• 방사성폐기물학회지
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• 제10권3호
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• pp.161-170
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• 2012

국내 심부지질환경조건을 반영한 처분안전성 평가에 필요한 입력자료를 제공하기위해, 그 동안 국내 지하시험시설(KURT)환경조건에서 많은 실험을 수행해 왔다. 안전성평가코드에 사용되는 많은 입력변수들 중 중요성이 부각되는 입력변수들을 선정하여, 각 변수별로 수집한 자료를 통계처리를 하여 값 분포 특성을 기술하고, 외국자료 값과 비교평가를 통해 값의 타당성을 검토하였다. 다룬 입력변수로서 용기물성분야에서 용기수명, 초기파손률을, 완충재물성분야에서는 핵종용해도, 완충재의 공극률, 밀도, 확산계수, 핵종분배계수를, 암반 및 원계영역에서는 수리전도도, 지하수유속, 핵종분배계수, 확산깊이, 암반균열폭, 주지하수유동통로까지 거리, 핵종이동오염운의 너비 등이다.

• Journal of Pharmaceutical Investigation
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• 제39권2호
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• pp.97-106
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• 2009

Although lovastatin (LS) is widely used in the treatment of hypercholesterolemia, its bioavailability is known to be around 5%. This study was aimed to increase the solubility and dissolution-permeation rates of LS using solid dispersions (SDs) with bile salts. The solubilities of LS in water, aqueous bile salt solutions and non-aqueous vehicles were determined, and effects of bile salts on the cellulose or duodenal permeation of LS from SDs were evaluated using a horizontal permeation system. SDs were prepared at various ratios of LS to carriers, such as sodium deoxycholate (SDC), sodium glycocholate (SGC) and/or 2-hydroxypropyl-$\beta$-cyclodextrin (HPCD). The addition of bile salts (25 mM) in water increased markedly the solubility of LS by the micellar solubilization. Some non-aqueous vehicles were effective in solubilizing LS. From differential scanning calorimetric studies, it was found that the crystallinity of LS in SDs disappeared, indicating a formation of amorphous state. The SDs showed markedly enhanced dissolution compared with those of their physical mixtures (PMs) and drug alone. In the dissolution-permeation studies using a cellulose membrane, the donor and receptor solutions were maintained as a sink condition using pH 7.0 phosphate buffer containing 0.05% sodium lauryl sulfate (SLS). The flux of LS alone was nearly same as that of LS-SDC-HPCD (1:3:6) PM. However, the flux of LS-SDC-HPCD (1:3:6) SD slightly increased compared with drug alone and PM, suggesting that entrapment of LS in micelles does not significantly hinder the permeation across cellulose membrane. In the dissolution-duodenal permeation studies using a LS-HPCD-SDC (1:3:6) SD, the addition of various bile salts in donor solutions (25 mM) enhanced the permeation of LS markedly, and the fluxes were found to be $0.69{\pm}0.41$, $0.87{\pm}0.51$, $0.84{\pm}0.46$, $0.47{\pm}0.17$ and $0.68{\pm}0.32{\mu}g/cm^2/hr$ for sodium cholate (SC), SDC, SGC, sodium taurodeoxycholate (STDC) and sodium taurocholate (STC), respectively. The stepwise increase of donor SGC concentration increased the flux dose-dependently. From the relationship of donor SGC concentration and flux, the concentration of SGC initiating the permeation across the duodenal mucosa was calculated to be 11.1 mM, which is nearly same as the critical micelle concentration (CMC, 11.6 mM) of SGC. However, with no addition of bile salts and below CMC, the permeation was very limited and irratic, indicating that LS itself is very poor permeable. Higher protions of bile salt in SD such as LS-SDC or LS-SGC (1 : 49 and 1 : 69) showed highly promoted fluxes. In conclusion, SD systems with bile salts, which may form their micelles in intestinal fluids, might be a promising means for providing enhanced dissolution and intestinal permeation of practically insoluble and non-absorbable LS.

• Journal of Pharmaceutical Investigation
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• 제38권2호
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• pp.111-117
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• 2008

To overcome the solubility of poorly water-soluble drug, the formation of solid dispersion using a spray-dryer with polymeric material, that can potentially enhance the dissolution rate extend of drug absorption was considered in this study. $Eudragit^{(R)}$ E100 as carrier for solid dispersion is acrylate copolymer that soluble in acidic buffer solutions (below pH 5.0). It was used to increase dissolution of atorvastatin calcium as a water-insoluble drug in acidic environments. In this study, a spray-dryer was used to prepare solid dispersion of atorvastatin calcium and $Eudragit^{(R)}$ E100 for purpose of improving the solubility of drug. Atorvastatin calcium and $Eudragit^{(R)}$ E100 were dissolved in ethanol and spray-dryed. DSC and XRD were used to analyze the crystallinity of the sample. It was found that atorvastatin calcium is amorphous in the $Eudragit^{(R)}$ E100 solid dispersion. FT-IR was used to analyze the salt formation by interaction between atorvastatin calcium and $Eudragit^{(R)}$ E100. Comparative dissolution study exhibited better dissolution characteristics than the commercial drug ($Lipitor^{(R)}$) as control. The dissolution rate of atorvastatin calcium was markedly increased in solid dispersion system in simulated gastric juice (pH 1.2). This study proposed that this solid dispersion system improved the bioavailability of poorly water-soluble atorvastatin calcium.

