• Title/Summary/Keyword: dissolution of solid mixture

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Dissolution Enhancements of Tiaprofenic Acid by ${\beta}-Cyclodextrin$ Complexation (${\beta}-Cyclodextrin$과의 복합체 형성에 의한 Tiaprofenic Acid의 용출증가)

  • Chun, In-Koo;Park, In-Sook
    • Journal of Pharmaceutical Investigation
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    • v.16 no.2
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    • pp.55-67
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    • 1986
  • Inclusion complexation of tiaprofenic acid (TPA) with cyclodextrins $({\alpha}-,\;{\beta}-,\;{\gamma}-CyDs)$ in aqueous solution and in solid phase was investigated by solubility method, measurement of partition coefficient, ultra-violet, circular dichroism, infrared spectroscopies, powder X-ray diffractometry and differential scanning calorimetry. Investigations were made to prepare inclusion complexes of TPA with ${\beta}-CyD$ in solid powdered form by coprecipitation, freeze-drying, spray-drying and co-pulverization methods. The coprecipitation, freeze-drying and spray-drying methods were successful in obtaining inclusion complexes. The results showed that the latter two methods might be originally superior to the former in obtaining powdered inclusion completes. Especially, it was shown by powder X-ray diffractometry that spray-dried ${\beta}-CyD$ alone, TPA-spray-dried ${\beta}-CyD$ physical mixture, and spray-dried $TPA-{\beta}-CyD$ complex were amorphous. The dissolution behaviours of $TPA-{\beta}-CyD$ systems prepared by above four methods were compared with those of TPA alone and $TPA-{\beta}-CyD$ physical mixture, and the rates of dissolution of TPA in pH 1.2 buffer were greatly enhanced by inclusion complexation and copulverization.

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A Novel Clotrimazole-Ioaded Suppository with Effective Anti-tumor Activity

  • Xuan, Jing Ji;Kim, Jong-Tae;Oh, Dong-Hoon;Han, Hong-Hee;Lee, Won-Seok;Lee, Jong-Sook;Rhee, Jong-Dal;Yong, Chul-Soon;Woo, Jong-Soo;Kim, Jung-Ae;Choi, Han-Gon
    • Journal of Pharmaceutical Investigation
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    • v.38 no.5
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    • pp.289-293
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    • 2008
  • To develop a poloxamer-based solid suppository with poloxamer and polyethylene glycol mixtures, the melting point of various formulations composed of P 188 and propylene glycol were investigated. The dissolution and antitumor activity of clotrimazole delivered by the poloxamer-based suppository were performed. The poloxamer mixtures composed of P 188 and propylene glycol were homogeneous phases. P 188 greatly affected the melting point of poloxamer mixtures. In particular, the poloxamer mixture [P 188/propylene glycol(70/30%)] with the melting point of about $32^{\circ}C$ was a solid form at room temperature and instantly melted at physiological temperature. Furthermore, the ratio of P 188/propylene glycol greatly affected the dissolution rates of clotrimazole from poloxamer-based suppository. It gave the more effective anti-tumor activity than conventional PEG-based suppository due to fast dissolution. Thus, the clotrimazole-Ioaded poloxamer-based solid suppository was an effective rectal dosage form with anti-tumor activity.

Physicochemical Characterization of Clotrimazole-Loaded Solid Suppository Using Poloxamer and Propylene Glycol (폴록사머 및 프로필렌글리콜을 이용한 클로트리마졸 고형 좌제의 물리화학적 특성)

  • Xuan, Jing-Ji;Oh, Yu-Kyoung;Kim, Jung-Ae;Gong, Kyung-Hwan;Kim, Ji-Hyun;Yang, Joon-Ho;Bae, Myung-Soo;Kim, Ho-Dong;Rhee, Jong-Dal;Chang, Hyeun-Wook;Yong, Chul-Soon;Choi, Han-Gon
    • Journal of Pharmaceutical Investigation
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    • v.35 no.2
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    • pp.107-110
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    • 2005
  • To develop a clotrimazole-loaded solid suppository with poloxamer and propylene glycol, the melting points of various formulations composed of poloxamer 188 (P 188) and propylene glycol were investigated. The dissolution study of clotrimazole delivered by the suppository composed of P 188 and propylene glycol was performed. The mixtures composed of P 188 and propylene glycol were homogeneous. Propylene glycol affected the melting points of poloxamer mixtures. In particular, the mixture [P 188/propylene glycol (70/30%)] with the melting point of about $32^{\circ}C$ was a solid form at room temperature and instantly melted at physiological temperature. Furthermore, propylene glycol affected greatly the dissolution rates of clotrimazole from the suppository. Dissolution mechanism analysis showed the dissolution of clotrimazole was proportional to the time. Our results indicated that the solid suppository with P 188 and propylene glycol would be a candidate of rectal dosage form for clotrimazole.

