propylene glycol-water cosolvents markedly decreased the solubility of progesterone, compared with solubilizing effects in water. Physical mixtures and solid dispersions of progesterone with HPCD or SBCD were prepared, and evaluated by differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR), near IR spectroscopy and dissolution studies. By DSC and IR studies, it was found that progesterone was dispersed in HPCD in monotectic state and dissolved rapidly from both solid dispersions. Based on solubility studies, new aqueous progesterone fonnulations (5 mg/ml) containing SBCD (200 mg/ml) could be prepared and did not form precipitates even after 2 months at $4^{\circ}C$. The solution was transparent when mixed with normal saline and 5% dextrose injection at 1: 1, 1:10 and 1:20 (v/v) even after 7 days. Permeation rates of progesterone through a cellulose membrane from 20% PEG 300 solution $(50\;{\mu}g/ml)$ containing HPCD or SBCD were compared with oily formulation. Permeation of progesterone from oily formulation did not occur up to 8 hr, but aqueous formulations showed fast permeation rates from early stage of permeation study. The addition of HPCD or SBCD retarded the permeation rates of progesterone with the increase of CD concentrations, suggesting the possibility of a controlled absorption from the site administered intramuscularly. These results demonstrate that it is feasible to develop a new progesterone parenteral aqueous injection (5 mg/ml) using SBCD.
Although lovastatin (LS) is widely used in the treatment of hypercholesterolemia, its bioavailability is known to be around 5%. This study was aimed to increase the solubility and dissolution-permeation rates of LS using solid dispersions (SDs) with bile salts. The solubilities of LS in water, aqueous bile salt solutions and non-aqueous vehicles were determined, and effects of bile salts on the cellulose or duodenal permeation of LS from SDs were evaluated using a horizontal permeation system. SDs were prepared at various ratios of LS to carriers, such as sodium deoxycholate (SDC), sodium glycocholate (SGC) and/or 2-hydroxypropyl-$\beta$-cyclodextrin (HPCD). The addition of bile salts (25 mM) in water increased markedly the solubility of LS by the micellar solubilization. Some non-aqueous vehicles were effective in solubilizing LS. From differential scanning calorimetric studies, it was found that the crystallinity of LS in SDs disappeared, indicating a formation of amorphous state. The SDs showed markedly enhanced dissolution compared with those of their physical mixtures (PMs) and drug alone. In the dissolution-permeation studies using a cellulose membrane, the donor and receptor solutions were maintained as a sink condition using pH 7.0 phosphate buffer containing 0.05% sodium lauryl sulfate (SLS). The flux of LS alone was nearly same as that of LS-SDC-HPCD (1:3:6) PM. However, the flux of LS-SDC-HPCD (1:3:6) SD slightly increased compared with drug alone and PM, suggesting that entrapment of LS in micelles does not significantly hinder the permeation across cellulose membrane. In the dissolution-duodenal permeation studies using a LS-HPCD-SDC (1:3:6) SD, the addition of various bile salts in donor solutions (25 mM) enhanced the permeation of LS markedly, and the fluxes were found to be $0.69{\pm}0.41$, $0.87{\pm}0.51$, $0.84{\pm}0.46$, $0.47{\pm}0.17$ and $0.68{\pm}0.32{\mu}g/cm^2/hr$ for sodium cholate (SC), SDC, SGC, sodium taurodeoxycholate (STDC) and sodium taurocholate (STC), respectively. The stepwise increase of donor SGC concentration increased the flux dose-dependently. From the relationship of donor SGC concentration and flux, the concentration of SGC initiating the permeation across the duodenal mucosa was calculated to be 11.1 mM, which is nearly same as the critical micelle concentration (CMC, 11.6 mM) of SGC. However, with no addition of bile salts and below CMC, the permeation was very limited and irratic, indicating that LS itself is very poor permeable. Higher protions of bile salt in SD such as LS-SDC or LS-SGC (1 : 49 and 1 : 69) showed highly promoted fluxes. In conclusion, SD systems with bile salts, which may form their micelles in intestinal fluids, might be a promising means for providing enhanced dissolution and intestinal permeation of practically insoluble and non-absorbable LS.
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