• Title/Summary/Keyword: Solvent evaporation

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Preparation and Evaluation of Sustained-Release $Eudragit^{\circledR}$ Microcapsules Containing ${\beta}-Lactam$ Antibiotics ($Eudragit^{\circledR}$ 마이크로캅셀화에 의한 ${\beta}$-락탐계 항생물질의 방출제어제제 개발)

  • Han, Kun;Shin, Do-Su;Jee, Ung-Kil;Chung, Youn-Bok
    • Journal of Pharmaceutical Investigation
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    • v.22 no.4
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    • pp.267-279
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    • 1992
  • Microencapsulations of amoxicillin and cephalexin, using Eudragit RS, RL, E, S and L were investigated. The microcapsules were prepared by the solvent evaporation process in liquid paraffin phase, which is based on dispersion of acetone/isopropanol containing the drug in liquid paraffin. Aluminium tristearate was used as an additive for the preparation of microcapsules. The size distribution, dissolution test and observation by SEM were examined. Good reproducibility in microcapsule preparation was observed. The microcapsules obtained were spherical and free-flowing particles. The dissolution rates of amoxicillin and cephalexin from the microcapsules were considerably decreased as compared with those from amoxicillin and cephalexin powder, respectively. As the dispersing agents (aluminium tristearate) increased, the particle size of microcapsules decreased and the dissolution rate increased. In order to control the release rate of drugs, microcapsules were prepared by mixing Eudragit RS/RL or Eudragit S/L. As Eudragit RL ratio in microcapsule of Eudragit RS/RL increased, the dissolution rate increased. As Eudragit L ratio in microcapsule of Eudragit S/L increased, the dissolution rate increased. Furthermore, the release rates of drugs from Eudragit RS/L or RS/polyelthylene glycol 1540 (PEG 1540) were examined. The dissolution rate of drugs increased with increasing of Eudragit L or PEG 1540 ratio. In conclusion, the release rates of drugs from Eudragit RS/RL or RS/PEG 1540 microcapsule could be controlled, and these microcapsules will be convenient for reducing frequency of administration.

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Preparation and Dissolution of Polyvinylpyrrolidone(PVP)-Based Solid Dispersion Systems Containing Solubilizers (가용화 조성물을 함유한 PVP형 고체분산체의 제조 및 특성)

  • Cao, Qing-Ri;Kim, Tae-Wan;Choi, Choon-Young;Kwon, Kyoung-Ae;Lee, Beom-Jin
    • Journal of Pharmaceutical Investigation
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    • v.33 no.1
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    • pp.7-14
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    • 2003
  • The PVP-based solid dispersion systems (SDs) containing lovastatin (LOS) and solubilizers (sodium lauryl sulfate, tween 80 and oleic acid) were prepared to enhance dissolution rate of practically water insoluble LOS using solvent evaporation method. Two different organic cosolvents either acetone/ethanol or acetonitrile/ethanol were used for the preparation of SDs. The LOS contents were highly decreased when acetone/ethanol cosolvents were used. The decrease of LOS contents was not caused by acetonitrile or acetone, based on HPLC data. The surface morphology as investigated by scanning electron microscope (SEM) and angle of repose as an index of flowability of SDs were highly dependent on the type and amount of solubilizers used. Based on differential scanning calorimetry (DSC) and X-ray powder diffraction data, the SDs made crystalline LOS into amorphous structure or partially eutectic mixtures. The simultaneous use of the solubilizers in SDs was also useful to increase dissolution rate of LOS in gastric or intestinal fluid. The SDs containing solubilizers reached 76% and 60% in gastric and intestinal fluid, respectively but the commercial tablet gave only less than 4%. These solubilizers in SDs could be also applicable for enhancing dissolution and bioavailability of poorly water-soluble drugs.

