• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-1
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• pp.44-46
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• 2003

Although Cyclosporin A (CsA) is a powerful immunosuppresant with little adverse effect on the bone marrow, CsA administered orally in the general formulation cannot obtain high bioavailability due to its poor aqueous solubility. To improve the solubility and enhance the bioavailability of poorly water-soluble CsA, many different approaches have been made in our laboratory. (omitted)

• Bulletin of the Korean Chemical Society
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• 제34권7호
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• pp.2011-2015
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• 2013

To improve the water solubility of arylsulfonylimidazolidinone (JSH-2282), a potent anti-cancer agent, two urea derivatives, sodium (S)-2-(3-(4-(5-((S)-2-oxo-4-phenylimidazolidin-1-ylsulfonyl)indoline-1-carbonyl)-phenyl)ureido)succinate (2a) and sodium (S)-2-(3-(4-(5-((S)-2-oxo-4-phenylimidazolidin-1-ylsulfonyl)indoline-1-carbonyl)phenyl)ureido)pentanedioate (2b), were synthesized and studied for solubility and anti-cancer activity.

• Preventive Nutrition and Food Science
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• 제14권3호
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• pp.220-225
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• 2009

In this study, the color value, water solubility, swelling power and sensory evaluation of Dioscorea batatas was examined with the addition of functional additives such as sugar alcohols and organic acids to investigate the browning inhibition and preference of these additives. Treatment with erythritol and citric acid were found to result in the highest hunter L-value, solubility and swelling power relative to the other functional additives. Therefore, erythritol and citric acid were selected as additives for Dioscorea batatas. The Dioscorea batatas containing the mixed additives (erythritol and citric acid) showed higher brightness, water solubility and swelling power than those containing only a single additive. In addition, the color and taste preference determined in the sensory evaluation had higher values when the mixed additives were used.

• Biomolecules & Therapeutics
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• 제8권4호
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• pp.332-337
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• 2000

Physicochemical properties of aspalatone (acetylsalicylic acid maltol ester, AM), which has been recently found to have an antithrombotic effect, were studied in terms of solubility, dissolution, partition coefficient (Pc) and stability. The solubility of AM at 37$^{\circ}C$ was about 1.2 mg/ml and the P$_{c}$ value for n-octanol/water and chloroform/water was 11.4 and 382.6, respectively. Dissolution rates of AM at pH 1.2 and 6.8 were more than 80% within 30 min. The degradation of AM followed apparent first-order kinetics, and was dependent on temperature, pH and ionic strength. From the pH-rate profile, the optimal pH was found to be at around 4.0. Half-lives at pH 1.2 and 6.8 were 33.5 and 44.4 hr, respectively. The degradation rate of AM at pH 1.2 was somewhat faster than that of aspirin, but at pH 7.0, the degradation rate of AM was slower than that of aspirin.n.

• Journal of Pharmaceutical Investigation
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• 제40권6호
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• pp.339-345
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• 2010

Fenofibrate has been used for many years to lower cholesterol levels and its pharmacokinetic profile is well understood. However, due to its low solubility in water, it has low bioavailability after oral administration. In order to improve the dissolution rate, fenofibrate was formulated into a self-microemulsifying drug delivery systems (SMEDDS). We used pseudo-ternary phase diagrams to evaluate the area of microemulsification, and an in vitro dissolution test was used to investigate the dissolution rate of fenofibrate. The optimized formulation for in vitro dissolution assessment consisted of Lauroglycol FCC (60%), Solutol HS 15 (27%), and Transcutol-P (13%). The mean droplet size of the oil phase in the microemulsion formed from the SMEDDS was about 130 nm. The dissolution rate of fenofibrate from SMEDDS was significantly higher than that of the reference tablet. Our studies suggested that the fenofibrate containing SMEDDS composition can effectively increase the solubility and oral bioavailability of poorly water-soluble drugs.

• Journal of Pharmaceutical Investigation
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• 제18권4호
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• pp.203-208
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• 1988

The stability and solubility of piroxicam in propylene glycol (PG), polyethylene glycol (PEC), and PG-water cosolvents have been studied by using high performance liquid chromatography. The degradation rate followed an apparent first-order kinetic and the reaction rate constants at 70, 80, and $90^{circ}C$ were determined. From these rate constants, the activation energy and the rate constant of piroxicam at $25^{circ}C$ in pure PG calculated by Arrhenius equation were 23.34 kcal/mole and $7.0\;{\times}\;10^{-4}\;day^{-1}$, respectively. Both of PG and PEG increased the solubility of the drug, but PEG was more effective.

