• Title/Summary/Keyword: amorphous form

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Crystal form of SKP1080 (SKP1080의 결정형)

  • Sohn, Young-Taek;Lee, Kyoung-Ee
    • Journal of Pharmaceutical Investigation
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    • v.30 no.4
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    • pp.289-293
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    • 2000
  • Three polymorphic modifications and one amorphous form were prepared by recrystallization under various conditions and characterized by DSC and X-ray crystallography. At $37{\pm}0.5^{\circ}C$, the polymorphic modifications showed significant differences in the dissolution rate. The dissolution rate of Mod. 4, amorphous form, was faster than that of other polymorphic modifications. When all modifications were stored at 52% RH, 95% RH, and in silica gel desiccator, amorphous form was transformed at 95% humidity condition.

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Studies on the Crystallization in Organic Solvents and the Stability of Sodium Cloxacillin (Sodium cloxacillin의 유기용매(有機溶媒)에 의한 결정화(結晶化) 및 안정성(安定性)에 관한 연구(硏究))

  • 백우현;김정우;봉득환
    • YAKHAK HOEJI
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    • v.22 no.1
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    • pp.8-14
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    • 1978
  • The method that changes sodium cloxacillin from amorphous form to hydrate form was investigated. Using organic solvents of which dielectric constants are greater than 9, the amorphous sodium cloxacillin could be changed to hydrate form. The difference of water content of sodium cloxacillin hydrate caused the differences of ir spectrum at $3,350~3,360cm_{-1}$, and owing to the decrease of water content, hydrate form was changed to the morphous form, which could be identified by x-ray diffraction pattern. Regarding the stability of sodium cloxacillin in activity, the hydrate form was stable but the amorphous form was very unstable. Moreover, the stable hydrate form was scarcely hygroscopic, while the other form was hygroscopic, becoming a fused state ar $50^{\circ}$. and R.H. 50%.

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Preparation and Evaluation of Non-Crystalline Cefuroxime Axetil Solid Dispersion (비결정성 세푸록심 악세틸 고체분산체의 제조 및 평가)

  • Woo, Jong-Soo;Chang, Hee-Chul;Lee, Chang-Hyun
    • Journal of Pharmaceutical Investigation
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    • v.32 no.2
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    • pp.73-80
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    • 2002
  • Cefuroxime axetil is a cephalosporin antibiotic having a high activity against a wide spectrum of Grampositive and Gram-negative microorganisms. It is a cephalosporin antibiotic which exist as 2 diastereoisomers: diastereoisomer A and B. It shows polymorphism of three forms: a crystalline form having a melting point of about $180^{\circ}C$, a substantially amorphous form having a high melting point of about $135^{\circ}C$ and a substantially amorphous form having a low melting point of about 70^{\circ}C$. The crystalline form of cefuroxime axetil is slightly soluble in water because diastereoisomer A has lower solubility than B in water. Substantially amorphous form of which there are no difference in solubility between diastereoisomer A and B has better solubility than crystalline form, but it forms a thicker gel than crystalline form upon contact with an aqueous medium. Based on this reason, cefuroxime axetil is not readily absorbable in the gastrointestinal tract, rendering its bioavailability on oral administration very low. The object of this study was to develop an improved non-crystalline cefuroxime axetil composition having a high physicochemical stability and bioavailability. A non-crystalline cefuroxime axetil solid dispersant showing no peak on a Differential Scanning Calorimetry (DSC) scan is prepared by dissolving cefuroxime axetil and a surfactant in an organic solvent; suspending a water-insoluble inorganic carrier in the resulting solution; and spray drying the resulting suspension to remove the organic solvent, said solid dispersant having an enhanced dissolution and stability of cefuroxime axetil and being useful for the preparation of a pharmaceutical composition for oral administration. Tablet was formulated with this cefuroxime axetil solid dispersant, disintegrants and other ingredients. It disintegrated and dissolved easily and dynamically in dissolution medium, so showed a good dissolution profile.

Characteristics of Heavy Metals In Contaminated Soil-Metal Binding Mechanism through Sequential Extraction in Soils with Lead and Copper (Sequential Extraction을 이용한 중금속(납.구리)과 토양 결합 기작 연구)

  • 조미영;현재혁;김원석
    • Journal of Korea Soil Environment Society
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    • v.4 no.3
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    • pp.77-84
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    • 1999
  • Sequential extraction was applied to characterize the soil-metal binding mechanism in three kinds of soils contaminated with lead and copper The results showed that soil-metal binding was dependent on soil characteristics and metal species. In Munwha dong soil, lead was mainly carbonate form (37.7%), in agriculture soil was associated with amorphous Fe oxide form (23.9%) and in industry area was associated with exchangeable form (22.9%) Meanwhile for copper. organically bound form represented main fraction in most soil and also carbonate and amorphous Fe oxide form showed high fraction. Crystallized Fe oxide and residuals form of copper showed higher fraction than those of lead. Thus, it can be concluded that copper is bound with soil stronger and more difficult wash out Consequently, this mechanism analysis through sequential extraction can provide useful informations for better soil remediation.

