• 제목/요약/키워드: soluble stability

검색결과 413건 처리시간 0.028초

PEG 접합: 단백질 및 펩타이드 치료제의 약효를 증가시키는 새로운 기술 (PEGYLATION: Novel Technology to Enhance Therapeutic Efficacy of Proteins and Peptides)

  • 박명옥;이강춘
    • Journal of Pharmaceutical Investigation
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    • 제30권2호
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    • pp.73-83
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    • 2000
  • Polyethylene glycol (PEG) is a water soluble, biocompatible, non-toxic polymer and PEGylation is a well established technique for the modification of therapeutic proteins and peptides. PEG-protein drugs have been extensively studies in relation to therapies for various diseases: cancer, inflammation and others. The covalent attachment of PEG to proteins and peptides prolonged plasma half-life, reduced antigenicity and immunogenicity, increased thermal and mechanical stability, and prevented degradation by enzymes. Several chemical groups for general and site specific conjugation have been exploited to activate PEG for amino group, carboxyl group, and cysteine groups. PEGylation of many proteins and peptides have been studied to enhance their properties for the potential uses. Also, the different positional isomers in several PEG-proteins have shown the difference in vivo stability and biological indicating that the site of PEG molecule attachment is one of the important factor to develop PEG-proteins as potential therapeutic agents.

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Studies on the interaction of thiamines and cyclodextrins

  • Im, In-Seon;Lee, Wang-Kyu;Park, Man-Ki;Kim, Bak-Kwang
    • Archives of Pharmacal Research
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    • 제6권1호
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    • pp.35-44
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    • 1983
  • Interactions between thiamine.HCl and its disulfide derivatives TTFD. TPD and .alpha., .betha. cyclodextrins were investigated. By measuring the H-NMR, C-NMR chemical shifts, the assumption that cyclodextrin may from a inclusion complex with thiamines was supported qualitatively. To calculated the stability constants of them, anion exchange chromatography was applied. The simple, rapid HPLC method was proved to be pertinent thiamine/cyclodextrin system which was chemically unstable and less soluble.

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Exothermic processes in nitric acid solutions imitating highly active raffinate

  • E.V. Belova;V.V. Kalistratova;A.S. Obedkov
    • Nuclear Engineering and Technology
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    • 제55권10호
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    • pp.3808-3814
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    • 2023
  • The thermal stability of nitric acid solutions after contact with non-irradiated and irradiated tributyl phosphate (TBP) and its solution in Isopar-M has been studied. It has been established that exothermic processes occur during heating due to the interaction of soluble radiolysis products and the decomposition of the extractant with nitric acid. Such processes can occur at temperatures below 100 ℃, but unlike a thermal explosion that occurs in seconds, they are longer in time and are accompanied by weak heat evolution. Their intensity depends on the composition of the extractant, the concentration of HNO3, and the volume ratio of the organic and aqueous phases. The presence of extractant degradation products in raffinates does not pose a risk of a rapid evolution of gaseous products during evaporation, however, the presence of reducing agents can significantly increase the intensity of the exothermic decomposition of raffinates.

Effects of calcium propionate on the fermentation quality and aerobic stability of alfalfa silage

  • Dong, Zhihao;Yuan, Xianjun;Wen, Aiyou;Desta, Seare T.;Shao, Tao
    • Asian-Australasian Journal of Animal Sciences
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    • 제30권9호
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    • pp.1278-1284
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    • 2017
  • Objective: To assess the potency of calcium propionate (CAP) used as silage additive, an experiment was carried out to evaluate the effect of CAP on the nitrogen transformation, fermentation quality and aerobic stability of alfalfa silages. Methods: Alfalfa was ensiled with four levels of CAP (5, 10, 15, and 20 g/kg of fresh weight [FW]) in laboratory silos for 30 days. After opening, the silages were analyzed for the chemical and microbiological characteristics, and subjected to an aerobic stability test. Results: The increasing proportion of CAP did not affect pH, lactic acid (LA) concentrations and yeast counts, while linearly decreased counts of enterobacteria (p = 0.029), molds (p<0.001) and clostridia (p<0.001), and concentrations of acetic acid (p<0.001), propionic acid (p<0.001), butyric acid (p<0.001), and ethanol (p = 0.007), and quadratically (p = 0.001) increased lactic acid bacteria counts. With increasing the proportion of CAP, the dry matter (DM) loss (p<0.001), free amino acid N (p<0.001), ammonia N (p = 0.004), and non-protein N (p<0.001) contents were linearly reduced, whereas DM (p = 0.048), water soluble carbohydrate (p<0.001) and peptide N (p<0.001) contents were linearly increased. The highest Flieg's point was found in CAP10 (75.9), represented the best fermentation quality. All silages treated with CAP improved aerobic stability as indicated by increased stable hours compared with control. Conclusion: The addition of CAP can suppress the undesirable microorganisms during ensiling and exposure to air, thereby improving the fermentation quality and aerobic stability as well as retarding the proteolysis of alfalfa silage. It is suggested that CAP used as an additive is recommended at a level of 10 g/kg FW.

