• Journal of Pharmaceutical Investigation
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• v.39 no.6
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• pp.417-422
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• 2009

Budesonide belongs to Class II in the Biopharmaceutics Classification System (BCS) for its high permeability and poor aqueous solubility. The purpose of this study was to improve the solubility and dissolution rate of budesonide using an o/w microemulsion system in order to develop a nasal formulation. Based on the results of the solubility study and pseudo ternary phase diagrams, microemulsions of about 80 nm in mean diameter were formulated using isopropyl myristate and Labrasol$^{(R)}$ as an oil phase and a surfactant, respectively. Solubility of budesonide in the microemulsions increased up to 6.50 mg/mL, which is high enough for a nasal formulation. In vitro release profiles of budesonide significantly increased from the microemulsions compared to that of the budesonide powder. These results suggest that the microemulsions of budesonide could further be developed into a clinically useful nasal formulation.

• Resources Recycling
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• v.24 no.2
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• pp.46-54
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• 2015

In this study, an applicability of thermal pretreatment for primary and secondary sludge, which are generated in a sewage treatment plant, was evaluated. The efficiency and charateristics was investigated with each sludge after pretreatment under the condition of $100{\sim}220^{\circ}C$ for 30 minutes. As the result, it was found that $SCOD_{Cr}$, $NH_4{^+}$, VFAs concentrations increased as the pre-treatment temperature increased. For COD solubilization, it was also highly dependent on an increase of temperature resulting in acceleration on hydrolysis and acid fermentation. In the BMP (Biochemical Methane Potential) experiment, for the primary sludge, it showed the higher biogas production rate at a temperature of $220^{\circ}C$, however, the effect was insignificant (5.6%). Whereas, for the secondary sludge, the increase on biogass production rate was 38.8% ($180^{\circ}C$) and this means that the secondary sludge is more suitable for an applicability of thermal pretreatment.

• Archives of Pharmacal Research
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• v.24 no.6
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• pp.584-589
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• 2001

Isopropryl 2-(1-3-dithiethane-2-ylidene)-2 [N-(4-methyl-thiazole-2-yl) carbamoyl] acetate (YH439) is currently under phase ll clinical trials by the Yuhan Research Center for use as a hepatoprotective agent. Unfortunately, the oral bioavailbility of YH439, which is sparingly soluble in water (i.e., $0.3{\;}\mu\textrm{g}/ml{\;}or{\;}0.91{$\mu}M$ at room temperature), reportedly, is negligibleregardless of the dose administered to rats in the 10-300 mg/kg range. The bioavailability of the compound increased up to 24%, when administered in the form of a micellar solution ($700{\;}\mu\textrm{g}/ml$or 2.1 mM for YH439) at a dose of 10 mg/kg, suggesting that its limited solubility is associated with its negligible bioavailability. In order to obtain additional informmation concerning the bioavailability of YH439, the mechanism(s) involved in gastrointestinal (Gl) absorption were investigated in the present study. For this purpose, the transport of YH430 across a Caco-2 cell monolayer was measured in a $Transwell^{\circledR}$. A permeability of $4.07{\times}10^{-5}{\;}cm/s$ was obtained for the absorptive (i.e., apical to basolateral direction) transport of $0.42{\mu}M$ YH439, implicating that the in vivo Cl absorption is nearly complete. The absorptive transport exhibited a slight concentration-dependency with an intrinsic clearance ($CL_{i}$) of $0.38{\mu}L/{\textrm{cm}^2}/sec$, which accounted for 28.1% of the total intrinsic clearance (i.e., $CL_i$ plus the intrinsic clearance for the linear component) of the transport. Thus, saturation of the absorption process appears to be a minor factor in limiting the bioavailability of the compound. The apparent permeability of YH439 from the basolateral to the apical direction (i.e., efflux, $6.67{\times}10^{-5}{\;}cm/s$) was comparable to that for absorptive transport, but, interestingly, a more distinct concentration-dependency was observed for this transport. However, the efflux does not appear to influence the bioavailability of the compound, as evidenced by the sufficiently high permeability in the absorption direction. Rather, a reportedly extensive first-pass hepatic metabolism appears to be a principal factor in limiting the bioavailability. In this respect, reducing the first-pass metabolism by some means would lead to a higher bioavailability of the compound. Thus, elevation of the absorption rate of YH439 becomes a necessity. From a practical point of view, increasing the concentration of YH439 in the Cl fluid appears to be a feasible way to increase the absorption rate, because the compound is primarily absorbed via a linear mechanism. In summary, the solubilization of YH439, as previously demonstrated for a micellar solution of the compound, appears to be a practical way to increase the oral bioavailability of YH439.

