• Polymer(Korea)
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• v.32 no.3
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• pp.193-198
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• 2008

Sibutramine is a highly crystalline and poorly water soluble drug as the appetite depressant for obesity treatment. In order to increase water solubility of sibutramine, microspheres including sibutramine were prepared by solid dispersion method using a spray dryer. The crystallinity and morphology of the prepared microspheres were confirmed by SEM and XRD. The morphology of micro spheres has gradually changed into spherical shape as increasing evaporation rate of solvent. According to XRD analysis, crystallinity of sibutramine in micro spheres was decreased by below 10%. Release behavior of microspheres was investiaged at pH 1.2, pH 6.8, and solubility of the sibutramine was significantly different depending on pH. The hard capsule showed fast release of sibutramine comparing with the tablet. These results demonstrated that the pharmaceutical preparation is able to control the release behaviors.

• Archives of Pharmacal Research
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• v.28 no.5
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• pp.604-611
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• 2005

Polyethylene glycol (PEG) 6000-based solid dispersions (SDs), by incorporating various pharmaceutical excipients or microemulsion systems, were prepared using a fusion method, t o compare the dissolution rates and bioavailabilities in rats. The amorphous structure of the drug in SDs was also characterized by powder X-ray diffractometry (XRD) and differential scanning calorimetry (DSC). The ketoconazole (KT), as an antifungal agent, was selected as a model drug. The dissolution rate of KT increased when solubilizing excipients were incorporated into the PEG-based SDs. When hydrophilic and lipophilic excipients were combined and incorporated into PEG-based SDs, a remarkable enhancement of the dissolution rate was observed. The PEG-based SDs, incorporating a self microemulsifying drug delivery system (SMEDDS) or microemulsion (ME), were also useful at improving the dissolution rate by forming a microemulsion or dispersible particles within the aqueous medium. However, due to the limited solubilization capacity, these PEG-based SDs showed dissolution rates, below 50% in this study, under sink conditions. The PEG-based SD, with no pharmaceutical excipients incorporated, increased the maximum plasma concentration (C$_{max}$) and area under the plasma concentration curve (AUC$_{0-6h}$) two-fold compared to the drug only. The bioavailability was more pronounced in the cases of solubilizing and microemulsifying PEG-based SDs. The thermograms of the PEG-based SDs showed the characteristic peak of the carrier matrix around 60$^{\circ}C$, without a drug peak, indicating that the drug had changed into an amorphous structure. The diffraction pattern of the pure drug showed the drug to be highly crystalline in nature, as indicated by numerous distinctive peaks. The lack of the numerous distinctive peaks of the drug in the PEG-based SDs demonstrated that a high concentration of the drug molecules was dissolved in the solid-state carrier matrix of the amorphous structure. The utilization of oils, fatty acid and surfactant, or their mixtures, in PEG-based SD could be a useful tool to enhance the dissolution and bioavailability of poorly water-soluble drugs by forming solubilizing and microemulsifying systems when exposed to gastrointestinal fluid.

• Journal of Pharmaceutical Investigation
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• v.28 no.1
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• pp.15-23
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• 1998

Extract of Centella asiatica(ECA), which is poorly water-soluble extract from the Centella asiatica is known to express excellent wound healing properties. $ECA-{\beta}-cyclodextrin$ $(asiaticoside-{\beta}-cyclodextrin\;and\;genin-{\beta}-cyc1odextrin)$ solid dispersion system, which was prepared by freezedrying method, was formulated as gels containing poloxamer 407 and propylene glycol, and evaluated with respect to their viscosity, stability, skin permeation and drug amount in the skin of hairless mouse. The average molar ratio $asiaticoside-{\beta}-CD$ and $genin-{\beta}-CD$ was 1:1.7 and 1:22, respectively. When the molar ratio of genin and ${\beta}-CD$ was 1:5, madecassic acid made 100% solid dispersion system and asiatic acid about 65%. In dissolution study, >99% of asiaticoside from $asiaticoside-{\beta}-CD$ was dissolved in 5 minutes, and >99% madecassic acid and >64% asiatic acid from $genin-{\beta}-CD$. The apparent viscosity of poloxamer 407 gels with $ECA-{\beta}-CD$ solid dispersion system increased in proportion to poloxamer 407 and propylene glycol concentration. In the accelerated stability test, all $ECA-{\beta}-CD$ poloxamer 407 gels showed that asiaticoside was most stable and madecassic acid stable and asiatic acid similar to stability of gel with free ECA. The permeation amount of asiaticoside in poloxamer gels through hairless mouse skin decreased as the concentration of poloxamer 407 increased. When propylene glycol was added at the level of 10%, the permeation amount of asiaticoside at poloxamer gels through hairless mouse skin increased but from 15% it decreased. The permeation of asiaticoside into the skin of hairless mouse was estimated to be about $0.10\;{\mu}g/cm^2$.

