• Title/Summary/Keyword: Solvent-Evaporation Method

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Enhanced Nasal Absorption of Ketoconazole by Inclusion with Cyclodextrin (시클로덱스트린과의 포접에 의한 케토코나졸의 비점막 흡수증가)

  • Park, Gee-Bae;Seo, Bo-Youn;Ann, Hong-Jik;Rho, Hyun-Goo;Onn, Yun-Sung;Lee, Kwang-Pyo
    • Journal of Pharmaceutical Investigation
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    • v.24 no.2
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    • pp.95-104
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    • 1994
  • Inclusion complexes of ketoconazole(KT) with ${\alpha}^_$, ${\beta}^_$cyclodextrin(CD) and $dimethy1-{\beta}-cyclodextrin$ (CD) and $dimethy1-{\beta}-cyclodextrin(DM{\beta}CD)$ as nasal absorption enhancer were prepared in 1: 2 molar ratios by freeze-drying and solvent evaporation methods. In order to compare with the intrinsic absorptivity of KT in the jejunum(J) and the nasal cavity(N), the in situ simultaneous perfusion method was employed. The in situ recirculation study revealed that KT-CD inclusion complexes with the greater stability constant and the faster dissolution rate proportionally increased the absorption of KT in the J and N of rats. The rank order of apparent KT permeability$(P_{app}\;:\;cm/sec\;{\time}\;1O^{-5}{\pm}S.E.)$, corrected by surface area of absorption, was $5.10{\pm}0.3(N,\; KT-DM{\beta}CD)$ )> $4.13{\pm}0.4(N,\;KT-{\beta}-CD)$ )> $3.52{\pm}0.2(N,\;KT-{\alpha}-CD)$ )> $2.76{\pm}0.3(J,\; KT-DM{\beta}CD)$ )> $2.61{\pm}0.5(J,\;KT-{\beta}-CD)$ )> $2.42{\pm}0.4(J,\;KT-{\alpha}-CD)$ at pH 4.0. The in crease in permeability of $KT-DM{\beta}CD$ inclusion complex was 2.6 folds in the J and 4.5 folds in the N when the perfusing solution was changed from the buffer(pH 4.0) to saline. The absorption rate of $KT-DM{\beta}CD$ inclusion complex after nasal administration was more rapid than those of ketoconazole alone and $KT-DM{\beta}CD$ inclusion complex after oral administration to rats. In comparision with an oral administration of ketoconazole suspension in corn oil, the relative bioavailability was calculated 137.3% for the oral and 195.0% for nasal $KT-DM{\beta}CD$ inclusion complex in rats. The present results suggest that $KT-DM{\beta}CD$ inclusion complex may serve as a potential nasal absorption enhancer for the nasal delivery of ketoconazole.

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Solubilization and Fomulation as Soft Gelatine Capsule of Biphenyldimethyldicarboxylate (비페닐디메칠디카르복실레이트의 가용화 및 연질캅셀제로의 설계)

  • Park, Gee-Bae;Chung, Chae-Kyong;Lee, Kwang-Pyo
    • Journal of Pharmaceutical Investigation
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    • v.26 no.1
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    • pp.1-11
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    • 1996
  • Biphenyldimethyldicarboxylate (PMC), which has been used to treat hepatitis, is insoluble in water, therefore it has low bioavailability after oral administration. For the purpose of increasing the dissolution rate of PMC, the physical mixtures and inclusion complexes of PMC and $dimethyl-{\beta}-cyclodextrin\;(DM\;{\beta}CD)\;or\;hydroxypropyl-{\beta}-cyclodextrin\;(HP{\beta}CD)$ in molar ratio of 1 : 1 and 1 : 2 were prepared by solvent evaporation method. Mixed micelles of PMC were prepared by reacting PMC with bile salts [sodium cholate(NaC), sodium glycocholate (NaGC)] and oleic acid (OA) or palmitoylcarnitine chloride(PCC). Chloroform/water partition coefficient (PC) of PMC was 36.14 in artificial gastric juice (AGJ) and 33.47 in artificial intestinal juice (AIJ), respectively, on the other hand octanol/water PC was 63.36. PMC formulation was prepared by reacting PMC with PEG400-glycerin system(95 : 5, 90 : 10, respectively) and PEG400-PEG4000-glycerin system (70 : 25 : 5, 65 : 25 : 10, respectively). Dissolution test was performed in AGJ and AIJ by paddle method at $37{\pm}0.5^{\circ}C$. The dissolution rates of PMC tablets on the market were 5.74% and 8.26% at AGJ and AIJ, respectively and marketed PMC capsules were 22.14% and 28.64% at AGJ and AIJ, respectively. The dissolution rates of inclusion complexes of PMC with $DM{\beta}CD$ and $HP{\beta}CD$ in a molar ratio of 1 : 1 were more fast than those of corresponding physical mixtures. The decreasing order of dissolution rates was as follows; PMC-PEG400-PEG4000-glycerin formulation > PMC-PEG400-glycerin formulation > mixed micelles > CD inclusion complexes. The dissolution rates of PMC-PEG400-glycerin and PMC-PEG400-PEG4000-glycerin formulation were most fast and the percentage of dissolution was almost 100% within 20 minutes. And their dissolution rates after 120 minutes were markedly increased as compared with capsules on the market (4.0-fold and 3.2-fold in PMC-PEG400-glycerin formulation at AGJ and AIJ, respectively, and 4.8-fold and 3.7-fold in PMC-PEG400-PEG4000-glycerin formulation at AGJ and AIJ, respectively).

