• Archives of Pharmacal Research
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• 제26권7호
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• pp.526-531
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• 2003

KR-31378 is a new drug candidate intended for the use in the prevention of ischemia-reperfusion damage. The objective of this preformulation study was to determine the physicochemical properties of KR-31378. The n-octanol to water partition coefficients of KR-31378 were 0.0504 at pH 3 and 0.8874 at pH 10. Accelerated stability of KR-31378 in solution and solid state was studied at 5, 40, $60^{\circ}C$. The stability testing indicated that the t90 for the drug in solid was estimated to be 2 years and 128.6 days at $25^{\circ}C$, while the that in aquesou solution was 68.6 days at $25^{\circ}C$. The KR-31378 was also found to be unstable under the relative humidity of 76%, probably because of the hygroscopic nature of the drug. In order to study compatibility of KR-31378 with typical excipients, potential change in differential scanning calorimetry spectrum was studied in 1:1 binary mixtures of KR-31378 and Aerosil, Avicel, Eudragit, lactose, PEG, talc, CMC, PVP, starch. As a result, CMC, PVP, and starch were found to be incompatible with KR-31378, indicating the addition of these excipients may complicate the manufacturing of the formulation for the drug. Particle size distribution of KR-31378 powder was in the size range of 9-93 $\mu$ m with the mean particle size of 37.9 $\mu$ m. The flowability of KR-31378 was apparently inadequate, indicating the granulation may be necessary for the processing of the drug to solid dosage forms. Crystallization of the drug with a number of organic solvents did not lead a crystalline polymorphism. In addition, dissolution of the drug from the powder was adequately rapid at $37^{\circ}C$ in water.

• 한국축산식품학회지
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• 제37권2호
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• pp.181-190
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• 2017

The aim of this study was to compare the quality and physicochemical characteristics of blue-shelled eggs (BE) and conventional eggs (CE). Proximate composition, quality, pH value, shell color, collagen content, fatty acid composition, total cholesterol, ${\alpha}$-glucosidase inhibition activity, and antioxidation activity were determined. The proximate composition, general qualities, and pH values of CE and BE showed no significant differences, except in moisture composition, weight, and shell thickness. Moisture content and weight of BE were significantly lower than those of CE. However, shell thickness and weight of BE were higher than those of CE (p<0.05). Lightness of BE was significantly higher than that of CE (85.20 vs. 58.80), while redness ($a^*$) and yellowness ($b^*$) of BE were lower than those of CE ($a^*$: -4.75 vs. 14.20; $b*$: 10.45 vs. 30.63). The fatty acid [C18:1n7 (cis-vaccenic acid) and C18:3n6 (gamma-linolenic acid)] contents of BE were significantly higher than those of CE. The total cholesterol contents of BE and CE were similar. DPPH radical scavenging activity of BE was significantly higher than that of CE (40.78 vs. 35.35). Interestingly, ${\alpha}$-glucosidase inhibition activity of whole egg and egg yolk in BE (19.27 and 36.06) was significantly higher than that of whole egg and egg yolk in CE (13.95 and 32.46). This result indicated that BE could potentially be used as a functional food material. Further studies are required to evaluate the specific compounds that affect functional activity.

• Journal of Pharmaceutical Investigation
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• 제35권4호
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• pp.279-285
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• 2005

Ground CS-891 (N-[1-(4-methoxyphenyl)-1-methylethyl]-3-oxo-4-aza-5a-androst-1-ene-$17{\beta}$-carboxamide) of poorly water soluble drug was obtained using a Heiko Seisakusho model TI-100 vibration mill, and samples with different crystallinity were prepared at mixture ratios of 10:0, 7:3, 5:5, 3:7 and 0:10 (intact;ground CS-891). Physicochemical characterizations were obtained using qualitative and quantitative X-ray diffractometry, different scanning calorimetry (DSC), scanning electron microscopy (SEM), Quantasorb surface area analyzer, and controlled atmosphere microbalance. With increase of amorphous CS-891 in mixture ratios, the intensities of X-ray diffraction peaks of crystalline CS-891 were decreased, whereas surface area, water absorption, and exothermic peaks in DSC were increased. The apparent solubility of ground CS-891 was $4.4\;{\mu}g/ml$ and the solubility of intact CS-891 was $3.1\;{\mu}g/ml$ at $37{\pm}1^{\circ}C$. The apparent precipitation rates of CS-891 in a supersaturated solution during the solubility test were increased with an increase of amorphous CS-891, and a crystalline form of CS-891 transformed from amorphous CS-891 after the solubility test was found by X-ray diffraction analysis, DSC and SEM. The dissolution profiles of CS-891 with different crystallinity at $37{\pm}1^{\circ}C$ by the USP paddle method were investigated, and the apparent dissolution rate constant of ground CS-891 was about 5.9-fold higher than that of intact CS-891. A linear relationships between the crystallinity of CS-891 and the apparent dissolution rate constant (r>0.96) were obtained.

