• Title/Summary/Keyword: Water-soluble surfactant

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Formulation Design and Evaluation of Ursolic Acid Microemulsion Delivery System for Topical Formulation (마이크로에멀젼을 이용한 우르솔릭산 피부 적용제제의 설계 및 평가)

  • Park, Jong-Hee;Kyong, Kee-Yeol;Lee, Gye-Won;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
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    • v.35 no.4
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    • pp.233-241
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    • 2005
  • Ursolic acid (UA), a bioactive triterpene acid, has been known to increase collagen content in human skin in addition to other actions such as anti-inflammatory, skin-tumor prevention and anti-invasion. However, it is poorly soluble in water. Therefore, we firstly prepared microemulsion system with benzyl alcohol, ethanol and Cremophor EL, RH 40 and Brij 35 as surfactant in order to increase solubility of UA and then prepared microemulsion was dispersed in o/w cream base for the topical delivery of UA in an effort to improve anti-wrinkle effect. The pseudo-ternary phase diagrams were developed and various microemulsion formulations were prepared using benzyl alcohol as an oil, Cremophor EL, RH 40 and Brij 35 as a surfactant. The droplet size of microemulsions was characterized by dynamic light scattering. The accumulation of VA in the skin from topical cream was evaluated in vitro using hairless mouse skins. The mean droplet size was $26.8{\pm}6.6$ nm for microemulsions II with Cremophor EL. All UA creams showed pseudoplastic flow and hysterisis loop in their rheogram, depending on the type of materials added in topical creams. The in vitro accumulation data demonstrated the UA topical cream prepared with the combination of Poloxamer 407 and Xanthan gum as a copolymer showed higher accumulation percentage than those prepared with either Poloxamer 407 or Xanthan gum. These results suggest that UA topical cream using microemulsion systems may be promising for the topical delivery of UA.

Transport behavior of a surfactant tracer(CPC) with Langmuir type adsorption isotherm on NAPL-water interface in a homogeneous porous medium (NAPL-물 계면에서 Langmuir형 흡착특성을 보이는 계면추적자(CPC)의 다공성 균질매질내 유동특성)

  • 김헌기;문희수;이상훈
    • Journal of Soil and Groundwater Environment
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    • v.6 no.2
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    • pp.3-13
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    • 2001
  • It has been known that nonlinear characteristics of sorption affect the transport behavior of water soluble pollutants in soils. However detailed experimental studies have not been performed to verify the effect of non-linearity of adsorption isotherm on transport of chemicals in porous media. In this research, the distortion of breakthrough curves of a cationic surfactant (cetylpyridinium chloride, CPC) in a engineered stainless steel column packed with glass beads were investigated. Glass beads with about 110 $\mu\textrm{m}$diameter coated with a thin n-decane film were used as the media providing the sorption surface for CPC. The CPC adsorption isotherm on the surface of n-decane from aqueous solution was a typical Langmuir type. The breakthrough curve of CPC using step Input showed a late breakthrough on the front side and early breakthrough on the back side accordance to the shape of the isotherm. The retardation factor of CPC was found to be a strong function of the input concentration, which also a manifestation of the non-linearity of the isotherm. The retardation factors for the CPC with step input agreed with those of pulse input that the maximum concentrations are controlled to be the same as the step input concentrations. This results support the validity of the unproven field practices of using hydrogeotracers with non-linear adsorption isotherms to determine the hydrogeological parameters, e.g., NAPL saturation, air-water or NAPL-water interfacial areas.

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Formulation of Rectal Supopositories of Omeprazole (오메푸라졸 함유 직장좌제의 제제설계)

