• Title/Summary/Keyword: particle size and molecular weight.

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Dissolution Characteristics of Hydrophobic Drug-Soluble Carrier Coprecipitates(III) -Dissolution Behaviour of Indomethacin from Several Fast Release Solid Dispersions of Indomethacin-

  • Jeon, In-Koo;Lee, Min-Hwa;Kim, Shin-Keun
    • Journal of Pharmaceutical Investigation
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    • v.6 no.3
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    • pp.58-69
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    • 1976
  • It is well established that dissolution is freruently the rate limiting step in the gastrointestinal absorpton of a drug from a solid dosage from. The relationship between the dissolution rate and absorption is particularly distinct when considering drugs of low solubility. Consequently, numerous attempts have been made to modify the dissolution characteristics of poorly water soluble drugs. Since dissolution rate is directly proportional to surface area, one may increase the rate by decreasing the particle size of the drug. Levy has considered a number of methods by which a drug may be presented to the GI fludids in finely divided from. The direct method is the utilization of microcrystalline or micronized particles. A second method involves the administration of solutions from which, upon dilution with gastric fluids, the dissolved drug will precipitate in the form of very fine particles. A more unique way of obtaining microcrystalline dispersions of a drug has been ercently suggested by Sekiguchi et al. They have first proposed the formation of a eutectic mixture of a poorly water soruble drug with a physiologically inert, easily soluble carrier. When such systems are exposed to water or GI fluids, the soluble carrier will dissolve rapidly and the finely dispersed drug particles will then be released. It has been suggested by Shefter and Higuchi that the formation of crystalline solvate could be a powerful tool in affecting rapid disslution of highly insoluble substances. Goldberg et al. have noted that the formation of solid solution could reduce the particle size to a minimum and increase the dissolution rate as well as the solubility of the durgs. It has also been shown that the rates of solution of drugs were appreciably increased by coprectipitating the drug with soluble polymers. The increase was found to be sensitive to the method of preparation, the molecular weight of polymer and the particular ratio of drugs to polymer. Although several investigations have demontrated that the solubility and/or dissolution rates of drugs can be increased in this manner, little information is available in the literature related to the in vivo absorption pattern of drugs orally administered as PVP coprecipitates. Recently, however, it was demonstrated that both the rate and extent of absorption of the insoluble drug could be markedly enhanced when orally administered to rats in the form of a coprecipitate with PVP. The purpose of the present investigation was to ascertain the general appility of soluble polymer coprectation technique as a method for enhancing the in vitro dissolution rate of hydrophobic indomethacin. To accomplish this aim, the dissolution characteristics of pure indomethacin, indomethcin-polymer physical mixtures and indomethacin-polymer coprecipitates were quantitatively studied by comparing their relative dissolution rates. The solubility and dissolution behavior of these systems were also examined.

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Preparation of Poly(vinylpyrrolidone) Coated Iron Oxide Nanoparticles for Contrast Agent (조영제로 활용하기 위한 폴리(비닐피롤리돈)이 코팅된 산화철 나노 입자의 제조)

  • Lee Ha Young;Lim Nak Hyun;Seo Jin A;Khang Gilson;Kim Jungahn;Lee Hai Bang;Cho Sun Hang
    • Polymer(Korea)
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    • v.29 no.3
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    • pp.266-270
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    • 2005
  • Iron oxide nanoparticles were prepared by the thermal decomposition of iron pentacarbonyl (Fe(CO)$_5$) Poly(vinylpyrrolidone) (PVP) was used as surface-modifying agent to control the size of the iron oxide nanoparticles. The crystalline structure of PVP coated iron oxide nanoparticles was determined by XRD. The size of PVP coated iron oxide nanoparticles was determined by TEM and ELS. The particle sizes of PVP coated iron oxide nanoparticles were controlled by adjusting the molar ratio of PVP/Fe (CO)$_5$, solvent and molecular weight of PVP Particle sizes increased with increasing PVP content. Spherical $50\~100$ nm sized iron oxide nanoclusters were produced when dimethylformamide was used as a solvent. And well-defined 10 nm iron oxide nanoparticles were produced in Carbitol. The prepared PVP coated iron oxide nanoparticles exhibited a well-dispersed property in water. The results obtained in this study confirmed the feasibility of the PVP-coated iron oxide nanoparticles as a biomaterial for MRI contrast agent.