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Sibutramine Release Behavior from Microspheres Prepared by Spray-Dry Method (분무건조 방법으로 제조된 미립구에서 Sibutramine의 방출거동)

  • Park, Jung-Soo;Oh, Jung-Soo;Oh, Jae-Min;Kim, Yun-Tae;Lee, Jun-Hee;Mo, Jong-Hyun;Lee, Hai-Bang;Khang, Gil-Son
    • Polymer(Korea)
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    • v.32 no.3
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    • pp.193-198
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    • 2008
  • Sibutramine is a highly crystalline and poorly water soluble drug as the appetite depressant for obesity treatment. In order to increase water solubility of sibutramine, microspheres including sibutramine were prepared by solid dispersion method using a spray dryer. The crystallinity and morphology of the prepared microspheres were confirmed by SEM and XRD. The morphology of micro spheres has gradually changed into spherical shape as increasing evaporation rate of solvent. According to XRD analysis, crystallinity of sibutramine in micro spheres was decreased by below 10%. Release behavior of microspheres was investiaged at pH 1.2, pH 6.8, and solubility of the sibutramine was significantly different depending on pH. The hard capsule showed fast release of sibutramine comparing with the tablet. These results demonstrated that the pharmaceutical preparation is able to control the release behaviors.

A review on Separation Technologies for Lithium Recovery from Waste Solutions in Recycling Process of Waste Battery (폐배터리 재활용 공정 폐액 중 리튬 회수를 위한 분리 기술 고찰)

  • Song, Daesung;Kim, Eunkyu;Vu, Thang-Toan
    • Korean Chemical Engineering Research
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    • v.60 no.4
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    • pp.473-477
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    • 2022
  • In this study, candidate technologies for lithium recovery from the process waste liquid generated in the waste battery recycling process were reviewed, and technologies applicable to the process from the commercialization point of view were reviewed from a qualitative point of view. The evaporation method is difficult to apply because it requires a large-scale land and shows a low recovery rate due to the loss of Li during the concentration process. In the case of precipitation, a commercially available technology shows a high recovery rate due to the high Li/Na selectivity of phosphoric acid, but there are disadvantages in that the process is complicated due to the use of expensive phosphoric acid, requiring a recovery step, and continuous operation is impossible because solids are handled in the Li concentration process. In the case of solvent extraction, if we find an inexpensive extractant with high Li/Na selectivity, continuous operation is possible with the method used in extraction of other metals in the previous step, and when Li is concentrated, continuous operation is possible because it is in a liquid state. If it shows a similar recovery rate compared to precipitation technology, commercialization will be the most likely.

Removal of Ethylene Over KMnO4/Silica-alumina: Effect of Synthesis Methods and Reaction Temperatures (KMnO4/실리카-알루미나 상에서 에틸렌 제거: 합성 방법과 반응온도의 영향)

  • Cho, Min-Whee;Yoon, Songhun;Park, Yong-Ki;Choi, Won Choon;Kim, Hee Young;Park, Seungkyu;Lee, Chul Wee
    • Applied Chemistry for Engineering
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    • v.20 no.4
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    • pp.407-410
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    • 2009
  • 18~19 wt% $KMnO_4$/$SiO_2-Al_2O_3$ with Si/Al = 1/5 and 1/10, and 20 wt% $KMnO_4$/$Al_2O_3$ were prepared by solvent evaporation method. Catalytic activity of ethylene abatement over those samples were evaluated and compared under the conditions of GHSV $1125h^{-1}$, ethylene gas (ethylene 0.2%, air 99.8%, relative humidity 50%) at 30, 40, 60 and $120^{\circ}C$ using a fixed-bed reactor. $KMnO_4$/$SiO_2-Al_2O_3$ was showed better performance than $KMnO_4$/$Al_2O_3$ by 170~210% at 30, $40^{\circ}C$, and by 60% at 60, $150^{\circ}C$, respectively.