• Biotechnology and Bioprocess Engineering:BBE
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• 제11권3호
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• pp.262-267
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• 2006

The objective of this study was to develop new self-organized nanogels as a means of drug delivery in patients with cancer. Pullulan (PUL) and deoxycholic acid (DOCA) were conjugated through an ester linkage between the hydroxyl group in PUL and the carboxyl group in DOCA. Three types of PUL/DOCA conjugates were obtained, differing in the number of DOCA substitutions (DS; 5, 8, or 11) per 100 PUL anhydroglucose units. The physicochemical properties of the resulting nanogels were characterized by dynamic light scattering, transmission electron microscopy, and fluorescence spectroscopy. The mean diameter of DS 11 was the smallest (approx. 100 nm), and the size distribution was unimodal. To determine the organizing behavior of these conjugates, we calculated their critical aggregation concentrations (CACs) in a 0.01-M phosphate buffered saline solution. They were $10.5{\times}10^{-4}mg/mL,\;7.2{\times}10^{-4} mg/mL,\;and\;5.6{\times}10^{-4} mg/mL$ for DS 5, 8, and 11, respectively. This indicates that DOCA can serve as a hydrophobic moiety to create self-organized nanogels. To monitor the drug-releasing behavior of these nanogels, we loaded doxorubicin (DOX) onto the conjugates. The DOX-loading efficiency increased with the degree of DOCA substitution. The release rates of DOX from PUL/DOCA nanogels varied inversely with the DS. We concluded that the PUL/DOCA nanogel has some potential for use as an anticancer drug carrier because of its low CAC and satisfactory drug-loading capacity.

• Journal of Ginseng Research
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• 제34권2호
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• pp.113-121
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• 2010

The fresh ginseng roots were extracted with aqueous methanol, and the obtained extracts were partitioned using ethyl acetate, n-butanol, and water, successively. The repeated silica gel and octadecyl silica gel column chromatogaraphy for n-butanol fraction afforded four diol ginseng saponins, ginsenosides $Rb_1$, $Rb_2$, $R_c$, and Rd. The physicochemical, spectroscopic, and chromatographic characteristics of these ginsenosides were measured and compared with those reported in the literature. Some of the peak assignments in previously published $^1H$- and $^{13}C$-nuclear magnetic resonance (NMR) spectra were inaccurate. This study employed two-dimensional NMR experiments, including $^1H-^1H$ correlation spectroscopy, heteronuclear single quantum correlation, and heteronuclear multiple bond connectivity, to determine exact peak assignments.

• Archives of Pharmacal Research
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• 제26권2호
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• pp.162-167
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• 2003

Liquid suppository systems composed of poloxamers and bioadhesive polymers were easy to administer to the anus and mucoadhesive to the rectal tissues without leakage after the dose. However, a liquid suppository containing diclofenac sodium could not be developed using bioadhesive polymers. since the drug was precipitated in this preparation. To develop a liquid suppository system using sodium chloride instead of bioadhesive polymers, the physicochemical properties such as gelation temperature, gel strength and bioadhesive force of various formulations composed of diclofenac sodium, poloxamers and sodium chloride were investigated. Furthermore, the pharmacokinetic study of diclofenac sodium delivered by the liquid suppository was performed. Diclofenac sodium significantly increased the gelation temperature and weakened the gel strength and bioadhesive force, while sodium chloride did the opposite. The liquid suppositories with less than 1.0％ of sodium chloride, in which the drug was not precipitated, were inserted into the rectum without difficulty and leakage. Furthermore, liquid suppository gave significantly higher initial plasma concentrations and faster Tmax of diclofenac sodium than did solid suppository, indicating that drug from liquid suppository could be absorbed faster than that from solid one in rats. Our results suggested that a thermosensitive liquid suppository system with sodium chloride and poloxamers was a more physically stable, convenient and effective rectal dosage form for diclofenac sodium.

• 미생물학회지
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• 제31권1호
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• pp.9-16
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• 1993

녹황색 세균인 Chlorobium limicola f. thiosulfatophilum NCIB 8327 로부터 광수확기구인 chlorosome 을 초원심분리법으로 분리하여 그들의 물리화학적 특성을 조사하였다. Chlorosome 은 Percoll self gradient 에서 초원심분리하였을 때 약 1.05 g/$cm^{3}$ 의 밀도인 것으로 측정되었다. UV-visible absorption spectra 에 의한 분석결과. chlorosome 은 세균엽록소 (bacteriochlorophyll)d, chlorobactene 및 약간의 세균엽록소 a 로 구성되었음을 확인하였다. 분리된 chlorosome 은 산성조건에서보다 염기성 조건(pH>7) 에서 더 안정하고, 0.deg. C 에서 $80^{\circ}C$ 까지 온도에서는 안정하나 그이상의 온도에서는 급격하게 파괴되었으며, 빛에 의해서도 쉽게 파괴되는 것을 확인하였다. 이러한 결과를 두고 볼 때, chlorosome 에서는 색소를 안정화시켜주는 단백질이나 지질이 존재할 석으로 생각된다.