Extraction of Carbohydrates and Minerals from Laminaria Using Organic Acid (다시마 뿌리로부터 유기산을 이용한 다당과 미네랄 추출)

  • Chun, Ji Yeon;Han, Cha Seong;Lee, Jung Shik;Kim, Young Suk;Park, Kwon Pil
    • Korean Chemical Engineering Research
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    • v.50 no.2
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    • pp.238-243
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    • 2012
  • Laminaria roots have not been practically used in Korea. In this study, the extraction process of carbohydrates and minerals from Laminaria roots was investigated and the properties of extracted components were measured. Hydrochloric acid generally used in carbohydrate extraction from seaweeds in order to obtain high extraction yield. But in this work, to utilize extracted components as a functional food material, organic acids such as citric acid were used. Organic acid as extraction solvent has low extraction yield compared to strong acids. Therefore optimum condition for maximum yield was investigated in carbohydrate extraction from Laminaria roots using organic acid. We measured the extraction yields of carbohydrate with variation of extraction temperature, extraction time, concentration of organic acid and particle size of samples. The extraction yield increased as the particle size decreased and temperature became high. The extraction yield was 19.0 wt% after 4.0 hours extraction with 0.2 wt% citric acid at $100^{\circ}C$. Potassium concentration was high compared other minerals in extraction solution, that is, the ratio of K/Na was about 3.0. Fucoidan from Laminaria roots had same carbohydrate composition and lower molecular weight compared that of Undaria pinnatifida.

Preparation and Characterization of Deoxycholic Acid-Conjugated Low Molecular Weight Water-Soluble Chitosan Nanoparticles for Hydrophobic Antifungal Agent Carrier (소수성 항진균제 전달체로 응용하기 위한 데옥시콜릭산이 결합된 저분자량 수용성 키토산 나노입자의 제조와 특성)

  • Choi, Chang-Yong;Jung, Hyun;Nam, Joung-Pyo;Park, Yoon-Kyung;Jang, Mi-Kyeong;Nah, Jae-Woon
    • Polymer(Korea)
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    • v.33 no.4
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    • pp.389-395
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    • 2009
  • To develop the carrier of hydrophobic antifungal agents based on low molecular weight water-soluble chitosan (LMWSC), LMWSC was chemically modified with deoxycholic acid (DA) which is one of the bile acid as a hydrophobic group. The nanoparticles (WSCDA) using DA conjugated LMWSC were characterized using dynamic light scattering (DLS) and transmittance electron microscope (TEM). The particle size of WSCDA ranged from 250 to 350 nm and increased with the number of DA substitution. The loaded itraconazole as an antifungal agent WSCDA nanoparticles (WSCDA-ITCN) were prepared by solvent evaporation method. The drug content and the loading efficiency were investigated approximately $9{\sim}10%$ and $61{\sim}68%$ by UV spectrophotometer, respectively. The release of drug from nanoparticles was slow and showed sustained release characteristics. Based on the results of release study that the higher DA contents in WSCDA, the slower the releasing rate, the WSCDA-ITCN could be used as an excellent antifungal agent.

Characterization of the Physical Form of Allergenic Cry j 1 in the Urban Atmosphere and Determination of Cry j 1 Denaturation by Air Pollutants

  • Wang, Qingyue;Morita, Jun;Gong, Xiumin;Nakamura, Shinichi;Suzuki, Miho;Lu, Senlin;Sekiguchi, Kazuhiko;Nakajima, Takuya;Nakajima, Daisuke;Miwa, Makoto
    • Asian Journal of Atmospheric Environment
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    • v.6 no.1
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    • pp.33-40
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    • 2012
  • In this study, we characterized the physical form of allergenic Cry j 1 in the urban atmosphere. Through an immunofluorescence antibody method, we showed that allergenic Cry j 1 exists as fine particles (${\leq}1.1{\mu}m$). To determine Cry j 1 concentrations and its particle size distribution, we used the ELISA method to confirm that most Cry j 1 exists as fine particles in the urban atmosphere and is found at high concentrations on fine day next to rainy day. Furthermore, we evaluated Cry j 1 denaturation by using the Biacore J system based on the surface plasmon resonence (SPR) principle and sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE). We showed that the dissociation constant ($K_D$) of Cry j 1 that has been exposed to urban polluted air is lower ($1.76{\times}10^{-14}$ M) than that of Cry j 1 ($1.32{\times}10^{-9}-3.37{\times}10^{-9}$ M) of original pollen grains that has not been exposed to air pollutants. Cry j 1 turns into low molecular weight proteins by reacting with various acidic solutions. In sum, we showed that allergenic Cry j 1 exists as fine particles that can deposit in the lower respiratory tract. This finding clarifies the relationship between Japanese cedar pollinosis and air pollutants.

Preparations and Release Property of Poly(ε-caprolacton)/ethyl cellulose Microcapsule Containing Pluronic F127 (Pluronic F127을 함유하는 Poly(ε-caprolacton)/ethyl cellulose 마이크로 캡슐의 제조 및 방출 특성)

  • Hong, Yeon Ji;Kim, Jin-Chul
    • Applied Chemistry for Engineering
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    • v.20 no.6
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    • pp.632-637
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    • 2009
  • Poly(${\varepsilon}-caprolacton$)/ethyl cellulose (PCL/EC) microcapsules containing pluronic F127 were prepared by a spray drying method. The aqueous phase, 20% of pluronic F127 was dissolved in distilled water, and the organic phase, 5% of PCL and EC were dissolved in dichloromethane. The microcapsules were obtained by spray drying the water-in-oil (W/O) emulsion. According to the data of scanning electron microscopy and particle analyzer, tens of micro size microcapsules were observed. On a differential scanning calorimeter, the phase transition temperatures of microcapsules were observed and they were found around those of pluronic F127 and poly(${\varepsilon}-caprolacton$), which were the main components of the microcapsules. At the range of $30{\sim}45^{\circ}C$, temperature-dependent release properties were investigated using fluorescein isothicyanate-dextran (FITC-dextran) and blue dextran as a model drug. When the temperature was increased, the degree of release of microcapsule was also increased. FITC-dextran, the relative low molecular weight, was more released than blue-dextran.

