• Proceedings of the Korean Society of Applied Pharmacology
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• 1997.04a
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• pp.116-116
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• 1997

Complex formation of practically insoluble dexamethasone dipropionate (DDP) with ${\beta}$-cyclodextrin (${\beta}$-CD), dimethyl-${\beta}$-cyclodextrin (DMCD), trimethyl-${\beta}$-cyclodextrin (TMCD), 2-hydroxypropyl-${\beta}$-cyclodextrin (HPCD) and sulfobutyl ether ${\beta}$-cyclodextrin (SBCD) in water was investigated by solubility method at various temperatures. Water solubility of DDP was found to be 1.78 $\mu\textrm{g}$/$m\ell$ at 37$^{\circ}C$. Propylene glycol (PG)-water cosolvent increased the solubility of DDP, but the solubilization was not sufficient (8.93 $\mu\textrm{g}$/$m\ell$ in 20% PG). The addition of CD markedly increased the solubility of DDP in water, and A$\sub$L/ type phase solubility diagrams were obtained with ${\beta}$-CD, TMCD, HPCD and SBCD, where the apparent stability constants of the soluble complexes at 25$^{\circ}C$ were determined to be 1388, 216, 1054, and 1992 M$\^$-1/, respectively. However, DMCD remarkably increased the solubility of DDP, and showed an A$\sub$P/ type diagram, suggesting that DMCD forms a soluble complex of high order with DDP. The stability constant for the DDP-DMCD complex at 25$^{\circ}C$ was determined to be 19132 M$\^$-1/. The thermodynamic parameters were calculated for the inclusion complex formation in aqueous solution. CD (1${\times}$10$\^$-2/M) remarkably decreased the partition coefficients of DDP between isopropyl myristate/water in the order of TMCD < ${\beta}$-CD < HPCD < SBCD < DMCD, and in squalane/water system in the order of HPCD < TMCD < ${\beta}$-CD < DMCD < DMCD $\leq$ SBCD. This finding represents that, in a o/w type cream, cyclodextrin complexation with DDP may result in high concentration of DDP in aqueous phase. The permeation of DDP through a cellophane membrane was highly suppressed by the addition of CD, and the degree of suppression was different among CDs, indicating that CD may control the skin permeation of DDP. The dissolution rates of solid dispersions with CDs were much faster than those of drugs alone and corresponding physical mixtures. All DDP-CD solid dispersions exceeded the equilibrium solubility. Consequently these results suggest that complex formation of DDP with CDs may provide useful means to markedly enhance the solubility, and CDs are useful in the semi-solid preparations such as creams and gels for topical application.

• Asian-Australasian Journal of Animal Sciences
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• v.24 no.11
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• pp.1560-1568
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• 2011

This study was conducted to evaluate the yield, nutrient characteristics, ruminal solubility, degradability and disappearance of spent mushroom (Agaricus bisporus) substrates for ruminants. The annual yield of spent Agaricus bisporus substrates was measured to be about 210,000 tons (M/T) in South Korea. The surface soil-removed spent substrates had nutritional characteristics of high crude ash (375 g/kg) and Ca (32 g/kg), medium protein (134 g/kg CP), and high fiber (384 g/kg NDF on a DM basis). Compared with initial mushroom substrates, spent mushroom substrates had twice higher (p<0.0001) CP content and 22.0% lower (p<0.0001) NDF content on an organic matter basis. Compared with raw rice straw, spent rice straw had much higher (p<0.05) predicted ruminal degradabilities and disappearances of DM and CP and a little lower (p<0.05) predicted degradability and disappearance of NDF. In conclusion, the general feed-nutritional value of spent mushroom (Agaricus bisporus) substrates appeared to improve after cultivation of mushrooms.

• Journal of Pharmaceutical Investigation
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• v.31 no.2
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• pp.95-100
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• 2001

Various alkyl ester prodrugs of diclofenac were synthesized in order to investigate the relationship between their skin permeation characteristics and physicochemical properties. Solubility in various vehicles was measured at room temperature. 1-Octanol/water partition coefficients (Log P) and capacity factors (k') were measured to determine the lipophilicity of the prodrugs. Stability of prodrugs in the skin extract and homogenate was also investigated before conducting the skin permeation studies. Increases in the Log P and capacity factor values were observed when alkyl esters of diclofenac were prepared. Since the aqueous solubility of the prodrugs was not high enough, they were saturated in propylene glycol (PG) for skin permeation studies. Prodrugs were rapidly metabolized to diclofenac, both in skin homogenate and in dermal extract of skin. The skin permeation rate of alkyl ester prodrugs was significantly higher than diclofenac with shorter lag time. Moreover, a parabolic relationship was observed between the permeation rate and the log P values of prodrugs, and the maximum flux was achieved at a log P value of around 4.0.

