• Title/Summary/Keyword: supercritical anti-solvent

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Preparation of Microparticulate Itraconazole/Hydroxypropyl-$\beta$-cyclodextrin Inclusion Complexes Using a Supercritical Anti-Solvent [SAS] Process (초임계 역용매 공정을 이용한 Itraconazole/Hydroxypropyl-$\beta$-cyclodextrin 포접복합체 미세입자 제조)

  • 이상윤;김정규;김우식;유종훈;임교빈
    • KSBB Journal
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    • v.19 no.4
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    • pp.321-326
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    • 2004
  • Microparticles of an inclusion complex between itraconazole and 2-hydroxypropyl-${\beta}$-cyclodextrin (HP-${\beta}$-CD) were prepared using an environmentally-benign supercritical anti-solvent (SAS) process. In order to evaluate the degree of complexation, the thermal behavior of solid micro particulate complexes was investigated using differential scanning calorimetry. The experimental results obatined for the solubility and dissolution rate of the microparticulate inclusion complexes in a buffer solution of pH 1.2 showed that the complexation of itraconazole with HP-${\beta}$-CD results in a significant increase in the solubility and dissolution rate of itraconazole. For the microparticulate itraconazole/Hp-${\beta}$-CD inclusion complexes prepared by the SAS process, about 80% of itraconazole was found to dissolve in the buffer solution. Our experimental results confirmed that the SAS process is a promising method for the preparation of microparticles of water-insoluble drug/cyclodextrin inclusion complexes.

Preparation and Characterization of Microparticles of $Poly(\gamma-glutamic\;acid)$ Containing Lysozyme by means of Supercritical Anti-Solvent (SAS) Precipitation Process (초임계 반용매 침전법에 의한 라이소자임이 내포된 폴리감마글루탐산의 미세입자 제조 및 특성)

  • Lee, Dong-Il;Ling, Yun;Sung, Moon-Hee;Park, Il-Hyun
    • Polymer(Korea)
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    • v.31 no.2
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    • pp.168-176
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    • 2007
  • The sub-micron particles of poly ($\gamma-glutamic$ acid) (PGA) containing lysozyme have been prepared using supercritical antisolvent (SAS) precipitation process at various experimental conditions such as pressure, temperature, inner diameter of nozzle, and concentration. As overall results of the application of SAS process to this system, the smaller size powder has been produced as (i) increasing pressure, (ii) decreasing temperature, (iii) decreasing the inner diameter of nozzle, and (iv) decreasing the concentration of PGA and lysozyme. It is found by means of FT-IR analysis that during SAS process, the composition has changed from the original composition of PGA : lysozyme=50 : 50 into PGA : lysozyme=33 : 67 at final product powder. It means that PGA has higher solubility for the mixed solvent of carbon dioxide and dimethyl sulfoxide (DMSO). Due to such difference of solubility, this particle forms the core-shell structure of which the core consists mainly of lysozyme. It is also found that the residual DMSO amount of $7.8\times10^{-3}wt%$ exists inside the powder.

Study of a Supercritical Fluid Process for the Preparation of Hydroxypropyl-β-cyclodextrin Inclusion Complexes (Hydroxypropyl-β-cyclodextrin 포접복합체 제조를 위한 초임계유체 공정 연구)

  • Lee, Sang-Yun;Kim, Jeong-Kyu;Kim, Woo-Sik;Ryu, Jong-Hoon;Lim, Gio-Bin
    • Korean Chemical Engineering Research
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    • v.43 no.1
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    • pp.110-117
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    • 2005
  • In this work, solid-state inclusion complex powders of itraconazole and $2-hydroxypropyl-{\beta}-cyclodextrin(HP-{\beta}-CD)$ were produced by a supercritical anti-solvent (SAS) process. In order to evaluate the degree of complexation, the thermal behavior of the microparticulate complexes was investigated using differential scanning calorimetry. The experimental results obtained for the solubility and dissolution rate of the microparticulate inclusion complexes in a buffer solution of pH 1.2 showed that the complexation of itraconazole with $HP-{\beta}-CD$ results in a significant increase in the solubility and dissolution rate of itraconazole. The particle size of the SAS-produced inclusion complexes was dramatically reduced ($<0.1-0.5{\mu}m$) compared with untreated itraconazole ($30-50{\mu}m$) and $HP-{\beta}-CD$ ($50-100{\mu}m$). The solubility of itraconazole was increased with the increase of pressure at a constant temperature to ca. $758.6{\mu}g/mL$ in an aqueous medium of pH 1.2. The dissolution rate of itraconazole was observed to be significantly improved and about 90% of itraconazole was found to be dissolved within 5-10 min.