  • 이창현;황성주;오세종;이계주
    • YAKHAK HOEJI
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    • v.37 no.4
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    • pp.370-382
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    • 1993
  • In order for formulation of rectal containing OMZ, the OMZ suppositories were prepared using water-soluble base, PEG 4000 base and oil-soluble base, Witepsol H 15. Chemical stability of OMZ in suppositories was increased when Witepsol H 15 was used as a suppository base and arginine was added as a stabilizer. The decomposition of OMZ in suppository bases followed the first-order kinetics and their rate constants were 0.11 day $^{1}(t_{1/2}$=/6.25 days) for Witepsol H 15 suppository and 0.48 day $^{1}(t_{1/2}$=/1.43 days) for PEG 4000 suppository, respectively. On the other hand, the decomposition rate constants of Witepsol suppository and PEG suppository stabilized with arginine were 3.89$\times$10$^{-3}$(t$_{1/2}$=171.1 days) and 8.76$\times$10$^{-3}$ day $^{1}(t_{1/2}=79.9 days), respectively. Shelf-lives of the Witepsol and PEG suppositories stabilized with arginine were t$_{90%}$=291.8 days and t$_{90%}$=282.1 days at $35^{\circ}C$ and 75% RH, respectively. The dissolution test of OMZ suppositories was performed by rotating dialysis cell(RDC) method and the release rate constant was calculated by the simplified Higuchi's equation, Q'=K' t$^{1/2}$. Dissolution of OMZ from suppositories was augmented as arginine was added, particle size of OMZ was reduced and a suitable surfactant such as SLS was added. RDC method was more appropriate and available than Paddle method to evaluate the dissolution rate of lipophilic-base suppositoies. Arginine was found to be a very useful exipient for the enhancement of stability and dissolution of OMZ in suppositories.

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Solid Dispersion as a Strategy to Improve Drug Bioavailability (고체분산체를 이용한 약물의 생체이용율 향상을 위한 전략)

  • Park, Jun-Hyung;Chun, Myung-Kwan;Cho, Hoon;Choi, Hoo-Kyun
    • KSBB Journal
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    • v.26 no.4
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    • pp.283-292
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    • 2011
  • Solid dispersion is one of well-established pharmaceutical techniques to improve the dissolution and consequent bioavailability of poorly water soluble drugs. It is defined as a dispersion of drug in an inert carrier matrix. Solid dispersions can be classified into three generations according to the carrier used in the system. First and second generations consist of crystalline and amorphous substances, respectively. Third generation carriers are surfactant, mixture of polymer and surfactants, and mixture of polymers. Solid dispersions can be generallyprepared by melting method and solvent method. While melting method requires high temperature to melt carrier and dissolve drug, solvent method utilizes solvent to dissolve the components. The improvement in dissolution through solid dispersions is attributed to reduction in drug particle size, improvement in wettability, and/or formation of amorphous state. The primary characteristics of solid dispersions, the presenceof drug in amorphous state, could be determined by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and fourier-transformed infrared spectroscopy (FTIR). In spite of the significant improvement in dissolution by solid dispersion technique, some drawbacks have limited the commercial application of solid dispersions. Thus, further studies should be conducted in a direction to improve the congeniality to commercialization.

Structure-Property Relationship of PVA-SbQ Water Soluble Photosensitive Polymer and its Application to Screening Process of Color Monitor (PVA-SbQ 수용성 감광성 고분자의 구조와 감도관계 및 칼라 수상관 스크린 공정에의 응용)

  • Park, Lee Soon;Han, Yoon Soo;Kim, Bong Chul
    • Applied Chemistry for Engineering
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    • v.7 no.2
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    • pp.379-386
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    • 1996
  • Photosensitive compound, 1-methyl-4-[2-(4-diethylacetylphenyl)ethenyl] pridinium methosulfate(SbQ-A salt), was synthesized from dimethyl sulfate, terephthalaldehyde mono-(diethylacetal) and 4-picoline. SbQ-A salts were reacted with poly(vinyl alcohol)s, (PVA) in aqueous solution with phosphoric acid as catalyst to give photosensitive PVA-SbQ with different SbQ content and molecular weight. Relative photosensitivity of PVA-SbQ was determined by gray scale(GS) method. The rotative sensitivity of PVA-SbQ increased with increasing amount of bound SbQ in the case of high molecular weight(MW=77,000-79,000g/mol) as substrate and decreased with decreasing molecular weight of PVA with about constant(1.3mol%) amount of bound SbQ. The most sensitive polymer was obtained when SbQ group content in PVA-SbQ reached about 2.63mol% in the case of high molecular weight(77,000-79,000g/mol) PVA. This sample showed 90 times greater sensitivity than dichromated PVA as reference photosensitive system. PVA-SbQ photosensitive polymer synthesized was applied to the photolithographic screening process of phosphor on the panel of cathode ray tube(CRT). Phosphor slurry was made with PVA-SbQ, phosphor, a small amount of surfactant and other additives using water as medium. The slurry was coated onto panel, dried by heater, exposed to UV light and then developed by distilled water. When a small amount of cationic surfactant such as cetyltrimethylammonium chloride was used in the slurry formulation, the sharpness of phosphor pattern was equal to or better than that of dichromated PVA photosensitive polymer system used currently.

