• Title/Summary/Keyword: Soluble group

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Physicochemical Characteristics and Pharmacokintics of Ibuprofen Lysine Salts (흰쥐에서 이부프로펜 리신염의 물리화학적 특성 및 약물동태에 관한 평가)

  • Shin, Dae-Hwan;Kim, Tai-Sung;Park, Seong-Hyeok;Kim, Si-Hyun;Jo, Han-Jun;Han, Kun;Chung, Youn-Bok
    • YAKHAK HOEJI
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    • v.55 no.3
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    • pp.260-266
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    • 2011
  • Two types of water soluble lysine salts of ibuprofen were prepared and evaluated. Physicochemical properties for ibuprofen-l-lysinate (IBL-l), ibuprofen-dl-lysinate (IBL-dl) and ibuprofen (IB) were studied on melting point, specific ratation, UV spectra and $^1H$-NMR spectra. There were not differences between IBL-dl and IBL-l in UV spectra and $^1H$-NMR spectra. The pharmacokinetic parameters of IB were compared to those of its lysine salts (IBL-l and IBL-dl) after i.v. or oral administration at the dose of 50 mg/kg (calculated as IB). Total body clearance ($CL_t$) and area under the plasma concentration-time curve (AUC) were not different between IB group and IBL groups after i.v. administration. On the other hand, IBL-l and IBL-dl produced peak plasma concentrations ($C_{max}$) significantly ealier and higher than IB. Time to reach peak concentration ($T_{max}$) after IBL administration was lower than that after IB administration. There was no difference in AUC across all different groups (IB, IBL-l and IBL-dl) after oral administration. However, absorption rate constant ($k_a$) of IBL-l and IBL-dl were significantly increased than that of IB. These results indicated that the administration of IBL-l and IBL-dl may be advantageous if rapid and reliable onset of pain relief is required.

Preparation and In Vitro Test of Sold Dispersion using Acyclovir and Water Soluble Polymer (아시클로비어와 수용성 고분자를 이용한 고체분산체 제조 및 생체외 방출)

  • Ahn, Yong-San;Lee, Ha-Young;Hong, Keum-Duck;Jung, Sung-Beum;Cho, Sun-Hang;Rhee, John-Moon;Lee, Hai-Bang;Khang, Gil-Son
    • Journal of Pharmaceutical Investigation
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    • v.34 no.3
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    • pp.169-176
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    • 2004
  • Acyclovir(ACV) is an important antiviral drug used extensively against infections caused by herpes viruses, especially herpes simplex and varicella zoster. Because of high crystallinity and large particle size, solubility of intact ACV is very low in water(1.3 mg/ml). The goal of this work is to enhance the solubility of ACV. To make solid dispersion, Polyethyleneglycol, Hydroxyprophylmethylcelluose and Polyvinylpyrrolidone were used as polymer carriers in this work. Polymer carriers and drug were dissolved in acetic acid. And then spray drying method and freeze drying method were used as solvent extraction. Morphology, crystallization and functional group were characterized using SEM, XRD and FT-IR. The result of in vitro test showed the sample using PVP as polymer carrier had higher dissolution rate(up to 466%) than intact ACV.

Inhibition of Tumor Formation and Changes in Hepatic Enzyme Activities by Kimchi Extracts in Sarcoma-180 Cell Transplanted Mice

  • Hur, Young-Mi;Kim, So-Hee;Park, Jong-Won;Park, Kun-Young
    • Preventive Nutrition and Food Science
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    • v.5 no.1
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    • pp.48-53
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    • 2000
  • Inhibitory effects of the methanol extract, hexane extract, methanol soluble fraction (MSF) and juice from 3 weeks fermented Kimchi on the tumor formation in sarcoma-180 cell transplanted mice were studied. Effects of the solvent extracts and juice of the Kimchi on the levels of lipid peroxide, glutathione, and the enzyme activities of the liver were also investigated in normal and sarcoma-180 cell transplanted mice. At 32 days following trans-plantation, MSF reduced the tumor formation by 54% compared with the control group, resulting in the smallest tumor weight. Lipid peroxided content in liver increased by the transplantation of sarcoma-180 cells. However, it decreased when MSF of Kimchi was treated to the mice. MSF also suppressed xanthine oxidase activity in cytosol of the liver cells in mice transplanted by sarcoma-180 cells. Kimchi extracts had no inhibitory effect on hepatic aminopyrine-N-demethylase activity in sarcoma-180 cell transplanted or normal mice. Methanol extract and hexane extract of Kimchi slightly increased hepatic glutathione contents in sarcoma-180 treated mice. The injection of MSF from Kimchi markedly increased glutathione levels in the liver of sarcoma-180 treated mice. The injection of MSF from Kimchi markedly increased glutathione levels in the liver of sarcoma-180 treated mice compared to the controls. The MSF recovered the activities of hepatic glutathione reductase and glutathione S-transferase that decreased by the injection of sarcoma-180 cells. These results showed that MSF of Kimchi could suppress the growth of tumors, inhibiting lipid peroxide production and xanthine oxidase activity, in mice. We also suggested that Kimchi extract might play an important role in the prevention of cancer by enhancement of the glutathione level itself as well as via glutathione reductase and glutathione S-transferase.