Preparation of Dextran Microparticles by Using the SAS Process (초임계 반용매 재결정 공정을 이용한 Dextran 입자의 제조)

  • Kang, Dong-Yuk;Min, Byoung-Jun;Rho, Seon-Gyun;Kang, Choon-Hyoung
    • Korean Chemical Engineering Research
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    • v.46 no.5
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    • pp.958-964
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    • 2008
  • In this work, micro-sized dextran particles, which have recently been focused as one of the candidate materials for the Drug Delivery System(DDS), were prepared by means of the Supercritical Antisolvent (SAS) process with $CO_2$. With dimethyl sulfoxide(DMSO) as the solvent, effects of the operating variables such as temperature (308.15~323.15 K), pressure(90~130 bar), solute concentration(10~20 mg/ml), and the molecular weight of the solute(Mw=37,500, 450,000) on the size and morphology of the resulting particles were thoroughly observed. The higher solute concentration led to the larger particles, however, the injection velocity of the solution and pressure did not show significant effects on the resulting particle size. With dextran of the lower molecular weight, the smallest particles were obtained at 313.15 K. On the other hand, the size of the particles from the high molecular weight dextran ranged between $0.1{\sim}0.5{\mu}m$ with an incremental effect of the temperature and pressure. For the solute concentration of 5 mg/ml, the lower molecular weight dextran did not form discrete particles while aggregation of the particles appeared when the solute concentration exceeded 15 mg/ml for the higher molecular weight dextran. It is believed that if the solute concentration is too low, the degree of the supersaturation in the recrystallization chamber would not be sufficient for initiation of the nucleation and growth mechanism. Instead, the spinodal decomposition mechanism leads to formation of the island-like phase separation which appears similar to aggregation of the discrete particles. This effect would be more pronounced for the smaller molecular weight polymer system due to the narrower phase-splitting region.

Optimization and Bioassay Guided Comparative Techniques for Efficient Extraction of Lutein Esters from Tagetes erecta (Var. Pusa Narangi Genda) Flowers

  • Kawar Lal Dabodhia;Brijesh Tripathi;Narendra Pal Lamba;Manmohan Singh Chauhan;Rohit Bhatia;Vivek Mishra
    • Mass Spectrometry Letters
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    • v.15 no.1
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    • pp.40-48
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    • 2024
  • Capacity of the analytical/quantitative evaluation techniques to satisfy both qualitative and quantitative considerations for effective extraction of marigold oleoresins/xanthophylls and their potential as anti-mycotic and antioxidant activity was assessed. Accelerated solvent extraction (ASE), Soxhlet extraction (SE), Supercritical fluid extraction (SCFE), Cold extraction (CE), and ultrasonically assisted extraction (USE) techniques were evaluated for extraction of oleoresin/xanthophyll content from Tagetes erecta (Var. Pusa Narangi Genda) with respect to solvent consumption, extraction time, reproducibility, and yield. Followed by the antifungal and antioxidant activity evaluation. The overall yield of Tagetes oleoresin was higher in ASE (64.5 g/kg) followed by SE (57.3 g/kg), USE (50.7 g/kg), SCFE (45.3 g/kg) and CE (31.6 g/kg). The lutein esters represented more than 80% of the constituents. Further, xanthophyll/ lutein content in oleoresin was found to be quite higher in HPLC (r2 = 0.996) analysis than in the AOAC recommended UV spectrophotometer analysis. The oleoresin exhibited moderate antioxidant activity (DPPH assay) and antifungal activity against three phytopathogenic fungi. Based on the various parameters, the reproducibility of ASE was better (0.3-8.0%) than that of SE (0.5-12.9%), SCFE (0.2-9.4%), USE (0.3-12.4%) and CE (0.8-15.3%). ASE with (RSD 1.6%) is preferred being faster, reproducible, uses less solvent, robust and automation allows sequential extraction of the sample in less time.

Study of Optimized Extraction Conditions for Simultaneous Anti-inflammatory and Antioxidant Activity of Artemisia iwayomogi using Response Surface Methodology (반응표면분석을 이용한 한인진의 항염 및 항산화 복합 활성 최적 추출 조건에 관한 연구)

  • Park, Dawon;Choi, Woo Seok;Lee, Chang Hyeon
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.45 no.3
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    • pp.319-331
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    • 2019
  • This study was conducted to find a solvent, a extraction method and optimized conditions for Artemisia iwayomogi extract. which is effective to anti-inflammatory and antioxidant activity. A. iwayomogi extract by distilled water, ethanol, methanol, hexane and ethyl acetate using ultrasonic, high-pressure and supercritical extraction was investigated for NO inhibitory and DPPH radical scavenging activity. Extract obtained by ethanol and ultrasonic extraction method showed high NO production inhibitory activity, DPPH free radical scavenging activity and yield. Response surface methodology (RSM) was applied to find a optimized ultrasonic extraction conditions. Results showed that the optimum conditions for the higher yield were ethanol solvent of 45.71% concentration with extraction time and ultrasonic power of 63.33min and 308.84 W, respectively. This condition predicted 15.85% yield, but real yield was $16.40{\pm}0.28%$. The optimum conditions for simultaneous anti-inflammatory and antioxidant activity were established as ethanol concentration (80.81%), extraction time (90.00 min) and ultrasonic power (400.00 W). NO production inhibitory and antioxidant activity were $89.77{\pm}1.37%$ and $60.12{\pm}0.39%$, respectively. These results showed similar to the predicted values of 94.54%, 58.03% respectively.