• 제목/요약/키워드: Solubilization rate

검색결과 105건 처리시간 0.018초

Effect of Solubilizing and Microemulsifying Excipients in Polyethylene Glycol 6000 Solid Dispersion on Enhanced Dissolution and Bioavailability of Ketoconazole

  • Heo, Min-Young;Piao, Zong-Zhu;Kim, Tae-Wan;Cao, Qing-Ri;Kim, Ae-Ra;Lee, Beom-Jin
    • Archives of Pharmacal Research
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    • 제28권5호
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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.

음식물쓰레기 세정산발효공정에서 세정율의 영향 (Effects of Elutriating Rates for Elutriated Acid Fermentation of Food Waste)

  • 권구호;이상협;민경석
    • 한국물환경학회지
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    • 제24권2호
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    • pp.201-205
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    • 2008
  • The korean government started to ban the sanitary landfill of food wastes as of 2005. The radical change of policy is primarily due to the limited landfill site, but aimed to promote not only to reduce the food waste production but also to enhance the reuse and recycle. The performance of elutriated acid fermentation to evaluate the effects of elutriating ratios was investigated. The fermenters were operated with elutriating water to food waste volumetric ratio of 2, 1, 0.5 and 0.25. Initial pH of elutriating water was set for 9 based on the pH effects study. The cumulative amounts of SCOD production rate were $0.34gSCOD/gVS_i$, $0.45gSCOD/gVS_i$, $0.26gSCOD/gVS_i$ and $0.28gSCOD/gVS_i$ with the ratios of 2, 1, 0.5 and 0.25, respectively. The cumulative productions of VFAs were 0.12 gVFAs as $COD/gVS_i$, 0.28 gVFAs as $COD/gVS_i$, 0.21 gVFAs as $COD/gVS_i$ and 0.14 gVFAs as $COD/gVS_i$ with the ratios of 2, 1, 0.5 and 0.25, respectively. The volume reduction were 58%, 52%, 45% and 47% with the ratios of 2, 1, 0.5 and 0.25, respectively.

비페닐디메칠디카르복실레이트 연질캅셀제의 설계 및 제제학적 평가 (Design and Pharmaceutical Evaluation of Biphenyl Dimethyl Dicarboxylate Elastic Capsules)

  • 전인구;곽혜선;문지현
    • Biomolecules & Therapeutics
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    • 제4권4호
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    • pp.419-427
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    • 1996
  • To solubilize practically insoluble biphenyl dimethyl dicarboxylate (DDB), which has been used for the treatment of chronic hepatitis as tablets or hard capsules, the solubilities of DDB in various hydrophilic, oily and hydrocarbon vehicles, and aqueous surfactant solutions were measured by high performance liquid chromatography. It was found that, among the vehicles studied, polyethylene glycol (PEG) 300 revealed the best solvency, and the solubility reached 17.6 mg/ml at 37$^{\circ}C$. The addition of glycyrrhizic acid ammonium salt (GAA) to DDB-PEG 300 solution (5-20 mg/g) inhibited the formation of precipitates, and at the concentration of 10 mg/g, any precipitaction was not observed even after 2 years at 4$^{\circ}C$. Furthermore, GAA markedly enhanced the permeation of DDB through the rabbit duodenal mucosa in a concentration dependent manner. The addition of copolyvidone (ca. 1.0%) to DDB-GAA-PEG 300 system (1 : 0.5 97.5 w/w) was most effective in preventing the considerable precipitation of DDB-PEG 300 solution (7.5 mg/750 mg) when mixed with water of 300-900 ml at 37$^{\circ}C$. GAA showed a synergistic effect in the prevention of precipitate formation. This finding suggests that this DDB formulation may form less precipitation when DDB soft capsules disintegrate and diffuse into the gastrointestinal fluid, resulting in improving the bioavailability Dissolution rate of DDB (7.5 mg) from sort elastic capsules of DDB-GAA-PEG 300 system was rapid. The supersaturation state was maintained for 2 hr at the concentration of 7.35$\pm$3.3 mg in 900 ml of water without precipitation. The total amount of DDB dissolved from this new formulation was 5.3 and 6.1 times higher, when compared to marketed DDB tablets (25 mg) and capsules (7.5 mg), respectively.