• Journal of Conservation Science
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• v.37 no.5
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• pp.411-425
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• 2021

The Stupa of State Preceptor Jigwang from Beopcheonsa Temple Site in Wonju (National Treasure) is a representative stupa of the Goryeo Dynasty, with outstanding Buddhist carvings and splendid patterns, clearly indicating its honoree and year of construction. However, it was destroyed by bombing during the Korean War (1950-1953) and repaired and restored with cement and reinforcing bars in 1957. The surface condition of the original stone shows long-term deterioration due to the m ortar used in past restorations. In order to identify the exact causes of deterioration, the m ortar and surface contaminants on the original stone were analyzed. Portlandite, calcite, ettringite, and gypsum from the mortar were identified, and its ongoing deterioration was observed through pH measurements and the neutralization reaction test. Analysis of surface contaminants identified calcite and gypsum, both poorly water-soluble substances, and their growth in volume among rock-forming minerals was observed by microscopy. Based on those results, semi-quantitative analysis of Ca and S contents significantly influencing the formation of salt crystals was conducted using P-XRF to analyze the basis of surface deterioration, and cross-validation was performed by comparing the body stone affected by the mortar and the upper stylobate stone unaffected by the mortar. Results indicate that the elements are directly involved in the surface deterioration of the body stone.

• Journal of Life Science
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• v.31 no.5
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• pp.502-510
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• 2021

The objective of this study was to develop a novel ticagrelor-loaded self-nanoemulsifying drug delivery system with an enhanced solubility and dissolution rate. Numerous oils and surfactants were screened, then medium chain triglyceride (MCT) oil and the surfactants polyoxyethylene sorbitan monooleate (Tween 80) and Labrafil M1944CS were selected for the preparation of the ticagrelor-loaded self-nanoemulsifying drug delivery system. A pseudo-ternary phase diagram was constructed to detect the nanoemulsion region. Of the various formulations tested, the liquid SNEDDS, composed of MCT (oil), Tween 80 (surfactant), and Labrafil M1944CS (cosurfactant) at a weight ratio of 20/70/10 produced the smallest emulsion droplet size (around 20.56±0.70 nm). Then, particle size, polydispersity, and zeta potential were measured using drugs containing liquid SNEDDS. The selected ticagrelor-loaded liquid SNEDDS was spray-dried to convert it into a ticagrelor-loaded solid SNEDDS with a suitable inert carrier, such as silicon dioxide, calcium silicate, or magnesium aluminometasilicate. The solid SNEDDS was characterized by scanning electron microscopy, transmission electron microscopy, and in vitro dissolution studies. SEM, PXRD, and DSC results suggested that amorphous ticagrelor was present in the solid SNEDDS. Also, the solid SNEDDS significantly increased the dissolution rate of ticagrelor. In particular, the emulsion particle size and the polydispersity index of the solid SNEDDS using silicon dioxide (SS1) as a carrier was the smallest among the evaluated solid SNEDDS, and the flowability and compressibility result of the SS1 was the most suitable for the manufacturing of solid dosage forms. Therefore, solid SNEDDS using silicon dioxide (SS1) could be a potential nano-sized drug delivery system for the poorly water-soluble drug ticagrelor.