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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Sintering Mixtures in the Stage of Establishing Chemical Equilibrium

  • Savitskii, A.P.
    • Proceedings of the Korean Powder Metallurgy Institute Conference
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    • 1999.04a
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    • pp.5-5
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    • 1999
  • The Principal deficiency of the existing notion about the sintering-mixtures consists in the fact that almost no attention is focused on the Phenomenon of alloy formation during sintering, its connection with dimensional changes of powder bodies, and no correct ideas on the driving force for the sintering process in the stage of establishing chemical equilibrium in a system are available as well. Another disadvantage of the classical sintering theory is an erroneous conception on the dissolution mechanism of solid in liquid. The two-particle model widely used in the literature to describe the sintering phenomenon in solid state disregards the nature of the neighbouring surrounding particles, the presence of pores between them, and the rise of so called arch effect. In this presentation, new basic scientific principles of the driving forces for the sintering process of a two-component powder body, of a diffusion mechanism of the interaction between solid and liquid phases, of stresses and deformation arising in the diffusion zone have been developed. The major driving force for sintering the mixture from components capable of forming solid solutions and intermetallic compounds is attributed to the alloy formation rather than the reduction of the free surface area until the chemical equilibrium is achieved in a system. The lecture considers a multiparticle model of the mixed powder-body and the nature of its volume changes during solid-state and liquid-phase sintering. It explains the discovered S-and V-type concentration dependencies of the change in the compact volume during solid-state sintering. It is supposed in the literature that the dissolution of solid in liquid is realised due to the removal of atoms from the surface of the solid phase into the melt and then their diffusicn transfer from the solid-liquid interface into the bulk of liquid. It has been shown in our experimental studies that the mechanism of the interaction between two components, one of them being liquid, consist in diffusion of the solvent atoms from the liquid into the solid phase until the concentration of solid solutions or an intermetallic compound in the surface layer enables them to pass into the liquid by means of melting. The lecture discusses peculimities of liquid phase formation in systems with intermediate compounds and the role of the liquid phase in bringing about the exothermic effect. At the frist stage of liquid phase sintering the diffusion of atoms from the melt into the solid causes the powder body to grow. At the second stage the diminution of particles in size as a result of their dissolution in the liquid draws their centres closer to each other and makes the compact to shrink Analytical equations were derived to describe quantitatively the porosity and volume changes of compacts as a result of alloy formation during liquid phase sinteIing. Selection criteria for an additive, its concentration and the temperature regime of sintering to control the density the structure of sintered alloys are given.

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Effect of Manufacturing Method and Acidifier on the Dissolution Rate of Carvedilol from Solid Dispersion Formulations

  • Lim, Dong-Kyun;Bae, Jeong-Woo;Song, Byung-Joo;Jo, Han-Su;Kim, Hyoung-Eun;Lee, Dong-Won;Khang, Gil-Son
    • Journal of Pharmaceutical Investigation
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    • v.41 no.6
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    • pp.363-369
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    • 2011
  • In this study, we demonstrated the release behavior of carvedilol with the content of polyvinylpyrrolidone K-30 (PVP K-30) and the effect of citric acid and fumaric acid as acidifiers on the release behavior of drug. In addition, it tries to inquire into the release behavior difference of the carvedilol according to the manufacturing method. The release behavior of the tablets was compared with Dilatrand$^{(R)}$ in the simulated gastric fluid (pH1.2). Differential scanning calorimeter (DSC), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FT-IR) were characterized for the physicochemical properties of the tablets. In case of mixing the carvedilol and PVP K-30, in case the ratio of the carvedilol and PVP K-30 was 1:5, the release behavior was the highest among. As well as the dissolution rate of tablets manufactured by lyophilization and rotary evaporator was higher than physical mixture. The dissolution rate of containing acidifiers was more improved. But, rather the excessive amount of the acidifier addition reduced the dissolution rate.

Improvement of the mechanical properties of titanium carbonitride-metal composites by modification of interfaces (계면 개선을 통한 타이타늄 탄/질화물 금속 복합재료의 기계적 물성 향상)