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Pharmacokinetic Characterization of Nano-emulsion Vitamin A, D and E (LaVita) in Rats

  • Lee, Young-Ju;Kwon, Min;Kim, Tae-Hwan;Kim, Kyun;Jeong, Sang-Hee;Chang, Hee-Ra
    • 한국환경농학회지
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    • 제30권2호
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    • pp.196-201
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    • 2011
  • BACKGROUND: Bioavailability enhancement by solubilization of lipophilic drugs in nano-emulsion has been reported and it may be useful in pharmaceutical and nutraceutical products. This study was performed to compare in vivo bioavailability of nano-emulsion formulation with that of the general product as control. METHODS AND RESULTS: The pharmacokinetics assessment of Vitamin A, D and E complex of nanoemulsion formulation (LaVita), in comparison to the general product, was performed in the male rat plasma by a single oral dose at 20 mL/kg body weight (n=3/group). For nano-emulsion formulation (LaVita), $C_{max}$ of vitamin A and E in plasma were much higher and the area under the curve (AUC) of vitamin A, D and E were 14-63% higher, and the half-life of vitamin E was 2-fold longer than the general product. According to statistical analysis, each $C_{max}$ of vitamin A, D & E was significantly higher (p<0.01, 0.05 and 0.01, respectively) than that of general product. Half-life of vitamin A was significantly higher (p<0.01) and AUC of vitamin A and D were also significantly higher than the general product. CONCLUSION(s): Considering significant increment of $C_{max}$ and AUC, LaVita made of nano-emulsion could be more effective the absorption rate and extent for bioavailability of vitamin A, D & E than those of general product.

고분자형 계면활성제가 마이셀 촉진 한외여과법에 의한 1-나프틸 아민의 제거에 미치는 영향 (Effect of Polymeric Surfactant on the Separation of 1-Naphthylamine by Micellar Enhanced Ultrafiltration Membranes)

  • Youngkook Choi;Soobok Lee;Minok Koo;Yutaka Ishigami;Toshio Kajiuchi
    • 멤브레인
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    • 제7권3호
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    • pp.131-135
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    • 1997
  • 신규 고분자형 계면활성제($\alpha$-allyl-$\omega$-methoxy polyoxyethylene and maleic anhydride block copolymer)를 사용하는 고분자형 마이셀 촉진 한외여과법을 제안하였다. 제거용질로서는 염료의 중간체이며 발암성 물질인 1-나프틸 아민을 사용하였다. 고분자형 마이셀의 촉진효과는 중공사형 폴리아크리로니트릴 막(분획 분자량 6,000, 표면적 0.017$m^2$)을 사용하여 조사하였다. 플럭스의 선형의존성은 0.6kg/${cm}^2$까지 유지되었고, 점차 압력증가에 따라 플럭스 증가율은 감소하였다. 고분자형 마이셀을 첨가하지 않은 상태에서의 제거율은 2mM의 용질에 대하여 0.19, 2 wt.%의 고분자를 첨가한 상태에서의 제거율은 0.96이었다 고분자형 마이셀 내부로의 가용화가 분리효율을 5배 촉진시킨 것을 확인하였다.

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하수 일차슬러지의 세정산발효 특성에 대한 Microwave 전처리의 영향 (Effects of Microwave Irradiation for Elutriated Acid Fermentation of Sewage Primary Sludge)

  • 권구호;이원식;민경석
    • 한국물환경학회지
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    • 제23권4호
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    • pp.498-503
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    • 2007
  • The performance of elutriated acid fermentation to evaluate the effects of microwave irradiation and pH control as pretreatment was investigated. The MW pH 7 reactor which was used the pretreated primary sludge as microwave irradiation was operated at pH 7 and $35^{\circ}C$. The EAF pH 9 reactor was operated at pH 9 and $35^{\circ}C$ without pretreatment. The SCOD and VFAs production rate were 0.17 gSeOD/gVSrem. and 0.27 gVFAs as COD/gVSrem. in MW pH 7 reactor, 0.16 gSCOD/gVSrem. and 0.24 gVFAs as COD/gVSrem. in EAF pH 9 reactor, respectively. VS and Volume reduction were 54% and 48% in MW pH 7 reactor, 54.6% and 36% in EAF pH 9 reactor, respectively. A comparison of the microwave irradiation and controlled pH in elutriated acid fermentation showed that the former is more efficient in SCOD and VFAs production and it rises to slightly higher reduction in the volume of the sludge. In addition, E. coli. was not detected in the wasting sludge of MW pH 7 reactor. Based on the results, microwave irradiation appeared to be one of the viable options for generating class A sludge. According to the batch tests, sequencing batch test which was used the pretreated primary sludge as microwave was performed at pH 7 and $35^{\circ}C$, SCOD production was 0.16 gSCOD/gVSrem., VS reduction and volume reduction were 64% and 63%, respectively.