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Inhibitory Effects of Anthocyanin-rich Fraction from Purple Sweet Potato on High Fat Diet-induced Insulin Resistance and Hepatic Steatosis (자색고구마로부터 분리한 안토시아닌 분획물의 고지방식이로 유도된 인슐린 저항성과 간 지질 축적 개선 효과)

  • Nam, Song Yee;Jang, Hwan Hee;Kim, Jung Bong;Lee, Sung Hyun;Lee, Young Min
    • Journal of the East Asian Society of Dietary Life
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    • v.26 no.3
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    • pp.278-284
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    • 2016
  • Anthocyanins, a class of flavonoids, are natural water-soluble pigments, mainly found in vegetables and fruits. Anthocyanins have attractive pharmacological activities, such as anti-oxidant, anti-inflammatory, anti-cancer, and anti-diabetic effects. The purpose of this study was to investigate the inhibitory effects of the anthocyanin-rich fraction (ANF) from purple sweet potato on high fat diet-induced insulin resistance and hepatic steatosis. C57BL/6J mice were assigned to the following groups (n=8 per group): normal fat diet (NF); high fat diet (HF); high fat diet with ANF 50mg/kg (ANF50). Normal fat or high fat diets were fed for a total of 17 weeks, and ANF was orally administrated for 8 weeks (from 10 to 17 weeks, five times/week). In our results, there were no significant differences in body weight, food intake, and tissue weight upon ANF supplementation. The levels of serum triacylglycerol, total-cholesterol, and glucose were also not affected by ANF supplementation. However, ANF supplementation significantly decreased serum insulin and HOMA-IR levels as well as prevented hepatic fat accumulation in high fat-fed mice. These results show that ANF may be beneficial for improving high fat-induced insulin resistance and protecting against development of hepatic steatosis.

A Study on Different Pre-processing of Ligularia fischeri Injeolmi to Standardize Its Processing (전처리 방법을 달리한 곰취 인절미의 제조법 표준화 연구)

  • Choi, So-Rye;Lee, Seung-Joo
    • Journal of the East Asian Society of Dietary Life
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    • v.26 no.4
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    • pp.359-369
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    • 2016
  • In this study Ragwort, which had various and excellent pharmacological activity, was selected as a functional material, and intended to present an optimum condition of Ragwort Injeolmi by the blanching method, commonly used in the field. The general components, antioxidation, and dietary fiber of Ragwort were analyzed, and produceableness of Ragwort added Injeolmi was reviewed through instrumental inspection and sensory evaluation of various adding ratio of lyophilized Ragwort power and Ragwort pre-processed by blanching. It was proved that the SOD-likely active of Ragwort was 45.69%, total poly- phenol content was 12.45 mg, and total flavonoid content was 10.25 mg. The pH of Injeolmi adding Ragwort powder showed an increasing trend in the order of 0%, 1%, 3%, 5%, while that of Injeolmi adding blanching Ragwort showed increasing trend in the order of 0%, 10%, 15%, 20%, and there were significant difference (p<0.001). The soluble solid content of all sample groups showed constant value, and it was understood that no sugar was added in the process. From chromatography measurement result, a-value (redness) of 1% sample group was the lowest, and there were significant differences among sample groups (p<0.001). During 3 days of storage period, total microbial count of Injeolmi showed increasing trend while the storage period was getting longer. From the acceptability test Injeolmi adding blanching Ragwort had shown generally higher value.