Characteristics of the Major Atmospheric Aromatic Hydrocarbons in the Yellow Sea

  • Park, Seung-Myung;Kim, Jeong-Soo;Lee, Gangwoong;Jang, Yuwoon;Lee, Meehye;Kang, Chang Hee;Sunwoo, Young
    • Asian Journal of Atmospheric Environment
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    • v.9 no.1
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    • pp.57-65
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    • 2015
  • We measured the concentrations of five aromatic hydrocarbons (benzene, toluene, ethylbenzene, m,p-xylene, and styrene) in the atmosphere during four seasonal campaigns at Deokjeok and Jeju Islands in the Yellow Sea from October 2005 to June 2006. Toluene was the most abundant aromatic hydrocarbon, with median of 0.24 ppb at Deokjeok and 0.20 ppb at Jeju, followed by benzene (0.21 ppb, 0.15 ppb) and m,p-xylene (0.06 ppb, 0.06 ppb). Aromatic hydrocarbon measurements exhibited the typical seasonality of the major emission sources, such as vehicle exhaust, solvent evaporation, and regional circulation patterns. The ratios of m,p-xylene/ethylbenzene of 1.57 at Deokjeok and 1.05 at Jeju reflected the degree of proximity to outflows of each source region, South Korea and China. The toluene/benzene ratios of 1.0 were consistently both on field observations and on the 3-D chemical model simulation, which is slightly higher than that in the Western Pacific area. It implied that the air over the Yellow Sea was influenced to a great extent by the surrounding areas. We confirmed that current emission inventories of aromatic hydrocarbons in Northeast Asia reasonably reproduced temporal and spatial variations of toluene and benzene over the Yellow Sea.

Preparation of Dexamethasone-21-palmitate Incorporated Lipid Nanosphere: Physical Properties by Varying Components and Ratio of Lipid (팔미틴산덱사메타손이 봉입된 지질나노입자의 제조: 지질종류와 함량에 따른 물리적 특성)

  • Jung, Suk-Hyun;Lee, Jung-Eun;Seong, Ha-Soo;Shin, Byung-Cheol
    • Journal of Pharmaceutical Investigation
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    • v.36 no.6
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    • pp.355-361
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    • 2006
  • Intraarticular corticosteroid injections for therapy of rheumatic arthritis are administered with the aim of optimal local anti-inflammatory effect at the injection site. Since the side effects of corticosteroidal drug, dexamethasone(DEX), administered at hish dose limited the therapeutic efficacy, there was a need to design a new drug delivery system for controlled release of dexamethasone. As a prodrug for continuous therapeutic efficacy, dexamethasone-21-palmitate(DEX-PAL) was prepared via esterification of palmitoyl chloride and dexamethasone. DEX-PAL was identified by NMR and MASS analysis. DEX-PAL or DEX was entrapped in lipid nanosphere which could be prepared by using a self emulsification-solvent evaporation method. Physicochemical characteristics such as mean particle diameter, zeta potential and drug loading efficiency of the lipid nanospheres were investigated with variation of either the kind of lipid or the lipid composition. The lipid nanospheres had a mean diameter $83{\sim}95$ nm and DEX-PAL loading efficiency of up to 95%. The drug loading efficiency increased with the increase of aliphatic chain length attached to the phospholipid. The incorporation of cationic lipid was very efficient for both reducing particle size of lipid nanospheres and enhancing drug loading efficiency. The lipid nanospheres containing DEX-PAL may be a promising novel drug carrier for the controlled release of the poorly water-soluble drugs.

Preparation and Drug Release of All-Trans Retinoic Acid-Loaded Poly(L-lactic acid) Nanoparticles (레티노산 함유 폴리락탄산 나노입자의 제조 및 약물 방출)

