• Polymer(Korea)
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• v.34 no.5
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• pp.459-463
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• 2010

Amphotericin B (AmB) is anti-fungal agent for the treatment of systemic fungal infections, but its poor solubility has limited clinical applications. In this study, a new gel formulation made up of L-arginine as solubilizer, thermosensitive Poloxamer 407 (P 407), and adhesive carbopol was designed for effective solubilization and delivery of AmB. The aqueous solubility of AmB was enhanced up to 2.6 mg/mL by addition of L-arginine. Aqueous P 407 solutions of more than 20% w/v showed thermo-induced sol-gel-sol phase transition. The phase transition behavior was affected by the presence of AmB and L-arginine, and the phase transition range was broadened by addition of carbopol. In vitro drug release was improved by the solubilizing effect of L-arginine, and the presence of mucoadhesive carbopol prolonged the release rate as a function of concentration.

• Polymer(Korea)
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• v.38 no.4
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• pp.434-440
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• 2014

We prepared nanoparticles containing insoluble celecoxib by the method of solid dispersions using a spray dryer to improve solubility of celecoxib. We used PVP K30 and Eudragit EPO as water-soluble carriers for the solid dispersion, and poloxamer 407 as a surfactant. Characterization of celecoxib solid dispersion was performed by scanning electron microscope (SEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FTIR). The results of SEM, DSC and XRD demonstrated that celecoxib is amorphous in solid dispersion. The dissolution rate measured in intestinal juice showed that the method of solid dispersion improved celecoxib solubility as compared with a conventional drug (Celebres$^{(R)}$). In conclusion, solid dispersion formulation prepared by a spray dryer would improve the solubility of celecoxib in oral administration.

• The Journal of Internal Korean Medicine
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• v.29 no.3
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• pp.554-566
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• 2008

Objectives : Modified Gamgil-tang is a prescription commonly used for respiratory diseases. This thesis was carried out to check the treatment effects and diversity of drug formulation by comparing extraction method of ethanol and water of modified Gamgil-tang. Methods : All experiments were carried out with water and 50% ethanol extraction for comparison. In vivo experiment, hyaluronidase inhibitory effects and trypsin inhibitory effects were tested to measure the anti-inflammatory effects activity. Scavenging effects of DPPH free radical, xanthine oxidase inhibitory effects and inhibition on TBA-RS formation were experimented to measure anti-oxidative effects. With the in vivo experiment, ICR group mice and SD group rats were used as experimental animals. An anti-inflammatory effects experiment were carried out to measure the action on carrageenin-induced hind paw edema: analgesic effects were measured using writhing syndrome induced by 0.7% acetic acid in mice: antipyretic effect was measured using endotoxin, and inhibitory effects of increase vascular permeability induced by 0.5% histamine were measured. Results : For extraction of glycyrrhizin contents, ethanol extract was extracted 2 times of that of water extract. Anti-inflammatory effects showed high in ethanol extract. Anti-oxidative effects measured high in ethanol extract. No significant result was found in inhibition on TBA-RS formation. Analgesic effects were found to be similar in water and ethanol extract. Antipyretic effects were found to be stronger in water extract. Inhibitory effects of increase vascular permeability induced by 0.5% histamine showed stronger in ethanol extract. Conclusion : By measuring anti-inflammatory effects, analgesic effects, antipyretic effects, anti-oxidative effects, and histamine permeation inhibition effects both in water extract and ethanol extract after adding agents such as Mentha Herba, Gardenias Fructus, and propolis to existing Gamgil-Tang, ethanol extract was found to be more effective in anti-inflammatory effects, analgesic effects, anti-oxidative effects, and histamine permeation inhibition effects. The converse was found for antipyretic effect.

• Journal of Veterinary Clinics
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• v.23 no.2
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• pp.87-90
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• 2006

The aim of the present study was to investigate the disposition pharmacokinetics of roxithromycin in broilers. Roxithromycin was administered at a single dose of 20 mg/kg body weight by intravenous (i.v.) routes. Plasma concentrations of roxithromycin were determined by liquid chromatography/mass spectrometry. After a single i.v. dose plasma concentrations were best fitted to a two-compartment open model. The values of the pharmacokinetic parameters after i.v. administration were: elimination half-life = $5.83{\pm}1.79h$, mean residence time = $6.33{\pm}0.32h$, total body clearance = $0.55{\pm}0.15L/h/kg$, and volume of distribution at steady state = $3.47{\pm}0.84L/kg$. The pharmacokinetic interpretation of roxithromycin after i.v. administration revealed that the drug was well distributed throughout the body in broilers and slowly eliminated. More studies for the application of roxithromycin against poultry disease are needed to establish a suitable pharmaceutical formulation, propose optimum dosage regimens, investigate clinical efficacy and study the tolerability of repeated doses.