Identification of a Mature form and Characterization of Thermostability of a Serine-type Protease from Aquifex pyrophilus

  • Kim, Yun-Kyeong;Choi, In-Geol;Nam, Won-Woo;Yu, Yeon-Gyu
    • BMB Reports
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    • v.33 no.6
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    • pp.493-498
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    • 2000
  • Aquifex pyrophilus, a hyperthermophilic bacterium, has a serine-type protease that is located at the cell wall fraction with a mature size of 43 kDa. Molecular cloning of the protease gene revealed that it has an ORF of 619 amino acids with homologous catalytic site of serine-type proteases [Choi, I.-G., Bang, W.-K., Kim, S.-H., Yu, G. Y., J. Biol. Chem. (1999), Vol. 274, pp. 881-888]. Constructs containing different regions of the protease gene, including a alanine-substituted mutant at the active site serine, were constructed, and the factors affecting the expression level of the cloned protease gene in E. coli were examined. The presence of the C-terminus hydrophobic region of the protease hindered over-expression in E. coli. Also, the proteolytic activity of the expressed protein appeared to toxic to E. coli. An inactive form that deleted both of the N-terminal signal sequence and the C-terminal polar residues was over-expressed in a soluble form, purified to homogeneity, and its thermostability examined. The purified protein showed three disulfide bonds and three free sulfhydryl group. The thermal denaturation temperature of the protein was measured around $90^{\circ}C$ using a differential scanning calorimeter and circular dichroism spectrometry. The disulfide bonds were hardly reduced in the presence of reducing agents, suggesting that these disulfide bonds were located inside of the protein surface.

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Synthesis and Characterization of Molybdeum Complexes with Schiff-Bases(II), Dioxobis(N-aryl-3-methoxysalicyaldiminato) Molybdenum(VI) Complexes (몰리브덴의 시프-염기착물의 합성과 그 성질 (제2보). 다이옥소비스(질소-아릴-3-메톡시살리실알디미나토)몰리브데늄(VI) 착물)

  • O, Sang O;Gu, Bon Gwon
    • Journal of the Korean Chemical Society
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    • v.29 no.3
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    • pp.257-264
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    • 1985
  • Dioxobis(3-methoxysalicyaldehydato)molybdeum(VI) complex has been synthesized by reactions of 3-methoxysalicylaldehyde and ammonium paramolybdate in methanol solution. With appropriate primary amine, the resulting complex gave schiff-base complexes, MoO$_2$(CH$_3$O-sal-N-R)$_2$ in which C=O oxide ligands had been replaced by nitrogen. The properties and possible molecular structure of these complexes were discussed by elemental analysis, spectroscopic studies and electric conductivities measurements. It was found that the Mo(VI) complexes contain a cis-MoO$_2$ group since their infrared spectra two Mo=O band at about 900cm$^{-1}$ and the combining ratios for MoO$_2$-ligand are 1 : 2. Also, electronic spectra of molybdenyl complexes assigned to ligand-to-metal charge transfer transition. All of these complexes are yellow or orange, depolar compound and slightly soluble in alcohol, dichloromethane, chloroform and N,N-dimethylformamide.

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Synthesis and Effect on t-Butyl PBD of the Blue Light Emitting Poly(phenyl-9,9-dioctyl-9',9'-dihexanenitrile) fluorene

  • Kim Byong-Su;Kim Chung-Gi;Oh Jea-Jin;Kim Min-Sook;Kim Gi-Won;Park Dong-Kyu;Woo Hyung-Suk
    • Macromolecular Research
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    • v.14 no.3
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    • pp.343-347
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    • 2006
  • A novel, blue light-emitting polymer, poly(phenyl-9,9-dioctyl-9',9'dihexanenitrile)fluorene (PPFC6N), containing an alkyl and cyano group in the side chain, was synthesized by Suzuki polymerization and characterized. The polymer structure was confirmed by $^1H-NMR$. The number average molecular weight and the weight average molecular weight of the obtained polymer were 9,725 and 9,943 respectively. The resulting polymer was thermally stable with a glass transition temperature ($T_g$) of $93^{\circ}C$, and was easily soluble in common organic solvents such as THF, toluene, chlorobenzene and chloroform. The HOMO and LUMO energy levels of the polymer were revealed as 5.8 and 2.88 eV by cyclic voltammetry study, respectively. The ITO/PEDOT:PSS (40 nm)/PPFC6N (80 m)/LiF (1 nm)/Al (150 nm) device fabricated from the polymer emitted a PL spectrum at 450 nm and showed a real blue emission for pure PPFC6N in the EL spectrum. When t-butyl PBD was introduced as a hole blocking layer, the device performance was largely improved and the EL spectrum was slightly shifted toward deep blue. The device with PPFC6N containing t-butyl PBD layer showed the maximum luminance of 3,200 $cd/m^2$ at 9.5 V with a turnon voltage of 7 V.