• KSBB Journal
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• 제23권6호
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• pp.546-550
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• 2008

본 연구에서는 아스타잔틴의 각종 유기용매와 물에 대한 용해도와 산화, 빛, 온도 및 pH에 의한 아스타잔틴의 안정성을 검토하였다. 아스타잔틴은 유기용매인 아세톤과 아세트산에 비교적 용해도가 높았으며 물에는 거의 용해되지 않았다. 아스타잔틴의 용해도에 미치는 pH의 영향을 검토한 결과, 산성 조건 (pH 2)에서는 중성이나 염기성 조건에 비하여 용해도가 10-20배 증가하였다. 아스타잔틴은 산화와 빛에 대한 안정성이 매우 낮았으며, pH 3에서도 안정성이 급격히 떨어지는 것으로 조사되었다. 온도에 대한 영향을 조사한 결과, 상온 보관시에도 아스타잔틴이 쉽게 분해되었으며, 특히 $100^{\circ}C$에서 5초 동안 가열할 경우 아스타잔틴이 90% 이상 분해되었다. 결론적으로 아스타잔틴을 식품이나 화장품 등의 산업적 활용을 위해서는 안정성과 용해도 개선이 요구되는 것으로 판단되었다.

• Journal of Pharmaceutical Investigation
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• 제22권2호
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• pp.105-113
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• 1992

To improve the solubility and dissolution rate of trimethoprim (TMP), which is slightly soluble drug, its inclusion complexes were prepared and studied in this experiment. Inclusion complexes of TMP with ${\beta}-cyclodextrin$ and ${\beta}-cyclodextrin$ polymer (CDPS) were prepared according to Fenyvesi method. These were compared with TMP and its physical mixture with CDPS. Water, diluted hydrochloric acid and phosphate buffer solution were used as dissolution media. And accelerated stability test was studied at $50,\;70\;and \;80^{\circ}C$. It was found that solubility and dissolution rate of inclusion complexes were increased in water. Especially, the solubility and dissolution rate of TMP was found to be markedly increased by inclusion complexation with CDPS. In stability test, ${\beta}-cyclodextrin$ inclusion complexes were more or less stable than TMP alone. This tendency was not led in CDPS. Consequently, CDPS was useful in increasing dissolution rate and stability of TMP.

• 한국환경과학회지
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• 제12권5호
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• pp.551-557
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• 2003

An experimental study of the absorption of CS$_{2}$ in the secondary amine diethanolamine(DEA) was performed in this work. The primary objectives were to investigate an analogy between N2O and CS$_{2}$ permitting estimation of the physical solubility and diffusivity of the sulfur gases in the reacting amino solutions. The solubilities of CS$_{2}$ in water at 25, 40 and 6$0^{\circ}C$ has been measured. The data show fair agreement with previous literature values. The solubility of CS$_{2}$ in 5-25 weight % polyethylene glycol has been measured in order to investigate a possible analogy between CS$_{2}$ and N$_{2}$O The diffusivities of CS$_{2}$ in water and the reaction rate between CS$_{2}$ and DEA has been measured at 25 and 4$0^{\circ}C$, using a wetted sphere apparatus operated at approximately 1/3 atmospheres pressure, which is a previously untried method.

• Korean Chemical Engineering Research
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• 제58권1호
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• pp.92-97
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• 2020

본 연구에서는 제약성분인 니페디핀이 세 종류의 혼합용매에 녹는 용해도를 측정하였다. 또한 용매(아세톤, DMF, 메틸렌클로라이드)에 녹아 있는 니페디핀을 반용매(물, 헥산, 이산화탄소)를 사용하여 결정화하였고, 생성된 결정입자의 외형, 크기, 용융점 등을 측정하였다. 혼합용매로는 아세톤+물, DMF+물, 메틸렌클로라이드+헥산 혼합물이 사용되었으며, 세 혼합용매에서 모두 반용매의 비율이 증가할수록 니페디핀의 용해도가 감소하였다. 아세톤+물의 경우에는 이 혼합물의 밀도 비이상성 현상에 기인한 용해도 최대값을 나타낸 반면, 나머지 두 혼합용매에서는 이 현상이 나타나지 않았다. 반용매 결정화에 의해 생성된 니페디핀 결정의 외형은 용매와 반용매의 종류에 따라 칼날형, 입자형, 프리즘형 등으로 변화하였으며, 입자의 크기는 원재료에 비해 매우 감소하였다. 니페디핀 원재료 입자의 평균크기는 33 ㎛였으며, 결정화된 입자의 평균크기는 11.6~69.8 ㎛의 범위에 있었다. 결정화된 모든 니페디핀 입자는 동일한 열분석 결과를 보여주었으며, 이 결과는 용매와 반용매의 변화에 의해 영향 받지 않았다.