• 한국식품과학회지
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• 제10권4호
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• pp.415-422
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• 1978

한국산 두류중 대두를 제외한 팥, 녹두, 강남콩에 대한 일반성분의 분석, 용해도에 의한 단백질의 분별(分別) 정량(定量) 및 polyacrylamide gel disc electrophoresis를 수행한 결과는 다음과 같다. 1) 일반성분으로는 지방이 적어 1%미만이었고 탄수화물은 60% 내외로 많았으며 단백질은 $20{\sim}25%$ 이었다. 2) 단백질중 총 globulin 함량은 $46{\sim}59%$로 대두에 비해 적었고 녹두>강남콩>팥의 순이었다. Albumin은 대두와 비교할 때 강남콩만 비슷하였고 팥, 녹두는 떨어졌으며 대신 glutelin의 함량이 많아 $10{\sim}19%$의 범위에서 팥>녹두>강남콩의 순이었다. 3) 전기영동(電氣泳動) 결과 전(全)단백질을 pH 7.6 완충액으로 추출한 것은 팥, 녹두, 강남콩에서 각각 9, 12, 11개의 band를 보였으나 pH 4.8 완충액으로 추출한 것은 분리가 더 되 어 각각 13, 13, 12개의 band를 보였다. Water extract의 경우는 팥, 녹두, 강남콩에서 각각 10, 8, 9개의 band를 보였으며 이 중 albumin획분(劃分)은 각각 8, 9, 7개, globulin 획분(劃分)은 모두 4개의 band를 보였다. 세가지 두류의 globulin 획분(劃分)중 Rm 치 $0.05{\sim}0.07$사이의 band는 모두 water extract에서 나타나지 않았던 것으로 물에 녹지 않는 globulin 고유의 band인 것으로 생각된다.

• 한국결정성장학회지
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• 제20권2호
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• pp.93-100
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• 2010

X-선 회절 분석방법을 통해 biphasic calcium phosphate(BCP) 분말의 Ca/P 몰 비율을 확인하고 특성을 평가하였다. 다양한 화학 양론적인 Ca/P 몰 비율을 가지는 BCP 분말은 공침반응 및 하소과정을 통해 합성하였다. 1.5에서 1.67의 Ca/P 몰 비율을 가지는 분말의 조성은 초기 출발물질의 Ca/P 몰 비율, pH 10에서의 공침 과정 및$900^{\circ}C$ 열처리에 의해 정해졌다. 화학 양론적 Ca/P 몰 비율을 가지는 BCP 분말의 구조, 형상 및 화학적 특성평가는 XRD의 상-정량 확인 분석을 바탕으로 주사전자현미경 및 유도 결합 플라즈마 분광분석기와 함께 수행 하였다. BCP 분말의 용해도는 $36.5^{\circ}C$ 및 pH 7.4 의 phosphate buffer solution(PBS)에서 특성평가 하였다.

• 한국수산과학회지
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• 제56권1호
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• pp.7-20
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• 2023

Boil-dried concentrate (BDC) and steam-dried concentrate (SDC) were prepared from olive flounder Paralichthys olivaceus roe using the cook-dried process, and their food functionality and in vitro bioactivity were examined. The buffer capacity of BDC and SDC was found to be stronger in the alkaline region than in the acidic region, and the buffer capacity of SDC was superior to that of BDC. The water holding capacities of these concentrates were 7.6 and 7.4 g/g protein, respectively, both of which were significantly lower than that of freeze-dried concentrate (FDC). The solubility of BDC (13.4%) and SDC (12.7%), foaming capacity of BDC (107.7%) and SDC (110.6%), and oil-in-water emulsifying activity index of BDC (7.7 m²/g) and SDC (9.7 m²/g) were all significantly lower than the corresponding values for FDC (P<0.05). The lower food functionality of BDC and SDC compared with FDC can be attributed to the high-temperature denaturation of proteins during the cook-dried process. The 2,2'-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid radical scavenging activities (IC₅₀) of SDC (2.5 mg protein/mL) was 60.4 ㎍/mL, and the angiotensin I converting enzyme inhibitory activity was 80.9%. Olive flounder roe concentrates have good antioxidant and antihypertensive activities, and can be used as materials or ingredients in the processing of seafood and other foods to enhance protein contents and food functionality.