• Korean Journal of Air-Conditioning and Refrigeration Engineering
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• v.10 no.6
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• pp.666-673
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• 1998

Solubilities (LiBr+$CaC1_2$) in water were measured at temperatures form 267.51 to 306.17K for $CaC1_2$ (LiBr+$CaC1_2$)=0.24 by mole. Experimental data were correlated with polynomial equations. Average absolute deviations between the measured and calculated values were 0.31% at concentration smaller than 60wt% and 0.41% at concentration larger than 60wt%, respectively. Vapor pressures were measured at temperatures from 296.75 to 436.75K and concentrations from 40 to 70wt%. Vapor pressure data were fitted to a Antoine-type equation and average absolute deviation was 2.98%. The P-T-X chart and H-T-X chart of $H_2O$/(LiBr+$CaC1_2$) system were constructed by using the correlation equations of solubility, vaper pressure, and heat capacity. The P-T-X chart indicates that $H_2O$/(LiBr+$CaC1_2$) system has potential as a possible working fluid for air-cooled absorption chillers.

• Journal of Sericultural and Entomological Science
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• v.42 no.1
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• pp.48-57
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• 2000

This study was undertaken to figure out the effects of hydrolysis conditions on the solubility of insoluble sericin, molecular weight distribution and thermal characteristics of hydrolysates in enzymatic hydrolysis by Alcalase 2.5L. It was indicated that the optimum treatment temperature and pH for the insoluble sericin were 50$\^{C}$ and 11, respectively. When the insoluble sericin was hydrolyzed with a various treatment conditions, the solubility of all hydrolysates were represented above 85% at given conditions. As the enzyme concentration increased, the solubility increased roughly, but the solubility increasement ratio was less above 2% enzyme concentration. As the treatment time increased, the solubility was also increased. It was showed in the molecular weight distribution of hydrolysates treated various enzyme concentrations and treatment times that when enzyme concentrations were 0.5, 2, 3%, the peaks of the distribution curve were shifted to left side which meant low molecular weight and was distributed much quantity with shifted to be left side, but treatment time was 6 hr. the peak was shifted to right side. When enzyme concentration was 5% and treatment time was below 2 hr., the peaks were shifted to right side, but treatment time was above 4hr. the peak was shifted to left side. The number-average molecular weights were distributed from 300 to 800 and those were decreased when treatment time was up to 4 hr., but increased a little when treatment time was 6hr. It was showed in the DSC curves of hydrolysates treated with treatment time of 0.5, 1, 2, 4, 6 hr. fixed 1% o.w.s enzyme concentration and control that the endothermic peak was observed near at 200$\^{C}$. The denaturation peak of the hydrolysates depending on treatment times had a tendency to shift to higher temperature. But, when the treatment time was 6 hr., the peak was shifted to lower temperature comparing another hydrolysates.

• Journal of Pharmaceutical Investigation
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• v.26 no.3
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• pp.169-174
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• 1996

Inclusion complexes of diclofenac sodium with ${\beta}-cyclodextrin$ were prepared in aqueous solution, alkaline solution and solid phase. The interaction of diclofenac sodium with ${\beta}-cyclodextrin$ in pH 9.0 alkaline solution was evaluated by the solubility method and the instrumental analysis such as thermal analysis, infrared spectroscopy, X-ray diffractometry. The solubility of diclofenac sodium was increased linearly with the increase in the concentration of ${\beta}-cyclodextrin$up to 0.15 mol and showed that the aqueous solubility rate of diclofenac sodium was significantly increased by complex with ${\beta}-cyclodextrin$. The optimum composition of this complex was one molecule of ${\beta}-cyclodextrin$ included 1.59 molecular weight of diclofenac sodium as a guest molecule. The pharmacokinetic parameters of the diclofenac sodium and the complex with ${\beta}-cyclodextrin$ were studied in rats by oral route. $T_{max}$ between drug alone and inclusion complex showed significant difference to be 120 minute and 20 minute respectively. Both of $C_{max}$ and AUC of inclusion complex was about 40% higher than drug alone. It is estimated from the data in this study that complexation of diclofenac sodium with ${\beta}-cyclodextrin$ increased the absorption rate and improved the bioavalability of the diclofenac sodium by the formation of a water-soluble complexes.