Solubility and Stability of Melatonin in Propylene glycol and 2-hydroxypropyl-${\beta}$-cyclodextrin vehicles

  • Lee, Beom-Jin;Choi, Han-Gon;Kim, Chong-Kook;Parrott, Keith-A.;Ayres, James-W.;Sack, Robert-L.
    • Archives of Pharmacal Research
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    • 제20권6호
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    • pp.560-565
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    • 1997
  • The physicochemical properties of melatonin (MT) in propylene glycol (PG) and 2-hydroxypropyl-.betha.-cyclodextrin $(2-HP{\beta}CD)$ vehicles were characterized. MT was endothermally decomposed as determined by differential scanning calorimetry (DSC). Melting point and heat of fusion obtained were $116.9{\pm}0.24^{\circ}C $.and $7249{\pm}217 cal/mol$., respectively. MT as received from a manufacture was very pure, at least 99.9%. The solubility of MT in PG solution increased slowly until reaching 40% PG and then steeply increased. Solubility of MT increased linearly as concentration of $2-HP{\beta}CD$ without PG INCREASED$(R^2=0.993)$. MT solubility in the mixtures of pg and $2-HP{\beta}CD$ also increased linearly but was less than the sum of its solubility in $2-HP{\beta}CD$ and PG individually. The MT solubility was low in water, simulated gastric or intestinal fluid but the highest in the mixture of PG(40v/v%) and $2-HP{\beta}CD$ (30w/v%) although efficiency of MT solubilization in $2-HP{\beta}CD$ decreased as the concentration of PG increased. MT was degraded in a fashion of the first order kinetics $(r^2>0.90)$. MT was unstable in strong acidic solution (HCl-NaCl buffer, pH 1.4) but relatively stable in other pH values of 4-10 at $70^{\circ}C$. In HCl-NaCl buffer, MT in 10% PG was more quickly degraded and then slowed dpwm at a higher concentration. However, the degradation rate constant of MT in 2-HP.betha.CD was not changed significantly when compared to the water. The current studies can be applied to the dosage formulations for the purpose of enhancing percutaneous absorption or bioavailability of MT.

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Potentiality of Beneficial Microbe Bacillus siamensis GP-P8 for the Suppression of Anthracnose Pathogens and Pepper Plant Growth Promotion

  • Ji Min Woo;Hyun Seung Kim;In Kyu Lee;Eun Jeong Byeon;Won Jun Chang;Youn Su Lee
    • The Plant Pathology Journal
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    • 제40권4호
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    • pp.346-357
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    • 2024
  • This study was carried out to screen the antifungal activity against Colletotrichum acutatum, Colletotrichum dematium, and Colletotrichum coccodes. Bacterial isolate GP-P8 from pepper soil was found to be effective against the tested pathogens with an average inhibition rate of 70.7% in in vitro dual culture assays. 16S rRNA gene sequencing analysis result showed that the effective bacterial isolate as Bacillus siamensis. Biochemical characterization of GP-P8 was also performed. According to the results, protease and cellulose, siderophore production, phosphate solubilization, starch hydrolysis, and indole-3-acetic acid production were shown by the GP-P8. Using specific primers, genes involved in the production of antibiotics, such as iturin, fengycin, difficidin, bacilysin, bacillibactin, surfactin, macrolactin, and bacillaene were also detected in B. siamensis GP-P8. Identification and analysis of volatile organic compounds through solid phase microextraction/gas chromatography-mass spectrometry (SPME/GC-MS) revealed that acetoin and 2,3-butanediol were produced by isolate GP-P8. In vivo tests showed that GP-P8 significantly reduced the anthracnose disease caused by C. acutatum, and enhanced the growth of pepper plant. Reverse transcription polymerase chain reaction analysis of pepper fruits revealed that GP-P8 treated pepper plants showed increased expression of immune genes such as CaPR1, CaPR4, CaNPR1, CaMAPK4, CaJA2, and CaERF53. These results strongly suggest that GP-P8 could be a promising biocontrol agent against pepper anthracnose disease and possibly a pepper plant growth-promoting agent.