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Solubilization of Talniflumate in Microemulsion Systems (마이크로에멀젼을 이용한 탈니플루메이트의 가용화)

  • Lee, Gye-Won;Cho, Young-Ho;Kim, Hak-Hyung;Kim, Sock-Young;Kim, Do-Kyun;Kim, Eun-Hea
    • Journal of Pharmaceutical Investigation
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    • v.38 no.3
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    • pp.171-176
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    • 2008
  • Talniflumate is a nonsteroidal anti-inflammatory drug (NSAID), which has been used treat of rheumatoid diseases, is insoluble in water, therefore it has low bioavailability after oral administration. The purposes of this study were to prepare O/W or W/O microemulsions for solubilization of poorly water soluble drug, talniflumate and to formulate into other dosage form. For this purpose, we made O/W or W/O microemulsion with oil(soybean oil, IPM), surfactant (Cremophor $EL^{(R)}$, Tween 80) and water or propylene glycol and evaluated solubility of talniflumate. The microemulsion systems were very stable and showed transmittance above 95% without flocculation or aggregation. Especially, the solubility of talniflumate in the formulation B-1 containing 18% of isopropyl myristate and 71% of tween 80 was 10 times higher than that of other O/W microemulsions. The addition of propylene glycol and N-methylglutamine to the fomulation B-1 showed excellent capacity on the solubilization of talniflumate and the percentage was almost 2.0%. These results suggest that the microemulsion system may be promising for the solubility improvement of talniflumate.

Preparation and Evaluation of Non-Crystalline Cefuroxime Axetil Solid Dispersion (비결정성 세푸록심 악세틸 고체분산체의 제조 및 평가)

  • Woo, Jong-Soo;Chang, Hee-Chul;Lee, Chang-Hyun
    • Journal of Pharmaceutical Investigation
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    • v.32 no.2
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    • pp.73-80
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    • 2002
  • Cefuroxime axetil is a cephalosporin antibiotic having a high activity against a wide spectrum of Grampositive and Gram-negative microorganisms. It is a cephalosporin antibiotic which exist as 2 diastereoisomers: diastereoisomer A and B. It shows polymorphism of three forms: a crystalline form having a melting point of about $180^{\circ}C$, a substantially amorphous form having a high melting point of about $135^{\circ}C$ and a substantially amorphous form having a low melting point of about 70^{\circ}C$. The crystalline form of cefuroxime axetil is slightly soluble in water because diastereoisomer A has lower solubility than B in water. Substantially amorphous form of which there are no difference in solubility between diastereoisomer A and B has better solubility than crystalline form, but it forms a thicker gel than crystalline form upon contact with an aqueous medium. Based on this reason, cefuroxime axetil is not readily absorbable in the gastrointestinal tract, rendering its bioavailability on oral administration very low. The object of this study was to develop an improved non-crystalline cefuroxime axetil composition having a high physicochemical stability and bioavailability. A non-crystalline cefuroxime axetil solid dispersant showing no peak on a Differential Scanning Calorimetry (DSC) scan is prepared by dissolving cefuroxime axetil and a surfactant in an organic solvent; suspending a water-insoluble inorganic carrier in the resulting solution; and spray drying the resulting suspension to remove the organic solvent, said solid dispersant having an enhanced dissolution and stability of cefuroxime axetil and being useful for the preparation of a pharmaceutical composition for oral administration. Tablet was formulated with this cefuroxime axetil solid dispersant, disintegrants and other ingredients. It disintegrated and dissolved easily and dynamically in dissolution medium, so showed a good dissolution profile.

Preparation of Poly(Dt-lactide-co-glycolide) Nanoparticles by PEG-PPG Diblock Copolymer (PEG-PPG 블록 공중합체를 이용한 폴리(DL-락타이드-co-글리콜라이드) 나노입자의 제조)

  • 정택규;오유미;신병철
    • Polymer(Korea)
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    • v.27 no.4
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    • pp.370-376
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    • 2003
  • Poly(DL-lactide-co-glycolide) nanoparticles were prepared by the modified spontaneous emulsification solvent diffusion method. Polymer solution was prepared by two water-soluble organic solvents, such as ethanol and acetone. Because of its biocompatible nature, PEG-PPG diblock copolymer was used as surfactant and stabilizer. The influence of several preparative variables on the nanoparticle formation, such as type and concentration of stabilizing agent, stirring methods, water/oil phase ratio and polymer concentration were investigated in order to control and optimize the process. After preparation of nanoparticles, particle size and distribution were evaluated by the light scattering particle analyzer. As results, the particle size was 50-200 nm and dispersibility was monodisperse. It was found that the appropriate selections of binary solvent mixtures and polymeric concentrations in both organic and aqueous phases could provide a good yield and favorable physical properties of PLGA nanoparticles.