• Restorative Dentistry and Endodontics
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• v.16 no.1
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• pp.87-105
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• 1991

The purpose of this experiment was to measure the leaking and solubility of commonly used dental restorative materials - Silux plus (CS), Hi-pol (CH), Clearfil F-II, Fissureseal (FS), Glass-Ionomer cement Fuji Type II (GI), Amalgam Cavex 68 (AM), Zinc Phosphate Cement (ZP) and gutta-percha (GP) and investigate the relation between the solubility and marginal leakage. Disc-shape specimens were fabricated with each material and dipped into deionized water, 0.01M lactic acid and 0.005M KOH solution, thus the total ionic concentrations in each solution was measured with ion chromatograph after 1, 3, and 7 days, respectively. For the solubility test, each specimen was immersed in 0.001M and 0.01M lactic acid for 24 hours, respectively and total weight loss was calculated. Also, Zn leaking through the margin of restorations was measured. The obtained results were as follows: 1. The amounts of eluted ion from the eight materials were most in 0.01M lactic acid and least in deionized water. 2. Of the eight materials, the fluoride release was greatest for glass ionomer cement (GI) in 0.01 M lactic acid after 7 days. 3. In analysis of the divalent cation, Mg was eluted most for zinc phosphate cement (ZP) and Ca for Clearfil F-II (CF) in 0.01M lactic acid after 7 days. 4. In analysis of transition metals, Cu and Zn were detected only. 5. The solubility rate of eight materials was greater in 0.01M lactic acid than in 0.001M for 24 hours, for zinc phosphate cement (ZP) the rate was greatest (5.4%) in 0.001M lactic acid, and amalgam least (0.01%). 6. The Zn concentration of restorative material with Z.P.C base was greater in 0.01M lactic acid than in 0.001M lactic acid.

• Journal of Microbiology and Biotechnology
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• v.32 no.11
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• pp.1471-1478
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• 2022

2'-Fucosyllactose (2'-FL), the most abundant fucosylated oligosaccharide in human milk, has multiple beneficial effects on human health. However, its biosynthesis by metabolically engineered Escherichia coli is often hampered owing to the insolubility and instability of α-1,2-fucosyltransferase (the rate-limiting enzyme). In this study, we aimed to enhance 2'-FL production by increasing the expression of soluble α-1,2-fucosyltransferase from Helicobacter pylori (FucT2). Because structural information regarding FucT2 has not been unveiled, we decided to improve the expression of soluble FucT2 in E. coli via directed evolution using a protein solubility biosensor that links protein solubility to antimicrobial resistance. For such a system to be viable, the activity of kanamycin resistance protein (Kan^R) should be dependent on FucT2 solubility. Kan^R was fused to the C-terminus of mutant libraries of FucT2, which were generated using a combination of error-prone PCR and DNA shuffling. Notably, one round of the directed evolution process, which consisted of mutant library generation and selection based on kanamycin resistance, resulted in a significant increase in the expression level of soluble FucT2. As a result, a batch fermentation with the ΔL M15 pBCGW strain, expressing the FucT2 mutant (F#1-5) isolated from the first round of the directed evolution process, resulted in the production of 0.31 g/l 2'-FL with a yield of 0.22 g 2'-FL/g lactose, showing 1.72- and 1.51-fold increase in the titer and yield, respectively, compared to those of the control strain. The simple and powerful method developed in this study could be applied to enhance the solubility of other unstable enzymes.

• Journal of the Korean Applied Science and Technology
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• v.36 no.4
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• pp.1208-1218
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• 2019

The study is on the cosmetic solubilizing power of organic plant surfactants. The blended high purity polyglyceryl-10 oleate and polyglyceryl-10 stearate mixtures were synthesized using organically certified raw materials to develop surfactants having excellent solubilizing power. The mixture is called "Solubil ORG-1300". The appearance of this material is a pale yellowish paste, with a specific odor. The specific gravity was 1.12 and it was high purity that acid value was 0.072±0.1. The HLB value of this natural surfactant was averaged = 15.1 and calculated through the Griffin equation. Mechanically it is explained how organic surfactant are available with fragrance and oils. The solubilizing test was determined by eye evaluation method through the dissolving performance test for the two oils and measured the transmittance at 890 nm using a UV spectrophotometer to measure the transparency. The results showed that the concentration of surfactant needed to make Bergamot oil available requires approximately more 2 times. It was also found that the concentration of surfactant needed to make the tocoperyl acetate available was about 8 times higher. Experiments on the solubility resulting from pH changes showed stabilized usable solubilizing power even in acidic areas of pH=3.5, neutral areas of pH=7.2, and alkaline areas of pH=1.5. Experiments on the solubility according to pH variation showed good solubility stabilized in acidic areas of pH=3.5, neutral areas of pH=7.2, and alkaline areas of pH=11.5. As an application of cosmetics, the company successfully developed a prescription for moisturizing activity based on these results, it is expected that a wide range of applications will be available for skin care, baby lotion, sensitivity or atopic skin cosmetics.