계면활성제 거품을 이용한 미생물반응기에서의 기체상 톨루엔 분해 (Bioactive Foam Reactors for the Enhanced Biological Degradation of Toluene)

  • 김용식;손영규;김지형;송지현
    • 대한환경공학회지
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    • 제27권5호
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    • pp.468-475
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    • 2005
  • 휘발성 유기화합물(VOCs)의 제거를 위한 담체충진형 바이오필터법은 운전이 용이하고 처리비용이 낮다는 장점에도 불구하고 낮은 운전성능과 막힘현상등의 문제를 안고 있다. 이에 대한 대안으로 계면활성제로 형성된 거품을 사용해 VOCs의 물질전달율과 분해효율을 향상시킨 미생물반응기(BFR)가 제안되었다. 본 연구는 VOCs 저감기술로서 BFR의 적용가능성을 확인하기 위하여 수행되었다. 우선, BFR에 사용될 계면활성제를 선정하기 위해, 4종류의 계면활성제를 대상으로 회분실험을 수행하였으며, 실험결과 TritonX-100이 미생물의 생분해도에 미치는 영향이 가장 적어 BFR에 적용하기 적합한 계면활성제로 판명되었다. 선정된 계면활성제를 BFR에 첨가하고, 반응기 내에 유입되는 가스의 체류시간과 톨루엔 유입부하량을 변화시키면서 반응기의 운전성능을 평가하였다. 가스체류시간이 0.5분에서 2분으로 증가하면서 반응기의 톨루엔 분해율도 50%에서 80%로 증가하였다. 그러나 톨루엔 유입부하량이 $38\;g/m^3/hr$에서 $454\;g/m^3/hr$으로 증가하면서 톨루엔 분해율은 70%에서 20%로 감소하였다. 본 실험에서는 BFR의 최대분해능은 $108\;g/m^3/hr$로 나타나 기존 담체 충진형 바이오필터에 비해 높았으며, 따라서 BFR 시스템이 기존의 담체를 이용하는 생물학적 VOCs 저감기술에 대한 대안으로서 가능성이 있음을 알 수 있었다. 하지만, 높거나 낮은 가스유속에서 거품이 안정적으로 발생하지 않는 점 등은 여전히 해결해야할 과제로 남아있다.

산/가스 분리 혐기소화공정을 이용한 음식물 탈리액의 처리효율 평가 (The Process Efficiency Evaluation of the Food Supernatant Using A/G (Acid/Gas) Phased Anaerobic Digestion)

  • 배종훈;박노백;전동걸;전항배;양석준
    • 대한환경공학회지
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    • 제34권3호
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    • pp.214-222
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    • 2012
  • 본 연구는 음식물쓰레기를 혐기성 소화를 이용하여 중온 및 고온에서의 OLR에 따른 처리효율을 평가하였다. 실험은 중온($35^{\circ}C$) 및 고온($55^{\circ}C$)의 온도조건에서 산발효 회분식 실험, BMP test 그리고 연속식 실험을 실시하였다. 산발효 회분식 실험의 경우 VS 제거효율은 각각의 온도에서 27.3, 30.6%이었으며, $35^{\circ}C$에 비해 $55^{\circ}C$에서 제거효율이 더 높았다. VS와는 반대로 SCOD는 시간이 지남에 따라 농도가 증가하였고, 각 온도의 가용화율은 27.4, 33.4%로 VS가 제거되는 농도와 SCOD가 증가하는 농도가 비슷하였다. BMP test에서 최종 메탄수율 결과 중온 461, 고온 413 $mL{\cdot}CH_4/gVS$가 발생하였다. 산발효조에서 SCOD 가용화율은 고온이 중온에 비해 8~7% 정도 높게 나타났다. 중온메탄발효조의 경우 낮은 유기물 부하에서 고온메탄 발효조에 비해 유기물제거 효율이 높게 나타났지만 높은 유기물 부하에서는 고온메탄발효조가 유리하였다. 고온메탄발효조의 VS제거 효율이 중온에 비해 낮은 경향이었으나, 6 $kgCOD/m^3{\cdot}day$ 고형물 농도에서는 중온소화의 VS제거 효율은 감소하였다. 중온메탄생성조의 유기물 부하에 따른 가스발생량은 12.6, 21.6, 27.4 L/day이었고, 고온의 경우 14.3, 20.6, 25.2 L/day로 중온소화에 비해 각각의 모드별로 약 5~10% 낮은 메탄발생량을 나타내었다.