  • Chae, Ji-Man;Lee, Kyung-Man;Kim, In-Sook;Lee, Yong-Bok;Shin, Sang-Chul;Oh, In-Joon
    • Journal of Pharmaceutical Investigation
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    • v.34 no.5
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    • pp.401-406
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    • 2004
  • To develop an intravenous delivery system of all-trans retinoic acid (ATRA) for the cancer therapy, poly(L-lactic acid) nanoparticles were prepared and characterized. Emulsification-solvent evaporation method was chosen to prepare submicron sized nanoparticles. Spherical nanoparticles less than 200 nm in diameter with narrow size distribution were prepared, and the entrapment efficiency of drug was more than 95%. The endothermic peak at $183^{\circ}C$ and X-ray crystallographic peak of ATRA appeared in the nanoparticle system, suggesting the inhibition of crystallization of ATRA by polymer adsorption during the precipitation process. ATRA was released at $37^{\circ}C$ for 60 days and the release rate was dependent on the concentration of drug incorporated in the nanoparticles. While ATRA was unstable in the light, it was very stable at $4^{\circ}C$. These results suggest the usefulness of PLA nanoparticles as a sustained and prolonged release carrier for ATRA.

Physical Properties of Gelucire-based Solid Dispersions Containing Lacidipine and Release Profiles (Lacidipine 함유 Gelucire 고체분산체의 물성 및 방출)

  • Park, Jun-Bom;Choi, Jong-Seo;Lee, Seung-Chul;Lee, Ho;Lee, Beom-Jin;Kang, Chin-Yang
    • Journal of Pharmaceutical Investigation
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    • v.40 no.1
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    • pp.9-14
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    • 2010
  • Lacidipine used for the treatment of hypertension has low water solubility and is classified as BCS Class II category. Gelucire-based solid dispersions (SD) containing lacidipine were prepared by solvent evaporation method to enhance drug dissolution. The powdered forms of SD showed irregularly spherical shape. Thermal behaviors of SD from differential scanning calorimetry indicated that distinct endothermic peak of lacidipine ($184^{\circ}C$) was shifted to lower region ($150.1^{\circ}C$). Drug was present in a crystalline form. NMR spectra also showed some molecular interaction between drug and Gelucire. There was no significant difference in DSC and NMR behaviors between Gelucire 44/14 and Gelucire 50/13. The initial dissolution rate of SD-loaded tablet linearly increased both in water and in water containing 1% tween 20, and much higher than the commercial tablet, $Vaxar^{(R)}$. When the amount of SD was increased, the release rate was greater. The Gelucire 50/13 showed higher dissolution than the Gelucire 44/14. The produced solid dispersion with various kinds of excipients and making tablets, it was found that solid dispersions can increase the solubility in artificial gastric juice and finally increases dissolution rate.

Development of Alkoxysilane Mixed Solution as Stone Preservation and Consolidation Materials (알콕시 실란계 석재 보존 및 강화제 개발)

  • Kim, Eun-Kyung;Park, Seong-Yong;Cho, Hyun-Dong;Won, Jong-Ok;Do, Jin-Young;Kim, Sa-Dug
    • Journal of Conservation Science
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    • v.21
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    • pp.21-32
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    • 2007
  • Low-viscosity alkoxysilanes that polymerize into the porous network of decayed stone by a sol-gel process are widely used as stone consolidants. During drying, the gel network contracts due to capillary pressure generated by solvent evaporation. We have prepared tetraethoxysilane mixed solution containing methyltrisilane, ethyl trisilane and (3-glycidyloxypropyl)trimethoxysilane having epoxy ring in order to reduce the shrinkage happened inside the stone porous structure during the gel formation. Mixed solutions were applied into sandstone and granites and characterized by FT-IR, SEM. The gelation time, water uptake, contact angles were measured and compared with those of the commercial stone conservation materials.