A study of Improvement on Washing and Rinsing Efficiency - Effect of the dissolution of detergent on washing and rinsing efficiency - (세탁 및 헹굼성능 향상 방안 연구 - 세제의 용해가 세탁 및 헹굼 성능에 미치는 영향 -)

  • 이옥기;표상연
    • Journal of the Korean Society of Clothing and Textiles
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    • v.18 no.1
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    • pp.23-30
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    • 1994
  • The objective of this study was to analyze the effect of the dissolution of detergent on washing and rinsing efficiency, and the possibility of saving detergent in washing. Washing and rinsing efficiency were reviewed in three different ways : A method was to input dissolved detergent by the use of rapid detergent dissolution instrument, B method was to input dissolved detergent beforehand, and C method was to input undissolved detergent. The results were as follows 1. A method > B method > C method was shown in detergency with washing time and three method's gaps were reduced because detergent dissolution effect was reduced by mechanical action in proportion of washing time. Especially, according to detergency of A method of 0.07% and C method of 0.1% was appeared approximately, saving detergent was expected by rapid dissolution of detergent. 2. A method > B method > C method was shown in detergency with washing temperature. As the washing temperature rose, the detergent reached chemically more activated state and become easily soluble. It resulted for the detergent to penetrate and adhere to laundry easily. 3. A method > B method > C method was shown in detergency with detergent concentration and C method was more sensitive than A, B method against change of detergent cocentration. Rapid detergent dissolution made it possible not only to enhance the washing efficiency but also to save the detergent because detergency of A method in low concentration is higher than that of C method. 4. A method $\geq$ B method > C method was shown in rinsing ratio with detergent input method. It indicated input dissolved detergent was advantageous in rinsing. 5. The result of anion surfactant concentration test of each process with detergent input method was shown like that A method In B method > C method in washing and reverse result was shown in rinsing. The anion surfactant concentration of C method was low during washing but high during rinsing. This was identical with previous results which shown the washing and rinsing efficiency improved with dissolved detergent usasge. 6. C method > B method > A method was shown in the degree of remaining detergent after rinsing. There was no remaining detergent after second rinsing in A and B method, but in C method four rinsings were required for the same result. Consequently, in A and B methods, less water and electricity were used, and less abrasion of cloth.

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Plasma Treatment Effect of Organic/Organic Core-Shell Acrylic Adhesive Binder (II) (Organic/Organic Core-Shell 아크릴 접착바인더의 플라즈마 처리영향 (II))

  • Seul, Soo-Duk
    • Polymer(Korea)
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    • v.34 no.2
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    • pp.89-96
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    • 2010
  • Adhesive binders with core-shell structure of organic/organic pair were prepared by emulsion polymerization of acrylic monomers, such as methyl methacrylate(MMA), ethyl acrylate(EA), n-butyl acrylate(BA), and styrene(St). Ammonium persulfate (APS) was used as an water soluble initiator in the presence of an anionic surfactant, sodium dodecyl benzene sulfonate (SDBS). Non-woven fabric and leather were impregnated with the adhesive binder. The surface of the impregnated fabric and leather were treated with plasma technique and then kinetics analysis and mechanical properties were measured. The conversions of the polymerization of core-shell binder (MMA/EA, MMA/BA) were greater than 90%. When the core-shell binder was prepared at equimolar conditions, the increasing effect of the core-shell binder on the state peel strength of the impregnated and plasma-treated non-woven/non-woven fabric has the order of MMA/St, EA/BA, BA/MMA, EA/St, and EA/MMA. When the core-shell binder was prepared at non-equimolar conditions, the increasing effect of the core-shell binder on the state peel strength of the non-woven fabric/leather has the order of MMA/BA, BA/EA, MMA/EA, St/MMA, and EA/St.