• Applied Chemistry for Engineering
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• v.21 no.3
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• pp.243-251
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• 2010

Nitrogen oxides (NOx) in combustion flue gas are currently mitigated by chemical processes such as catalytic reduction, absorption and adsorption. However, development of environmentally sustainable biological processes is necessary in the near future. In this paper, the up-to-dated R&D trend of biological methodologies regarding NOx removal was reviewed, and their advantages and disadvantages were discussed. The principles and applications of bacterial system including nitrification and denitrification and photosynthetic microalgae system were compared. In order to enhance biological treatment rate and performance, the insoluble nitric oxide (NO) should be first absorbed using a proper solubilization agent, and then microbial degradation or fixation is to be followed. The use of microalgal system has a good prospect because it can fix $CO_2$ and NOx simultaneously and requires no additional carbon for energy source.

• Archives of Pharmacal Research
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• v.8 no.3
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• pp.177-186
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• 1985

Effect of food on the absorption characteristics of oral rifampicin was studied in the fasted rats. Rifampicin dissolved in a new cosolvent was also injected to the rats intravenously, and the pharmacokinetic analysis was performed to explain the effect of food on the gastrointestinal absorption of rifampicin. Rifampicin was absorbed rapidly and completely in the fasting state. Food had a profound effect on the gastrointestinal absorption of rifampicin, i. e., bioavailability and the extent of absorption were decreased to less than one-third of the fasting state in the postprandial state. Food seemed to imhibit the absorption and reabsorption of rifampicin in the gastrointestinal tract, but not the absorption rate constant. Hepatobiliary excretion seemed to be the major route of elimination, since the renal clearance accounted for only 8 % of the systemic clearance. Nevertheless, first-pass effect was negligibly small and most of rifampicin absorbed could reach systemic circulation. Serum concentration change of oral rifampicin on multiple dosing differed markedly in the fasting and postprandial state, which suggested the need of careful adjustment of dosage regimen in both states.

• Polymer(Korea)
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• v.34 no.5
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• pp.459-463
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• 2010

Amphotericin B (AmB) is anti-fungal agent for the treatment of systemic fungal infections, but its poor solubility has limited clinical applications. In this study, a new gel formulation made up of L-arginine as solubilizer, thermosensitive Poloxamer 407 (P 407), and adhesive carbopol was designed for effective solubilization and delivery of AmB. The aqueous solubility of AmB was enhanced up to 2.6 mg/mL by addition of L-arginine. Aqueous P 407 solutions of more than 20% w/v showed thermo-induced sol-gel-sol phase transition. The phase transition behavior was affected by the presence of AmB and L-arginine, and the phase transition range was broadened by addition of carbopol. In vitro drug release was improved by the solubilizing effect of L-arginine, and the presence of mucoadhesive carbopol prolonged the release rate as a function of concentration.

• Korean Journal of Food Science and Technology
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• v.28 no.1
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• pp.169-178
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• 1996

Target parameters such as water solubility index (WSI), intrinsic viscosity (IV), water holding capacity (WHC), oil holding capacity (OHC), soluble dietary fiber (SDF) and microstructure were investigated on three different screw configurations during twin-screw extrusion of wheat bran. WSI of raw wheat bran (RWB) was 13.7%, while that of extrudates ranged $16.3{\sim}23.2%$ when extruded using screw configurations with 5 reverse screw elements (RSE). It was found that the moisture content of RWB greatly affected WSI of extrudates. IV of wheat bran extrudates increased from 10.6 ml/g of RWB to $37.86{\sim}44.37\;ml/g$ of extrudates extruded using 3, 4 and 5 RSE, whose trend was highly related to the moisture content of RWB and the extrusion pressure. Multiplication of IV and soluble solid (SS) content exhibited good correlation $(R^2=0.85)$ with specific mechanical energy (SME). The results suggested that SS and molecular size are an important factor governed by the SME in solubilization of wheat bran. WHC increased with increasing feed rate and moisture content, while OHC decreased. SDF increased from 2.68% of RWB to $4.32{\sim}6.48%$ of extruded wheat bran, indicating the significant breakdown of cell wall components. Microstructure of the extrudates showed the distinct patterns of degradation and solubilization of cell wall structure, depending on the moisture content of RWB.