• The Journal of Internal Korean Medicine
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• v.29 no.1
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• pp.130-148
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• 2008

Objective : This study was designed to investigate the effect of the water extract of Gamisamgibopae-tang(GMSGBPT), an oriental herbal formulation, on the growth of NCI-H460 and A549 human non-small-cell lung cancer cell lines. Methods : Cytotoxicity and cell morphology were evaluated by MTT assay and inverted microscope, respectively. Apoptosis was detected using agarose gel electrophoresis and flow cytometer. The expression levels of mRNAs and proteins of target genes were determined by RT-PCR and western blot analyses, respectively Result and Conclusion : We found that exposure of A549 cells to GMSGBPT resulted in the growth inhibition in a dose-dependent manner as measured by MTT assay, but GMSGBPTdid not affect the growth of NCI-H460 cells. The anti-proliferative effect of GMSGBPT treatment in A549 cells was associated with morphological changes, formation of apoptotic bodies and DNA fragmentation, and flow cytometry analysis confirmed that GMSGBPT treatment increased the populations of apoptotic-sub G1 phase. Growth inhibition and apoptotic cell death by GMSGBPT were connected with a up-regulation of cyclin-dependent kinase inhibitor p21 (WAF1/CIP1) mRNA and protein in a tumor suppressor p53-independent fashion. However GMSGBPT treatment did not affect other growth regulation-related genes such as early growth response-1 (Egr-1), nonsteroidal anti-inflammatory drug (NSAID)-activated gene-1 (NAG-1), inducible nitric oxide synthase (iNOS), cyclooxygenases (COXs), telomere-regulatory factors in A549 orNCI-H460 cells. Taken together, these findings partially provide novel insights into the possible molecular mechanism of the anti-cancer activity of GMSGBPT.

• Analytical Science and Technology
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• v.14 no.3
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• pp.221-229
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• 2001

The bioequivalence study of two tiropramide products was evaluated in 16 health male volunteers following intra-muscular injection. Test product was Tiram$^{(R)}$ injection (S Pharm. Co, Ltd.) and reference product was Tiropa$^{(R)}$ injection(D Pharm. Co., Ltd.). The drug concentration in plasma was determined by GC/MS for over a period of 8 hours after injection. Analysis of variance reveal that there are no differences in AUC (area under the plasma concentration-time curve from time zero to infinity), Cmax (maximum plasma concentration) and Tmax (time to reach Cmax). The differences of mean AUC, Cmax and Tmax between two products were 0.73, -1.385 and -12.994%, respectively. Minimum detectable differences (%) at ${\alpha}=0.05$ were all less than 20% given as a guideline (10.05, 17.90 and 19.01% for AUC, Cmax and Tmax, respectively). From these results, the two formulations of tiropramide are bioequivalent and thus, may be prescribed interchangeably.

• Journal of Veterinary Clinics
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• v.29 no.2
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• pp.154-159
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• 2012

The efficacy of water soluble formulation of diclazuril (Coccimuel-S 0.5%) was tested against $Eimeria$ spp. infection broiler chickens. The experiment was performed both experimentally infection and in the field test. Coccimuel-S composed with diclazuril induced a marked inhibitory effect on the different stages of $Eimeria$ life cycle in experimentally infected broiler chickens treated with the drug. The tested dosage levels of Coccimuel-S (0.5 ml/L, equivalent to diclazuril 2.5 ppm) in drinking water showed the significant effect compared with the control group in controlling coccidial infection and reducing the total oocyst numbers, lesion and fecal scores ($p$ < 0.001). In addition, testing of Coccimuel-S (0.25 and 0.5 ml/L) in naturally infected poultry farms (1,200 broiler chickens), showed the significant anticoccidial effect compared to control ($p$ < 0.001). In conclusion, addition of Coccimuel-S at the dose of 0.25 and 0.5 ml/L in the drinking water, induced efficacious effect for the treatment of coccidiosis in naturally coccidia infected broiler chickens.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.35 no.2
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• pp.79-89
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• 2009

The objective of this study was to find out the stable formulation of nano-emulsion containing high concentration of quercetin and to investigate the effect of an ethanol on the nano-emulsion prepared by POE (30) hydrogenated castor oil (HCO-30)/oil/quercetin/ethanol/water system. Nano-emulsion was prepared using emulsion inversion point (EIP) method as low-energy method plus homogenizer as high-energy method. To evaluate effect of ethanol and other components on the nano-emulsion, physical properties such as droplet size, morphology, and size distribution were determined. The optimal quercetin concentration was 0.2 % on the nano-emulsion. The droplet diameter was below 300 nm at the HCO-30 concentration below 2.00 %. Nano-emmulsion containing 4.75 % HCO-30 was the most stable and its mean droplet size was 172.40 nm. Finally, the size of nano-emulsion containing 4.00 % ethanol was 128.15 nm and size distribution was also narrow. The results showed that the breakdown process of this nano-emulsion could be attributed to Ostwald ripening. This study about effect of ethanol on the nano-emulsion showed that loading capacity of drug could be increased by using a small amount of ethanol. As prepared stable nano-emulsion, this study showed that these results could be applied to pharmaceutics, cosmetic including skin-care products, perfume and etc.