Characterization and Formation of Chemical Bonds of Silica-Coupling Agent-Rubber (실리카-커플링제-고무의 화학 결합 형성과 특성 분석)

  • Ko, Eunah;Choi, Sung-Seen
    • Elastomers and Composites
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    • v.49 no.3
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    • pp.239-244
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    • 2014
  • Reaction between silica and silane coupling agent without solvent was investigated using transmission mode Fourier transform infrared spectroscopy (FTIR) and thermogravimetric analysis (TGA). Bis[3-(triethoxysilylpropyl) tetrasulfide] (TESPT) was used as a silane coupling agent. After removing the unreacted TESPT, formation of chemical bonds was analyzed using FTIR and content of reacted TESPT was determined using TGA. Content of the coupling agent bonded to silica increased with increase in the coupling agent content, but the oligomers were formed by condensation reaction between coupling agents when the coupling agent was used to excess. In order to identify bonds formed among silica, coupling agent, and rubber, a silica-coupling agent-BR model composite was prepared by reaction of the modified silica with liquid BR of low molecular weight and chemical bond formation of silica-coupling agent-BR was investigated. Unreacted rubber was removed with solvent and analysis was performed using FTIR and TGA. BR was reacted with the coupling agent of the modified silica to form chemical bonds. Polarity of silica surface was strikingly reduced and particle size of silica was increased by chemical bond formation of silica-coupling agent-BR.

A Study on the Effect of Surfactants in Acrylic Emulsion Polymerization (아크릴 에멀젼 중합에서의 계면활성제 영향에 관한 연구)

  • Song, Ju-Ho;Park, Sang-Joon;Park, Sang-Kwon;Lee, Myung-Cheon;Lim, Jong-Choo
    • Applied Chemistry for Engineering
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    • v.10 no.4
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    • pp.523-530
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    • 1999
  • Acrylic pressure-sensitive adhesive has been made utilizing organic solvents, but nowadays it is made by solvent-free system due to environmental problems. In this study, emulsion polymerization were carried out at $40^{\circ}C$ with methacrylic acid(MAA), n-butyl acrylate(n-BA) and 2-ethylhexyl acrylate(2-EHA) as monomers in the presence of anionic(sodium dodecyl sulfate, SDS) and nonionic(ethylene oxide types) surfactant mixtures. The overall conversion of the polymerization reaction in a mixed surfactant system was found to be higher than that in a single surfactant system. Emulsion stability in mixed or anionic surfactant systems was found to be over 12 week, which was better than that in nonionic surfactant system. Emulsion particle size decreased as surfactant content increased. The Tg and molecular weight of emulsion polymer were inependent of the type, the amount and the mixing ratio of surfactant. Based on the results of stability and peel strength, the optimum nonionic surfactant ratio in total 4 g of surfactant mixture systems is found to be 40~60% by weight where the nonionic surfactant has 50 ethylene oxide groups and 16~18 carbon atoms in hydrophobic alkyl chain.

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Decomposition Characteristics of Raw Rubber and Tire by Thermal Degradation Process (열분해 공정을 이용한 원료고무와 타이어의 분해 특성)

  • Kim, Won-Il;Kim, Hyung-Jin;Jung, Soo-Kyung;Hong, In-Kwon
    • Applied Chemistry for Engineering
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    • v.10 no.7
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    • pp.1052-1060
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    • 1999
  • Tire and raw material of tire, i.e., SBR were degraded using pyrolysis process. The yield of pyrolytic oil was increased and that of gas was decreased with increase of operating temperature in pyrolysis. And the yield of pyrolytic oil was increased and that of gas and char was decreased with increase of heating rate. The maximum oil yields of SBR and tire were 86% and 55% each at $700^{\circ}C$ with a heating rate of $20^{\circ}C/min$. The number average molecular weight ranges of SBR and tire were 740~2486, 740~1719, and the calorific value of SBR and tire was 39~40 kJ/g. The oil components were consisted of mostly 50 aromatic compounds. The particle size was decreased and the surface area was increased with increase of operating temperature, and the BET surface area was $47{\sim}63m^2/g$. The optimum condition of pyrolysis was the temperature of $700^{\circ}C$ with heating rate of $20^{\circ}C$, and the reactor was continuously purged with inert gas to sweep the evolved gases from the reaction zone.

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