  • Kwon, Hanjung
    • Ceramist
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    • v.23 no.2
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    • pp.114-131
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    • 2020
  • Fracture in the titanium carbonitride-metal composites occurs by crack propagation through the carbonitride grains or in the interfaces. Thus, intrinsic properties of the carbonitride need to be enhanced and the interfaces should be also modified to coherent structure to strengthen the composites. Especially, interfacial structure can be the main factor to determine the mechanical properties of titanium carbonitride-metal composites because the interfaces between carbonitride grains and metallic phase are weak parts due to heterogeneous nature of carbonitride and metallic phase. In this paper, methodologies for improving the interfacial structure of titanium carbonitride-metal composites are suggested. Total area of the interfaces can be reduced using solid solution type carbonitrides as raw materials instead of a mixture of various carbonitrides in the composites. Also, synthesis of titanium carbonitride-metal composite powders and the low-temperature sintering of the composite powders for short time can be the way for formation of coherent interfaces. The sintering of the composite powders for short time at low temperature can reduce the potential of formation of interfaces by dissolution and precipitation of carbonitride in the liquid metal. As a result of formation of coherent boundaries due to low-temperature and short-time sintering, interfaces between titanium carbonitride grains and metallic phase have the favorable structure for the enhanced fracture toughness. It is believed that the low-temperature sintering of solid solution type composite powders for short time can be the way to improve the low toughness of the titanium carbonitride-metal composites.

Phase analysis of simulated nuclear fuel debris synthesized using UO2, Zr, and stainless steel and leaching behavior of the fission products and matrix elements

  • Ryutaro Tonna;Takayuki Sasaki;Yuji Kodama;Taishi Kobayashi;Daisuke Akiyama;Akira Kirishima;Nobuaki Sato;Yuta Kumagai;Ryoji Kusaka;Masayuki Watanabe
    • Nuclear Engineering and Technology
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    • v.55 no.4
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    • pp.1300-1309
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    • 2023
  • Simulated debris was synthesized using UO2, Zr, and stainless steel and a heat treatment method under inert or oxidizing conditions. The primary U solid phase of the debris synthesized at 1473 K under inert conditions was UO2, whereas a (U, Zr)O2 solid solution formed at 1873 K. Under oxidizing conditions, a mixture of U3O8 and (Fe, Cr)UO4 phases formed at 1473 K, whereas a (U, Zr)O2+x solid solution formed at 1873 K. The leaching behavior of the fission products from the simulated debris was evaluated using two methods: the irradiation method, for which fission products were produced via neutron irradiation, and the doping method, for which trace amounts of non-radioactive elements were doped into the debris. The dissolution behavior of U depended on the properties of the debris and aqueous solution for immersion. Cs, Sr, and Ba leached out regardless of the primary solid phases. The leaching of high-valence Eu and Ru ions was suppressed, possibly owing to their solid-solution reaction with or incorporation into the uranium compounds of the simulated debris.

Effect of 50 ㎛ class granules on the Injection Behavior of Brushite Bone Cement Prepared via Pre-dissolution Route

  • Mun, Da Hye;Lee, Sang Cheon;Oh, Kyung-Sik
    • Journal of Powder Materials
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    • v.27 no.6
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    • pp.468-476
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    • 2020
  • The bone cement used for vertebroplasty must be sufficiently injectable. The introduction of granules reduces the amount of liquid required for liquefaction, implying that higher fluidity is achieved with the same amount of liquid. By employing β-tricalcium phosphate granules with an average diameter of 50 ㎛, changes in injectability are observed based on the paste preparation route and granular fraction. To obtain acceptable injectability, phase separation must be suppressed during injection, and sufficient capillary pressure to combine powder and liquid must work evenly throughout the paste. To achieve this, the granules should be evenly distributed. Reduced injection rates are observed for dry mixing and excessive granular content, owing to phase separation. All these correspond to conditions under which the clustered granules weakened the capillary pressure. The injected ratio of the paste formed by wet mixing displayed an inverted U-type shift with the granular fraction. The mixture of granules and powder resulted in an increase in the solid volume fraction, and a decrease in the liquid limit. This resulted in the enhancement of the liquidity, owing to the added liquid. It is inferred that the addition of granules improves the injectability, provided that the capillary pressure in the paste is maintained.

The characterization of charge-discharge and initial impedance of $LiMn_{2-y}Mg_yO_4$ by change of temperature (온도 변화에 따른 $LiMn_{2-y}Mg_yO_4$의 충방전 및 초기 임피던스 특성)

  • Jeong, In-Seong;Lee, Seung-Woo;Kim, Min-Sung;Gu, Hal-Bon;Gu, Gye-Choon
    • Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
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    • 2001.05a
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    • pp.18-22
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    • 2001
  • Spinel $LiMn_{2-y}Mn_{y}O_4$ powder was prepared solid-state method by calcining the mixture of $LiOH{\cdot}H_2O$, $MnO_2$ and MgO at $800^{\circ}C$ for 36h. To investigate the effect of temperature for cycle behaviour of cathode material during cycling, charge-discharge experiments and initial impedance spectroscopy performed by the condition of the charge-discharge temperature. Initial charge-discharge capacity was gradually increased by rising charge-discharge temperature. However, capacity was suddenly decreased at high temperature during cycling. Capacity at low temperature was almost constant during cycling. It confirmed because Mn dissolution is more serious at high temperature than at low temperature.

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