종이 기록물 보수용 테이프 점착제 합성 및 열화 안전성 연구 (The Stability of Aging and Synthetic Development of Paper Mending Tape for Conservation of Archive Document)

  • 신종순;이귀복
    • 한국인쇄학회지
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    • 제30권1호
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    • pp.35-45
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    • 2012
  • Polyacrylate dispersion(emulsion) as adhesive material was superior in quality such as preservation characteristics and reversibility. The tapes for repairing archival documents manufactured with four different types of formulation resulted in pH 7~8.8, soluble solid 50~52%, and viscosity 1,300~2,500 cps. Sample 4 of those was most excellent. Probably, sample 4 included inorganic materials such as MgO, silica gel, and zeolite. For selecting carrier of tape, tracing papers, were applied for manufacturing tapes and tested for adhesive strength and peel strength. Adhesive strength of tracing papers, was 3.1~3.8(N/10mm), 2.2~2.8(N/10mm), and 1.7-2.3(N/10mm), respectively. Peel strength was similar in all samples. To determine characteristic of conservation to the selected carriers, stability of deterioration was examined at conditions of $105^{\circ}C$ and $80^{\circ}C$ 65% for 7 days.

Synthesis and Nonlinear Optical Properties of Novel T-type Polyester Containing Thiophene with Enhanced Thermal Stability

  • No, Hyo-Jin;Cho, You-Jin;Lee, Ju-Yeon
    • Bulletin of the Korean Chemical Society
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    • 제31권2호
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    • pp.429-434
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    • 2010
  • A novel T-type polyester 7 containing 1-(2,5-dioxyphenyl)-2-{5-(1,2,2-tricyanovinyl)-2-thienyl}ethenes as nonlinear optical (NLO) chromophores, which are part of the polymer backbone, was prepared and characterized. Polyester 7 is soluble in common organic solvents such as dimethylsulfoxide and N,N-dimethylformamide. It showed a thermal stability up to $300^{\circ}C$ in thermogravimetric analysis thermogram and the glass-transition temperature ($T_g$) obtained from differential scanning calorimetry thermogram was around $113^{\circ}C$. The second harmonic generation (SHG) coefficient ($d_{33}$) of poled polymer films at 1,560 nm fundamental wavelength was around 1.85 pm/V. The dipole alignment exhibits a greater thermal stability even at $10^{\circ}C$ higher than $T_g$, and there is no SHG decay below $125^{\circ}C$ due to the partial mainchain character of the polymer structure, which is acceptable for nonlinear optical device applications.

Effects of Chitosan Coating for Liposomes as an Oral Carrier

  • Lee, Chang-Moon;Kim, Dong-Woon;Lee, Ki-Young
    • 대한의생명과학회지
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    • 제17권3호
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    • pp.211-216
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    • 2011
  • The chitosan-coated liposomes (chitosomes) were designed to improve the stability in the gastrointestinal (GI) tract and to enhance the efficacy for oral drug delivery of liposomes. The phosphatic acid (PA)-incorporated anionic liposomes were surface-coated with water soluble chitosan (WSC) by electro-ionic interaction. The shape of the chitosomes observed by transmission electron microscopy (TEM) was spherical in all the formulations and the coating layer by WSC could be founded through TEM images. The mean size and the zeta potential values of the chitosomes increased significantly with depending on the content of WSC added for coating the liposomes. The stability of the chitosomes in the GI tract was confirmed through the change of relative turbidity of the liposomal suspension. The plain liposomes (plasomes) suspension without adding WSC clearly showed the change of relatively turbidity in simulated gastric fluid (SGF), while the change degree of turbidity of the chitosomes in the SGF decreased as increasing of WSC content added for coating liposome. In the 5-CF release study from the plasomes and chitosomes, the plasomes released >90% of the initial 5-CF content at 4 h of release measurement. In contrast, the chitosomes released below 40% of initial content of 5-CF. In conclusion, these results indicate that the chitosomes can be used as a potential carrier for effective oral drug delivery.