• BMB Reports
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• v.30 no.5
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• pp.370-377
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• 1997

A novel assay method is described for rapid quantitation of reaction rate of sterol ${\Delta}^7$-reductase (${\Delta}^7$-SR) which catalyzes reduction of the ${\Delta}^7$-double bond of sterols. Of six different organ tissues-liver, small intestine, brain, lung, kidney, and testis-. ${\Delta}^7$-SR activity was detected only in liver (2.30 nmol/min/mg protein) and testis (0.11 nmol/min/mg protein). Using a newly developed method which employs diet-induced enzyme proteins and ergosterol as substrate, we assessed both kinetics ($K_m=210\;{\mu}M$, $V_{max}=1.93\;nmol/min/mg$) and inhibition of the rat hepatic ${\Delta}^7$-SR against well-studied cholesterol lowering agents such as triparanol ($IC_{50}=16\;{\mu}M$). 3-$\beta$-[2-(diethylamino)ethoxy]androst-5-en-17-one (U18666A) ($IC_{50}=5.2\;{\mu}M$), and trans-1.4-bis(2-chlorobenzylaminomethyl)cyclohexane dihydrochloride (AY-9944) ($IC_{50}=0.25\;{\mu}M$). Of the three well-known AY-9944-sensitive cholesterogenic enzymes (i.e., ${\Delta}^7$-SR, sterol ${\Delta}^8$-isomerase, and sterol ${\Delta}^14$-reductase). ${\Delta}^7$-SR was found to be the most sensitive enzyme with a noncompetitive inhibition of this compound ($K_i=0.109\;{\mu}M$). Substrate specificity studies of the microsomal ${\Delta}^7$-SR indicate that the relative reaction rate for 7-dehydrocholesterol and ergosterol are 5.6-fold and 1.6-fold higher than that for lathosterol. ${\Delta}^7$-SR activity was also modulated by feeding rats a diet supplemented with 0.5% ergosterol (>2.6-fold) in addition to 5.0% cholestyramine plus 0.1% lovastatin ($\simeq$5.0-fold). Finally, microsomal ${\Delta}^7$-SR was solubilized by 1.5% 3-[3-(cholamidopropyl)-dimethylammonio]-1-propanesulfonate (CHAPS) and enriched on PEG (0~10%) precipitation, which should be suitable for further purification of the enzyme.

• Journal of Soil and Groundwater Environment
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• v.8 no.2
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• pp.44-54
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• 2003

A kinetic model for evaluating effects of surfactant on the biodegradation of HOC(hazardous organic chemicals) in soil-slurry systems was developed. The model includes the partition of HOC and surfactant, the dissolved-, micellar-, and sorbed-phase biodegradation, the enhanced solubilization of HOC by surfactant addition, and the mass transfer of HOC. Phenanthrene as HOC and Trition X-100, Tergitol NP-10, Igepal CA-720, and Brij 30 were used in the model simulations. The biodegradation rate was increased even with a small micellera-phase bioavailability. The biodegradation was not greatly enhanced due to decreased aqueous HOC concentration by increasing surfactant dose in both cases with and without micellar-phase bioavailability. The effect of sorbed-phase biodegradation on total biodegradation rate was not highly important compared to aqueous- and micellar-phase biodegradation. The model can be applied for surfactant screening and optimal design of surfactant-based soil bioremediation process.

• The Korean Journal of Food And Nutrition
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• v.16 no.4
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• pp.379-387
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• 2003

The freeze dried young antler was extracted by water and proteases. In case of water extraction, the extraction rate was highest when it was reacted in 5% of concentration for 6 hours at 50$^{\circ}C$. The result of HPLC analysis of extract shows that high molecular peak in water extract was transformed into low molecular polk by proteases. The rate of low molecular peak was highest when bacteria protease was used, and its second highest rate was pepsin, but the effect of papain on it was low, The extraction rate of young antler reacted for 5 hours was 33.4%(absorbance 13.25 at 280nm) of bacteria protease, 22.4%(absorbance 10.06) of papain, and 30.2% (absorbance 11.34) of pepsin. The young antler was boiled for 30min and it was reacted by proteases for 5 hours at 50$^{\circ}C$. The extraction rate of it was 47,6%(absorbance 12,54) of bacteria protease, and 26,4%(absorbance 7,48) of papain, and 45.6%(absorbance 7.23) of pepsin, In protein content, water extract was 52,1%, bacteria protease extract was 37.8%, and in amino acid content, water extract was 16.3%, bacteria protease extract was 31.96%, in ash content, water extract was 8.8%, bacteria protease extract was 5.6% by dry base. In mineral content, water extract contains 3.6% of Ca, 8.6% of P, 0.01% of Mg, 1.4 % of Na, 0.02 % of F, and bacteria protease extract contains 2.5% of Ca, 11.8% of P, 0.046 % of Mg, 2.1 % of Na, 0.018 % of F by dry base.