Astudy on the Anticancer Activies of Lipid Soluble Ginseng Extract and Ginseng Sapongin DErivatives Against Some Cancer Cells (인삼의 지용성 성분과 사포닌 유도체의 항암작용 연구)

  • 항우익;오수경
    • Journal of Ginseng Research
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    • v.8 no.2
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    • pp.153-166
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    • 1984
  • The anticancer activities of petroleum ether extract of Panax ginseng root(crude GX) and its partially purified fraction from silicic acid column chromatography (7:3 GX) were studied with Sarcoma 180(S-180) or Walker carcinosarcoma 256 (Walker 256) in vivo and with L1210 leukemic lympocyte in vitro. Potential cytotoxic activities of the crude GX and against L1210 cells were compared with those of 5-Fluorouracil (5-FU) and saponin derivatives (Panax-diol, Panax-triol, Diol saponin, Triol saponin) in vitro. In order to observe the physiological effects of the crude GX and 7:3 GX on the animals with cancer, hemoglobin(Hb), red blood cell(R.B.C) and white blood cell after treatment with each GX in comparison with corresponding control groups, respectively. The anticancer effects of the crude GX and 7:3 GX were estimated by measuring the survival time of S-180 bearing mice after treatment with them. The experimental results obtained are summarized as follows; 1. The one unit of cytotoxic activity against L1210 cells was equivalent to 2.54$\mu\textrm{g}$ and 0.88$\mu\textrm{g}$of the crude GX and 7:3 GX per ml of culture medium, respectively. 2. The cytotoxic activities of Panax-diol, Panax=triol, Diol saponin and triol saponin against L1210 cells were not detected. 3. The anticancer activities of 5-FU against L1210, S-180 and Walker 256 were very effective in vivo and vitro tests. 4. The significantly increased W.B.C values of mice after inoculation with S-180 cells were reduced to normal range by the crude GX treatment. 5. The significantly decreased Hb values of rats after inoculation with Walker 256 were recovered to normal range by oral administration of the crude GX. 6. The survival times of mice inoculated with S-180 cells were extended about 1.5 to 2 times by the 7:3 GX treatment compared with their control group.

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Effect of Types and Mixing Ratios of Water-Soluble Polymers on In Vitro Release Profile of Sold Dispersion for Acyclovir (아시클로비어 고체분산체의 용해도에 대한 수용성 고분자의 종류 및 배합 비율에 따른 효과)

  • Ahn, Yong-San;Lee, Ha-Young;Hong, Keum-Duck;Jung, Sung-Beum;Cho, Sun-Hang;Rhee, John M.;Lee, Hai-Bang;Khang, Gil-Son
    • Journal of Pharmaceutical Investigation
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    • v.34 no.4
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    • pp.289-297
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    • 2004
  • Acyclovir (ACV) is one of the most effective and selective agents against viruses of the herpes group. Because of low solubility, bioavailability of ACV has shown below 30% with oral dosage form. In our previous study, we reported that the fabrication of solid dispersion of ACV was possible and the solid dispersion of ACV and PVP was the most useful in all samples. In this study, we examined the effect of mixture ratio of polymers (PEG and PVP) to ACV. Solubility of ACV was dramatically increased up to 25 mg/ml in $80^{\circ}C$ distilled water. So water was used as a solvent to eliminate problem of residual solvent. Spray drying method was used for the solid dispersion of ACV as solvent extraction. Different scanning calorimeter was used to check degradation of drug. Polymer carriers were PEG 6,000 and PVP. In summary, ACV-PVP (1:3) showed the best solubility in distilled water.