Solid Dispersion of an HIV Protease Inhibitor

  • Park, Jae-Hyeon;Lee, Sung-Hack;Lee, Yong-Hee;Kim, Ae-Ri
    • Journal of Pharmaceutical Investigation
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    • 제41권2호
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    • pp.75-82
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    • 2011
  • LB71350 is an HIV protease inhibitor with poor aqueous solubility and extensive first pass effect. The purpose of the present study was to test the feasibility of solid dosage form of LB71350 with improved bioavailability utilizing solid dispersion. Three different compositions with varying ratio of (LB71350: Gelucire 44/14: Tween 20) were studied. Capsule filling of these solid dispersion compositions was tested using a semi-automatic capsule filling system. Oral bioavailability in dog was tested. Chemical and physical stability at 4, 25 and $40^{\circ}C$ was monitored by HPLC assay, dissolution test, powder XRD and microscopy. The capsule filling system yielded uniform products of drug loading up to 10%. Oral bioavailability in dog was improved compared to the aqueous suspension of crystalline LB71350. Capsules were chemically stable for up to 6 months at $40^{\circ}C$. However, there were temperature and composition dependent physical changes. Decrease in dissolution rates after storage at $40^{\circ}C$ was due to the polymorphic change. In conclusion, manufacturing process, bioavailability, and physico-chemical stability have been considered to propose a solid dispersion capsule formulation for the HIV protease inhibitor with poor physico-chemical properties. A new less soluble crystalline form identified during the physical stability test warrants further study.

$\beta-cyclodextrin$ 및 유도체의 포접체 형성에 의한 LG 106W의 유용성 및 안정성 개선에 관한 연구 (Improvement in availability and stability of to 106w by inclusion with $\beta-cyclodextrin$ and its derivatives)

  • 정성훈;이천구;조완구;강세훈
    • 대한화장품학회지
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    • 제25권1호
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    • pp.120-136
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    • 1999
  • A newly synthesized polyhydroxy aromatic compound(LG 106w) has good skin lightening effect. Inclusion complexation of LG 106w with $\beta$-cyclodextrin and its hydroxypropyl and dimethyl derivatives was studied by the solubility method, scanning electron microscopy and differential thermal analysis. A relationship between host and guest was clearly reflected in the magnitude of the stability constant(DM-$\beta$> HP-$\beta$>$\beta$ -cyclodextrin). Formulation problems, which resulted from its very low solubility in aqueous solution, were resolved by the inclusion formation. LG 106W from inclusions is much more water-soluble than pure one. The improvement of pH and temperature stability correlated with the increased solubility was also observed. Inclusion complex of LG 106w had similar activity to pure LG 106w on the inhibition of melanin synthesis in B-16 melanoma cell but showed lower irritation on cultured cell test in vitro. According to the results, cyclodextrins might be one of the reliable candidates for improving the availability of LG 106w.

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Synthesis of Novel Y-type Nonlinear Optical Polyesters with Enhanced Thermal Stability of Dipole Alignment

  • Jang, Han-Na;Lee, Ju-Yeon
    • Bulletin of the Korean Chemical Society
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    • 제29권5호
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    • pp.933-938
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    • 2008
  • 2,4-Di-(2'-hydroxyethoxy)benzylidenemalononitrile (3) was prepared and polymerized with terephthaloyl chloride and adipoyl chloride to yield novel Y-type polyesters 4 and 5 containing dioxybenzylidenemalononitrile groups as NLO-chromophores, which constituted parts of the polymer backbone. The resulting polymers 4 and 5 are soluble in common organic solvents such as acetone and N,N-dimethylformamide. Polymers 4 and 5 showed thermal stability up to 300 ${^{\circ}C}$ in thermogravimetric analysis with glass-transition temperatures obtained from differential scanning calorimetry in the range 83-94 ${^{\circ}C}$. The second harmonic generation (SHG) coefficients ($d_{33}$) of poled polymer films at the 1064 nm fundamental wavelength were around $6.48\;{\times}\;10^{-9}$ esu. The dipole alignment exhibited high thermal stability even at 10 ${^{\circ}C}$ higher than $T_g$ and no significant SHG decay was observed below 105 ${^{\circ}C}$ partially due to the main-chain character of polymer structure, which is acceptable for NLO device applications.