Hydrophobic Cyclodextrin Derivatives as a Sustained Release Carrier of Azidothymidine (아지도싸이미딘의 지속성방출형담체로서의 소수성시클로덱스트린유도체)

  • Seo, Bo-Youn;Park, Gee-Bae;Lee, Kwang-Pyo
    • Journal of Pharmaceutical Investigation
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    • v.26 no.2
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    • pp.71-82
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    • 1996
  • This study has been undertaken to evaluate hydrophobic cyclodextrin(CD) derivatives as a sustained release carrier of azidothymidine(AZT), AZT, which has potent activity against AIDS and AIDS-related complex as thymidine analogue, has been reported that it has significant toxicity and short half life. Therefore, it is necessary to design sustained release oral dosage form to avoid undesirable side effects attributable to an excessive plasma concentration and to reduce the frequency of administration of AZT. Inclusion complexes of AZT with $acetyl-{\beta}-cyclodextrin\;(AC{\beta}CD)$ and $triacetyl-{\beta}-cyclodextrin(TA{\beta}CD)$ were prepared by solvent evaporation method. Interactions of AZT with CD were investigated by Differential Scanning Calorimetry(DSC) and Infrared Spectrophotometry(IR). The decreasing order of water solubilities of AZT and AZT-CD inclusion complexes were as follows; $AZT\;(27.873{\pm}0.015,mg/ml)\;>\;AZT-AC{\beta}CD\;(3.377{\pm}0.003)\;>\;AZT-TA{\beta}CD\;(2.528{\pm}0.001)$. Partition coefficients of $AZT-AC{\beta}CD\;and;\AZT-TA{\beta}CD$ inclusion complexes were increased by 1.27-fold, 1.54-fold in pH 1.2 and 1.32-fold, 1.47-fold in pH 6.8 in comparison with that of AZT. The mean dissolution time (MDT, min) which represents the rapidity of dissolution rate of AZT, $AZT-AC{\beta}CD,\;AZT-TA{\beta}CD$ were 5.12, 14.02 and 19.38 min in pH 1.2 and 2.52, 15.19 and 18.19 min in pH 6.8. AZT was very rapidly and completely dissolved in pH 1.2 and pH 6.8 within 5 minutes. But AZT-CD inclusion complexes showed the sustained release pattern in comparison with AZT alone. The simultaneous in situ nasal and jejunal recirculation study to compare the intrinsic absorptivity and the property of absorption sites revealed that the absorption of $AZT-TA{\beta}CD\;(N:35.35{\pm}1.08%,\;J:27.47{\pm}1.18%)$ was more than that of $AZT\;(N:16.89{\pm}2.25%,\;J:15.86{\pm}2.33%)$. The above results suggest that $TA{\beta}CD$ which is a hydrophobic cyclodextrin may serve as sustained release carrier with absorption enhancing effect.

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Enhancement of cyanoacrylate-developed marks using p-dimethylaminobenzaldehyde (DMAB) on semi-porous surfaces and analysis of the influence factors on fluorescence intensity (반다공성 재질에 유류된 지문의 CA 훈증 후 p-dimethylaminobenzealdehyde(DMAB) 형광시약 적용 시 표면적과 주변 온도, 기압이 형광착색에 미치는 효과에 관한 연구)

  • Yu, Je-Sul;Kim, Ju-Hah
    • Analytical Science and Technology
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    • v.27 no.4
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    • pp.187-195
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    • 2014
  • It is very important to minimize the damage of latent fingerprints at enhancing the contrast. This study proves the enhancement effects of cyanoacrylate-fumed latent fingerprints using p-dimethylaminobenzealdehyde (DMAB) on semi-porous surfaces and the influence factors. The latent fingerprints in experiment were developed for cyanoacrylate treatment in a vacuum chamber and used after drying at room temperature for 24 hours. For fluorescence staining, the cyanoacrylate-developed marks using DMAB were sublimated during 48 hours under the different conditions of surface area, temperature, atmospheric pressure. First experiment showed how surface area effects on the sublimation rate and fluorescence intensity by DMAB of particle size and container size. In addition, the fluorescence staining using DMAB with solvent-free contact method had the greatest fluorescence intensity after 36 hours and a low fluorescence intensity over a certain size of surface area. Second experiment showed that the evaporation of DMAB solid crystals got a satisfying result in a temperature of $20^{\circ}C$ and reduced time to get the greatest fluorescence intensity. It took a long time to get a optimum level of fluorescence intensity at $30^{\circ}C$ or more and it was less effective in fluorescence intensity. Third experiment on the pressure indicated that the fluorescence intensity of vacuum was weaker than nonvacuum but it was inapplicable to very high variations in pressure.