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The Extraction of Metal Contaminants using Supercritical CO2 (초임계이산화탄소를 이용한 방사성 금속이온 추출)

  • Ju, Minsu;Kim, Jung-Hoon;Kang, Se-Sik
    • The Journal of the Korea Contents Association
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    • v.16 no.5
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    • pp.660-667
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    • 2016
  • Conventional decontamination methods utilize water-based systems, which generate high amounts of secondary wastes. Herein, we describe an environmentally benign decontamination method using liquid and supercritical $CO_2$. The use of $CO_2$ as a solvent affords effective waste reduction by its ability to be recycled, thereby leaving be hind only the contaminants upon its evaporation. In this study, a $CO_2$ solution process was assessed using t-salen(t-butylsalen), DC18C6 (dicyclohexano-18Crown6), 8-HQN(8-hydroxyquinoline), NEt4PFOSA(perfluoro-1-octanesulfonic acid tetra-ethyl ammonium salt), and NEt4PFOA(pentadecafluorooctanoic acid ammonium salt) to extract spiked radioactive contaminants(Nb,Zr,Co,Sr) from an inert sample matrix, namely filter paper. With the static extraction method, Sr was extracted with a maximum extraction rate of 97%, and Nb was extracted with a maximum extraction rate of 75%. Additionally, we were also able to extract Co and Zr with maximum extract ion ratesof 73% and 64%, respectively.

Isolation and Structure Identification of Phytotoxins from Lasiodiplodia theobrorme, the Cause of JAVA Black Rot of Sweet Potato (고구마 검은썩음병균(Lasiodiplodia theobromae)으로부터 식물독소의 분리 및 구조)

  • Lim, Chi-Hwan
    • Korean Journal of Agricultural Science
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    • v.25 no.1
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    • pp.118-123
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    • 1998
  • Lasiodiplodia theobrorme is a pathogen of Java black rot on sweet potato. This fungus infects the tuberous root during storage after harvest. Invasion of the fungus results in the expansion of necrosis sites into the tuberous roots. The resultant necrotic symptom of the tissue is also induced by application of acetone extract of the fungus growing on potato sucrose agar (PSA) culture. The active principles to induce the necrosis are purified from the acetone extract as follows. After evaporation of hexane-benzene-EtOAc (1:2:1, v/v/v) the extract was fractioned on silica gel column, using a solvent gradient system from n-hexane to EtOAc and then to MeOH. The active fractions were purified with HPLC on Nucleosil 50-5 column by eluting n-hexane to EtOAc. Their structures are established by using spectroscopic techniques and synthesis to 4-hydroxymellein and mellein, respectively. Application of small amount of these compounds induce expansion of the necrotic symptom into the tissue and accumulated ipomeamarone. Conclusively, these compounds acted as phytotoxins (inducing necrosis) and as elicitors (eliciting the phytoalexin).

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The Influence of Water Storage on Mechanical Properties of Adhesive Resin (수중 보관이 접착용 레진의 물리적 성질에 미치는 영향)

  • Kim, Won-Chan;Lee, Kwang-won;Lee, Jeong;Yu, Mi-Kyoung;Kim, Jeong-Hee
    • Journal of Dental Rehabilitation and Applied Science
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    • v.22 no.2
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    • pp.193-202
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    • 2006
  • Objective To evaluate the influence of water storage on the mechanical properties of dental adhesives over 1 and 3 months. Materials and Methods Adhesive resin sheets were prepared by pouring either All-bond 2(AB), Clearfil SE Bond(SE) into a mold measuring $15{\times}15{\times}0.9mm$. After solvent in primer evaporation, the adhesives were light-cured and removed from the mold and divided in two pieces, trimmed to hourglass shape that were used to determine the micro-tensile strength(MTS). Another hourglass shaped metal mold measuring $2.0{\times}1.5mm$ in cross-section area was made to determine the Young's modulus(E). Adhesive specimens for Young's modulus(E) were prepared in the same method. Specimens were stored at $37^{\circ}C$ in distilled water and tested after 1 and 3 months. The data were analyzed by one-way ANOVA and Tukey's test. Results Water storage significantly decreased the micro-tensile strength(MTS) of AB and SE specimens after 1 and 3 months(P<0.05). The Young's modulus(E) were also decreased after water storage for 1 and 3 months, but statistically not significant in each group of AB and SE group respectively. Conclusions Long-term exposure of adhesive resin to water can cause reduction of mechanical properties. It may compromise resin/dentin bonds and affect longevity of restorations.