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Effect of Crystal Form on Bioavailability (결정형이 생체이용률에 미치는 영향)

  • Sohn, Young-Taek
    • Journal of Pharmaceutical Investigation
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    • v.34 no.6
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    • pp.443-452
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    • 2004
  • Habit is the description of the outer appearance of a crystal. If the environment of a growing crystal affects its external shape without changing its internal structure, a different habit results. Crystal habit and the internal structure of a drug can affect bulk and physicochemical properties, which range from flowability to chemical stability. A polymorph is a solid crystalline phase of a given compound resulting from the possibility of at least two different arrangements of the molecules of that compound in the solid state. Chemical stability and solubility changes due to polymorphism can have an impact on a drug's bioavailability and its development program. During crystallization from a solution, crystals separating may consist of a pure component or be a molecular compound. Solvates are molecular complexes that have incorporated the crystallizing solvent molecule in their lattice. When the solvent incorporated in the solvate is water, it is called a hydrate. To distinguish solvates from polymorphs, which are not molecular compounds, the term pseudopolymorph is used. Identification of possible hydrate compounds is important since their aqueous solubilities can be significantly less than their anhydrous forms. Conversion of an anhydrous compound to a hydrate within the dosage form may reduce the dissolution rate and extent of drug absorption. An amorphous solid may be treated as a supercooled liquid in which the arrangement of molecules is random. Amorphous solids lack the three-dimensional long-range order found in crystalline solids. Since amorphous forms are usually of higher thermodynamic energy than corresponding crystalline forms, solubilities as well as dissolution rates are generally greater. A study on crystal form includes characterization of (l)crystal habit, (2)polymorphism, (3)pseudopolymorphism, (4)amorphous solid.

HRTEM Analysis of Apatite Formed on Bioactive Titanium in Modified-SBF (수정된 유사체액 내에서 티타늄에 생성된 아파타이트의 고분해능 전자현미경에 의한 분석)

  • Kim, Hyun-Ook;Kim, Woo-Jeong;Lee, Kap-Ho;Hon, Sun-Ig
    • Korean Journal of Materials Research
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    • v.17 no.8
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    • pp.408-413
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    • 2007
  • Process of the hydroxyapapite(HA) precipitation on bioactive titanium metal prepared by NaOH in a modified-simulated body fluid(mSBF) was investigated by high resolution transmission electron microscope (HRTEM) attached with energy dispersive X-ray spectrometer(EDX). The amorphous titanate phase on titanium surface is form by NaOH treatment and an amorphous titanate incorporated calcium and phosphate ions in the liquid to form an amorphous calcium phosphate. With increasing of soaking time in the liquid, the HA particles are observed in amorphous calcium phosphate phase with a Ca/P atomic ratio of I.30. The octacalcium phosphate (OCP) structure is not detected in HRTEM image and electron diffraction pattern. After a long soaking time, the HA particles grow as needle-like shape on titanium surface and a large particle-like aggregates of needle-like substance were observed to form on titanium surface within needle-like shape. A long axis of needle parallels to c-direction of the hexagonal HA structure.

Fabrication and Characteristics of Thermal Sprayed Ni-Cr-B-Si System Amorphous Coatings (Ni-Cr-B-Si계 비정질 용사피막의 제조 및 특성)

  • 정하윤;김태형;박경채
    • Journal of Welding and Joining
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    • v.17 no.4
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    • pp.53-59
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    • 1999
  • Amorphous alloys have also been called glassy alloys or non-crystalline alloys. They are made by the rapid solidification. The solidification occurs so rapid that the atoms are frozen in their liquid configuration. There are unique magnetic, mechanical, electrical and corrosive behaviors which result form their amorphous structure. In the study. amorphous coatings were manufactured with Ni-Cr-B-Si powders by flame spray. Measurement of hardness, were resistance, corrosion resistance and observation of microstructures and XRD, DSC were performed to investigate characteristics of amorphous coatings. The experimental results obtained as follow: 1) Amorphous powders could not be manufactured with the spraying in the spraying in the liquid nitrogen. But, amorphous coatings could be manufactured with the rotation cooling method by liquid nitrogen. In the fabrication of amorphous coatings, major factor was the rapid cooling by rotation of the substrate. 2) Hardness of coatings was obtained Hv 960 by formation of amorphous phase. But, wear resistance decreased. That was due to porosity in the coatings by the rapid cooling. 3) In the case of corrosion resistance, amorphous coatings were superior to air-cooled coatings. That was due to formation of amorphous phase. 4) After amorphous coatings were heat-treated at 520℃ for 1hr. hardness increased 80% and wear resistance increased 30% comparing with air cooled coatings. These were due to crystallization of amorphous phase and decrease of porosity by heat-treatment.