• 한국수소및신에너지학회논문집
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• 제21권6호
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• pp.580-586
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• 2010

Acid and alkali pretreatments were applied to tofu processing waste (TPW) to increase the solubility of ingredients in TPW. Pretreatment at 1.0% of HCl and 2.5% of NaOH condition resulted in the increase of SCOD concentration from 3.2 g COD/L to 27 g COD/L and 33 g COD/L, respectively. The acid and alkali-pretreated TPW was studied for its fermentative $H_2$ production capacity in batch mode using a thermophillic mixed culture. Alkali pretreatment on presence of 2.5% NaOH exhibited more soluble portion released compared to acid pretreatment using HCl, however the $H_2$ production from acid pretreated TPW was better than alkali-pretreated TPW probably due to the sodium inhibition on microbial activity. In addition, sewage sludge was externally added to the acid-pretreated (1.0% HCl) TPW by 20% (on volume basis). Average H2 production rate was increased from 31 to 78 ml/L-broth/hr, and it was attributed to the high buffer capacity and abundant nutrients especially divalent cation in sewage sludge.

• Journal of Pharmaceutical Investigation
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• 제32권4호
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• pp.313-319
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• 2002

Rat skin permeation of various nonsteroidal antiinflammatory drugs (NSAIDs) was investigated in vitro using Franz diffusion cell at $37^{\circ}C$. The effect of various skin permeation enhancers was also observed as a preliminary study of developing transdermal delivery systems of NSAIDs. Lipophilicity of NSAIDs was determined from thε partition coefficient (log P) in 1-octanol/water and 1-octanol/IPB mutual-saturated solutions. The solubility was determined in water, isotonic phosphate buffer (IPB), and propylene glycol (PG) at $37^{\circ}C$. The rat skin permeation rate of acetaminophen, piroxicam, and aceclofenac was almost negligible, although they were saturated in PG. Addition of 1 % permeation enhancer increased the permeation rate of ketoprofen, ketorolac, and diclofenac. However, the skin permeation rate of ibuprofen did not increase with the addition of various enhancers. Among the permeation enhancers testεd, oleic acid was the most effective for various NSAIDs. Based on the daily dose, lipophilicity, and the skin permeation ratε achieved in this study, ketoprofen and ketorolac seem to be the most promising drug candidates for transdermal delivery systems, especially when formulated with unsaturated fatty acids, such as oleic acid.

• Toxicological Research
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• 제11권2호
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• pp.295-302
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• 1995

Menadione-ghitathione conjugate (MEN-SG), a metabolite of menadione, is known to be a redoxcycler in rat hepatocyte subcellular fraction. Therefore, it was assumed that MEN-SG could exert cytotoxlclty to ral platelets, another target tissue of menadione. We first synthesized MEN-SG, the identity of which was verified by mass, $^1{H}$-NMR and UV-visible spectra. In addition, the stability of MEN-SG was investigated in biological assay system. MEN-SG was degraded in a time-dependent manner in DMSO which had been used as a vehicle and thus, tris-HCl buffer was used as a vehicle of MEN-SG despite the low solubility in it. Perchloric acid as well as platelets itself did not affect the stability of MEN-SG. Our next attempt was the evaluation of cytotoxicity of MEN-SG in rat platelets. MEN-SG did not induce cytotoxicity to rat platelets measured by two different methods, LDH release and turbidity changes. The extents of oxygen consumption by MEN-SG in intact platelets were significantly lower than those by menadione, though it had been observed that oxygen consumptions by menadione and MENSG were similar in subcellular fractioas of platelets. These results suggest that MEN-SG is not toxic to rat platelets despite its redox cycling capacity and glutathione conjugation reaction of menadione could be regarded as a detoxification process.

• Archives of Pharmacal Research
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• 제26권4호
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• pp.258-263
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• 2003

Colon-specific delivery of glucocorticoids is highly desirable for the efficient treatment of inflammatory bowel disease. We synthesized prednisolone 21-sulfate sodium (PDS) as a colon-specific prodrug of prednisolone (PD) and investigated its properties using rats as test animals. We expected that introduction of sulfate ester as a sodium salt might increase the hydrophilicity and restrict the absorption in the GI tract. If PDS is stable and nonabsorbable in the upper intestine, it will be delivered to the colon as an intact form, where it hydrolyze by the sulfatase to release PD. Compared with PD, the solubility of PDS increased and the apparent partition coefficient decreased greatly. PDS was stable on incubation with pH 1.2 and 6.8 buffer solutions and with the contents of the stomach and small intestine. On incubation with the cecal contents, PDS decreased to 9.6％ of the dose in 10 h producing PD. The amount of PD increased to give a maximum 54％ of the dose and decreased. As a control, when PD was incubated with the cecal contents, it decreased to 29％ of the dose in 8 h, which implied that reduction of PD proceeded under such conditions. These results suggested that hydrolysis of PDS took place to produce and accumulate PD, which decreased by reduction as the incubation period extended. Our results suggested that PDS can be a promising colon-specific prodrug of PD, and sulfate ester group might serve as a potential colon-specific promoiety, especially for the drugs which are resistant to reduction in the colon.