Influence of Surface Treatment of SiO$_2$ and Stirring Rate on Fragrant Oil Release Behavior of Poly($\varepsilon$-caprolactone) Microcapsules (실리카의 표면 처리와 교반 속도가 폴리카프로락톤 마이크로캡슐의 향유 방출 거동에 미치는 영향)

  • 박수진;양영준;이재락;서동학
    • Polymer(Korea)
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    • v.27 no.5
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    • pp.464-469
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    • 2003
  • In this work, the fragrant oil release behavior of poly($\varepsilon$-caprolactone) (PCL) microcapsules containing SiO$_2$ was investigated. The SiO$_2$ was chemically treated in 10, 20, and 30 wt% hydrochloric acid and sodium hydroxide. The acid and base values were determined by Boehm's titration technique and $N_2$/77 K adsorption isotherm characteristics, the specific surface area and total pore volume were studied by BET. The PCL microcapsules containing SiO$_2$ and fragrant oil were prepared by oil-in-water (o/w) emulsion solvent evaporation method. The shape and surface of PCL microcapsules were observed using image analyzer and scanning electron microscope (SEM). The fragrant oil release behavior of PCL microcapsules was characterized using UV/vis. spectra. The average diameters of PCL microcapsules were decreased from 35 to 21 $\mu$m with increasing stirring rate. It was found that in the case of acidic treatment the fragrant oil adsorption capacity and release rate were increased due to the increase of specific surface area and acid value. In the case of basic treatment, the fragrant oil adsorption capacity and release rate were decreased due to the decrease of sp ecific surface area and the increase of acid-base interactions between SiO$_2$-NaOH and fragrant oil with increasing base value of SiO$_2$.

Effect of Molecular Weight of PLGA on Release Behavior of Doxorubicin for Double-Layered PLGA Microspheres (PLGA 분자량에 따른 이중층 독소루비신 미립구의 방출거동)

  • Park, Jung-Soo;Yang, Jae-Chan;Yuk, Soon-Hong;Shin, Hyung-Shik;Rhee, John-M.;Kim, Moon-Suk;Lee, Hai-Bang;Khang, Gil-Son
    • Polymer(Korea)
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    • v.31 no.3
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    • pp.189-193
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    • 2007
  • We developed the doxorubicin-loaded PLGA double-layered microspheres using relatively simple oil-in-water (O/W) solvent evaporation method for sustained release of doxorubicin and investigated the release behavior according to PLGA molecular weight and initial drug loading. The double-layered microsphere was characterized on the surface, the cross-section morphology, the behavior of doxorubicin release for 5 weeks by SEM and fluorescence spectrophotometer. Double-layered microspheres showed smooth surfaces and clear difference between core and outer-shell. As the PLGA molecular weight increased, the release rate of doxorubicin-loaded, double-layered microspheres decreased. These results showed that the release behaviors can be controlled by the variation of molecular weight of PLGA.

Preparation and Release Behavior of Atorvastatin Calcuim - Encapsulated Polyoxalate Microspheres (아토르바스타틴 칼슘을 함유한 폴리옥살레이트 미립구의 제조 및 방출거동)

  • Lee, Cheon Jung;Kim, Su Young;Lee, Hyun Gu;Yang, Jaewon;Park, Jin Young;Cha, Se Rom;Lim, Dong-Kwon;Lee, Dongwon;Khang, Gilson
    • Polymer(Korea)
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    • v.38 no.5
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    • pp.656-663
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    • 2014
  • Atorvastatin calcium-loaded polyoxalate (POX) microspheres were prepared by an emulsion solvent-evaporation/ extraction method of oil-in-oil-in-water ($O_1/O_2/W$) for sustained release. We investigated the release behavior according to initial drug ratio, molecular weight ($M_w$) and concentration of POX and concentration of emulsifier. The microsphere was characterized on the surface, the cross-section morphology and the behavior of atorvastatin calcium release for 10 days by scanning electron microscopy (SEM) and high performance liquid chromatography (HPLC). The analysis of crystallization was analyzed to use X-ray diffraction (XRD), differential scanning calorimeter (DSC) and Fourier transform infrared (FTIR). These results showed that the release behaviors can be controlled by preparation conditions.