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HREM Analysis of Apatite Formation in Modified-Simulated Body Fluid Containing Bovine Serum Albumin (소 혈청 알부민이 함유된 유사체액 내에서 아파타이트의 생성에 대한 고분해능 전자현미경 분석)

  • Kim, Woo Jeong;Lee, Kap Ho;Hong, Sun Ig
    • Korean Journal of Metals and Materials
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    • v.46 no.2
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    • pp.105-110
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    • 2008
  • Process of the hydroxyapatite (HA) formation on bioactive titanium metal prepared by NaOH treatment in a modified-simulated body fluid (mSBF) containing bovine serum albumin (BSA) was investigated by high resolution transmission electron microscope attached with energy dispersive X-ray spectrometer (EDX). The amorphous titanate, which was formed on titanium surface by NaOH treatment, combined with the calcium ions in the liquid to form an amorphous calcium titanite. With increasing of soaking time in the liquid, an amorphous calcium titanite combined with the phosphate ions to form an amorphous calcium phosphate with low Ca/P atomic ratio, and it grows as aggregates of plate (or needle)-like substance on titanium surface. The crystalline apatite layers, which are needle-shaped with the c axis parallel to the long axis, are formed in an amorphous calcium phosphate with further increase in soaking time. The formation of needle-shaped apatite layers can be explained by electrostatic effects and difference of concentration between calcium, phosphate, and albumin ions.

A Feasibility Study on the Brazing of Zircaloy-4 with Zr-Be Binary Amorphous Filler Metals (비정질 이원계 합금 Zr-Be 용가재를 이용한 지르칼로이-4의 브레이징 타당성 검토)

  • 고진현;박춘호;김수성
    • Journal of Welding and Joining
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    • v.17 no.4
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    • pp.26-31
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    • 1999
  • An attempt was made in this study to investigate the brazing characteristics of Zr-Be binary amorphous alloys for the development of a new brazing filler metal for joining Zircaloy-4 nuclear fuel cladding tubes. This study was also aimed at the feasibility study of rapidly solidified amorphous alloys to substitute the conventional physical vapor-deposited(PVD) metallic beryllium. The $Zr_{1-x}Be_{x}$($0.3\leq$x$\leq0.5$) binary amorphous alloys were produced in the ribbon form by the melt-spinning method. It was confirmed by x-ray diffraction that the ribbons were amorphous. The amorphous. the amorphous alloys were used to join bearing pads on Zircaloy-4 nuclear fuel cladding tubes. Using Zr-Be amorphous alloys as filler metals, it was found that the reduction in the tube wall thickness caused by erosion was prevented. Especially, in the case of using $Zr_{0.65}Be_{0.35}$ and $Zr_{0.7}Be_{0.3}$ amorphousalloys, the smooth and spherical primary $\alpha$-Zr particles appeared in the brazed layer, which was the most desirable microstructure from the corrosion-resistance standpoint.

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Drug Polymorphism and its Importance on Drug Development Process

  • Jeong, Seong-Hoon;Youn, Yu-Seok;Shin, Beom-Soo;Park, Eun-Seok
    • Journal of Pharmaceutical Investigation
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    • v.40 no.spc
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    • pp.9-17
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    • 2010
  • Polymorphism has been recognized to be a critical issue throughout the drug product development process. Most of solid phase drugs have polymorphism, which has generated a great deal of interest and the field has been evolving rapidly. Preferably, thermodynamically most stable form of a drug substance is selected to obtain consistent bioavailability over its shelf life and various storage conditions. Moreover, it has the lowest potential for conversion from one polymorphic form to another. However, metastable or amorphous forms may be used intentionally to induce faster dissolution rate for rapid drug absorption and higher efficacy. For pharmaceutical industry, polymorphism is one of the key activities in form selection process together with salt selection. This article introduces the main features in the investigation of solid form selection especially polymorphic behavior with thermodynamic backgrounds, physicochemical properties with solubility, dissolution, and mechanical properties, and characterization techniques for proper analysis. The final form can be recommended based on the physicochemical and biopharmaceutical properties and by the processability, scalability and safety considerations. Pharmaceutical scientists especially in charge of formulation need to be well aware of the above issues to assure product quality.