• Applied Chemistry for Engineering
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• v.33 no.2
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• pp.179-187
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• 2022

In this study, the synthesis of 1,2-dodecylaminopropanediol (1,2-DDAP) having a 12 carbon chain length and an amine group was designed to improve the preservation and hydrophilicity of 1,2-alkanediol-based compounds. 1,2-DDAP was prepared by reacting dodecylamine (DDA) with 3-monochloro-1,2-propanediol (3-MCPD) in an ethanol solvent at 40 ℃, and its yield and purity were about 56% and 98%, respectively, under a reaction condition of 2 h and a DDA:3-MCPD molar ratio of 1:0.8. The antimicrobial effect of 1,2-DDAP showed the values of the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) against microorganisms at concentrations of 10 to 100 times lower than those of 1,2-octanediol(1,2-ODIOL) or 1,2-decanediol (1,2-DDIOL). Based on the hydrophilic properties of 1,2-DDAP, mixed preservatives were prepared by adding small amounts of 1,2-ODIOL or 1,2-DDIOL, which are poorly soluble in water, with 1,2-DDAP. Mixed preservatives exhibited an effect of inhibiting microorganisms equal to or greater than that of 1,2-DDAP alone in antimicrobial activity tests. As a result of confirming the preservation effect in lotion (cosmetic formulation) for application, 1,2-DDAP showed similar antimicrobial activity at concentrations of 0.3 to 0.6 times lower than that of 1,2-ODIOL or 1,2-DDIOL. Therefore, it is considered that the use of 1,2-DDAP alone and the mixed use with small amounts of 1,2-ODIOL or 1,2-DDIOL can be a good alternative to preservatives in the product.

• The Korean Journal of Pesticide Science
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• v.14 no.1
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• pp.10-15
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• 2010

Most pesticides are poorly soluble in water and must be dissolved in a solvent carrier before being added to the test medium on aquatic toxicity test. The concentration of solvent is critical to the success of a test. This study were conducted to recommend possible organic solvents which have good solubility for pesticides and low toxicity to Korean native water flea to establish new standard toxicity test methods using Korean native water flea for ecological risk assessment of pesticide. Four Korean freshwater cladocerans, Daphnia obtusa, Daphnia sp., Moina macrocopa and Simocephalus vetulus were exposed to 10 different organic solvents during 48 hours to evaluate their toxic response to solvents. Ethyl acetate was the most toxic to cladocerans tested. Although ethyl ether was the least toxic to cladocerans tested, it may not adequate as possible solvent in aquatic toxicity test due to high volatility and low water solubility. In conclusion, acetone, methanol, ethanol and acetonitrile which has low toxicity as well as good water solubility are recommended as optimal organic solvent to use in aquatic toxicity tests with Korean native cladocerans tested.

• Economic and Environmental Geology
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• v.39 no.3 s.178
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• pp.213-227
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• 2006

The geochemical evolution of mine drainage and leachate from waste rock dumps and stream water in Pb-As-rich abandoned Sechang mine area was investigated to elucidate mechanisms of trace metals. Total and sequential extractions were applied to estimate the distribution of trace metals in constituent phases of the waste rocks and to assess the mobility of trace metals according to physicochemical conditions. These discharged waters varied largely in chemical composition both spatially and temporally, and included cases with significant]y low pH (in the range 2.1-3.3), and extremely sulphate (up to 661 mg/l and metal contents (e.g. up to 169 mg/l for Zn, 27 mg/l for As, 3.97 mg/l for Pb, 2.99 mg/l for Cu, and 1.88 mg/l for Cd). Arsenic and heavy metal concentrations at the down-stream of Sechang mine have been decreased nearly to the background level in downstream sites (sites 8 and 16) without any artificial treatments. The oxidation of Fe-sulfides and the subsequent hydrolysis, of Fe(II), with precipitation of poorly crystallized minerals, constituted an efficient mechanism of natural attenuation which reduces considerably the transference of trace metals (i.e. Fe and As) to rivers. The dilution of drainage by mixing with pristine waters provoked an additional decrease of trace metal concentrations and a progressive pH increase. On the other hand, the most soluble cations (i.e. Zn) remained significantly as dissolved solutes until the pH was raised to approximately neutral values. With respect to ecotoxicity, it is likely that the Zn pollution is of particular concern in Sechang mine area. This was confirmed by the sequential extraction experiment, where Zn in wet waste-rock samples occurred predominantly in the exchangeable fraction (65-89% of total), while Pb was the highest in the reducible and carbonate fractions, and Cd, Cu and As in the residual fraction. Pb concentration in the readily available exchangeable fraction (34-48% of total) was dominated for dried waste rock samples. Considering the proportion of metals bound to the exchangeable and carbonate fractions, the comparative mobility of metals probably decreased in the order of Zn>Pb>Cd>As=Cu.