• Journal of Microbiology and Biotechnology
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• 제16권9호
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• pp.1369-1376
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• 2006

Self-organized nanogels were prepared from pullulan/biotin conjugates (PU/Bio) for the development of an effective anticancer drug delivery system. The degree of biotin substitution was 11, 19, and 24 biotin groups per 100 anhydroglucose units of pullulan. The physicochemical properties of the nanogels (PU/Bio1, 2 and 3) in aqueous media were characterized by dynamic light scattering, transmission electron microscopy, and fluorescence spectroscopy. The mean diameter of all the samples was less than 300 nm with a unimodal size distribution. The critical aggregation concentrations (CACs) of the nanoparticles in distilled water were $2.8{\times}10^{-2},\;1.6{\times}10^{-2}$, and $0.7{\times}10^{-2}mg/ml$ for the PU/Bio1, 2, and 3, respectively. The aggregation behavior of the nanogels indicated that biotin can perform as a hydrophobic moiety. To observe the specific interaction with a hepatic carcinoma cell line (HepG2), the conjugates were labeled with rhodamine B isothiocyanate (RITC) and their intensities measured using a fluorescence microplate reader. The HepG2 cells treated with the fluorescence-labeled PU/Bio nanoparticles were strongly luminated compared with the control (pullulan). Confocal laser microscopy also confirmed internalization of the PU/Bio nanogels into the cancer cells. Such results demonstrated that the biotin in the conjugate acted as both a hydrophobic moiety for self-assembly and a tumor-targeting moiety for specific interaction with tumor cells. Consequently, PU/Bio nanogels would appear to be a useful drug carrier for the treatment of liver cancer.

• 융합정보논문지
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• 제10권2호
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• pp.102-108
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• 2020

지속적으로 감소하는 쌀 소비량을 해결하기 위해 쌀을 주원료로 하며 식사대용식은 물론 스낵으로도 제공될 수 있는 누룽지 제품의 다양성을 확보하고자 기능성을 보유한 7종의 천연 소재를 첨가하여 기호도와 상품성을 증가시킬 수 있는 누룽지를 제조하고 이화학적 특성을 분석하였다. 물 결합력은 흑임자를 첨가한 누룽지에서 264.13%로 가장 높게 나타났으며 경도는 갈색거저리를 첨가한 누룽지에서 0.36 N으로 가장 낮은 값을 보였다. 환원당 함량은 단호박을 첨가한 누룽지를 30분 침지하였을 때 1.47%로 가장 높게 나타났다. 다양한 소재를 첨가한 누룽지의 2,2-diphenyl-1-picryl-hydrazyl 유리라디칼 소거활성을 측정한 결과 단호박과 비트 첨가 누룽지에서 높은 소거능을 보였다. 관능평가 결과 전체적 기호도는 흑임자 첨가 누룽지에서 4.3으로 가장 높게 나타났다. 여러 소재가 첨가된 누룽지의 이화학적 특성 분석과 관능평가 결과 다양한 식품으로서의 적용이 가능한 것을 확인하였다.

• 동아시아식생활학회지
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• 제24권3호
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• pp.400-406
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• 2014

본 연구에서는 아피오스로부터 전분을 추출하여 epichlorohydrin으로 가교결합을 시킨 후 가교결합 아피오스 전분의 이화학적 특성을 분석하였다. 가교결합 아피오스 전분은 치환도가 증가함에 따라 몰가교화도가 0.1225에서 3.5124로 비례적으로 증가하였으며, FT-IR을 측정한 결과, CLAP-2%는 에테르 결합으로 인하여 $1,646cm^{-1}$과 $2,930cm^{-1}$에서 피크의 강도가 강해져 가교결합 반응이 이루어졌음을 확인할 수 있었다. 천연 아피오스 전분의 X-선 회절도는 $2{\theta}$=15.1, 17.1, 17.9, $23.2^{\circ}$에서 피크가 나타나는 전형적인 A형 전분 형태를 나타내었으며, 가교결합 아피오스 전분은 가교화에 의해 회절도와 상대결정화도에 큰 변화를 보이지 않아 무결정 영역에서 가교결합 반응이 일어난 것으로 추정되었다. 아피오스 전분 입자를 SEM으로 관찰한 결과, 전분 입자는 구형 또는 타원형 모양을 나타내었으며, 가교결합 아피오스 전분은 천연 아피오스 전분과 비교하였을 때 전체적인 형태에는 변화가 없는 것이 관찰되었다. 색도는 가교결합이 진행되면서 명도와 청색도가 변화하였으며, 청가는 천연 아피오스 전분과 가교결합 아피오스 전분 사이에 유의적인 차이가 나타나지 않았다.