• Nutrition Research and Practice
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• v.11 no.1
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• pp.3-10
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• 2017

BACKGROUND/OBJECTIVES: Sargassum horneri is an edible brown alga that grows in the subtidal zone as an annual species along the coasts of South Korea, China, and Japan. Recently, an extreme amount of S. horneri moved into the coasts of Jeju Island from the east coast of China, which made huge economic and environmental loss to the Jeju Island. Thus, utilization of this biomass becomes a big issue with the local authorities. Therefore, the present study was performed to evaluate the anti-inflammatory potential of crude polysaccharides (CPs) extracted from S. horneri China strain in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. MATERIALS/METHODS: CPs were precipitated from S. horneri digests prepared by enzyme assistant extraction using four food-grade enzymes (AMG, Celluclast, Viscozyme, and Alcalase). The production levels of nitric oxide (NO) and pro-inflammatory cytokines, including tumor necrosis factor (TNF)-${\alpha}$ and interleukin (IL)-$1{\beta}$ were measured by Griess assay and enzyme-linked immunosorbent assay, respectively. The levels of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), nuclear factor (NF)-${\kappa}B$, and mitogen-activated protein kinases (MAPKs) were measured by using western blot. The IR spectrums of the CPs were recorded using a fourier transform infrared spectroscopy (FT-IR) spectrometer. RESULTS: The polysaccharides from the Celluclast enzyme digest (CCP) showed the highest inhibition of NO production in LPS-stimulated RAW 264.7 cells ($IC_{50}$ value: $95.7{\mu}g/mL$). Also, CCP dose-dependently down-regulated the protein expression levels of iNOS and COX-2 as well as the production of inflammatory cytokines, including TNF-${\alpha}$ and IL-$1{\beta}$, compared to the only LPS-treated cells. In addition, CCP inhibited the activation of NF-${\kappa}B$ p50 and p65 and the phosphorylation of MAPKs, including p38 and extracellular signal-regulated kinase, in LPS-stimulated RAW 264.7 cells. Furthermore, FT-IR analysis showed that the FT-IR spectrum of CCP is similar to that of commercial fucoidan. CONCLUSIONS: Our results suggest that CCP has anti-inflammatory activities and is a potential candidate for the formulation of a functional food ingredient or/and drug to treat inflammatory diseases.

• Journal of Ginseng Research
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• v.39 no.1
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• pp.22-28
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• 2015

Background: Sun ginseng (SG), a specific formulation of quality-controlled red ginseng, contains approximately equal amounts of three major ginsenosides (RK1, Rg3, and Rg5), which reportedly has antitumor-promoting activities in animal models. Methods: MTT assay was used to assess whether SG can potentiate the anticancer activity of epirubicin or paclitaxel in human cervical adenocarcinoma HeLa cells, human colon cancer SW111C cells, and SW480 cells; apoptosis status was analyzed by annexin V-FITC and PI and analyzed by flow cytometry; and apoptosis pathway was studied by analysis of caspase-3, -8, and -9 activation, mitochondrial accumulation of Bax and Bak, and cytochrome c release. Results: SG remarkably enhances cancer cell death induced by epirubicin or paclitaxel in human cervical adenocarcinoma HeLa cells, human colon cancer SW111C cells, and SW480 cells. Results of the mechanism study highlighted the cooperation between SG and epirubicin or paclitaxel in activating caspase-3 and -9 but not caspase-8. Moreover, SG significantly increased the mitochondrial accumulation of both Bax and Bak triggered by epirubicin or paclitaxel as well as the subsequent release of cytochrome c in the targeted cells. Conclusion: SG significantly potentiated the anticancer activities of epirubicin and paclitaxel in a synergistic manner. These effects were associated with the increased mitochondrial accumulation of both Bax and Bak that led to an enhanced cytochrome c release, caspase-9/-3 activation, and apoptosis. Treating cancer cells by combining epirubicin and paclitaxel with SG may prove to be a novel strategy for enhancing the efficacy of the two drug types.