• Title/Summary/Keyword: PROPYLENE GLYCOL

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Formulation and Evaluation of Loxoprofen Plasters (록소프로펜 플라스터의 제제설계 및 평가)

  • 김태성;전인구
    • Biomolecules & Therapeutics
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    • v.9 no.4
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    • pp.298-306
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    • 2001
  • To develop a novel transdermal delivery system of loxoprofen (LP), a potent antiinflammatory and analgesic agent, the effects of vehicle composition and drug loading dose on the skin permeation property were investigated. And in vivo skin absorption property studied by analysing the $C_{max}$ and AUC was investigated after applying the developed plaster systems on rabbit back skin. Addition of isopropyl myristate (IPM) and IPM-diethylene glycol monoethyl ether (DGME) cosolvent in the plaster showed higher permeation rates than those from propylene glycol laurate-DGME cosolvent systems. As the concentration of LP in the plaster increased from 0.56 mg/$\textrm{cm}^2$ to 1.19 mg/$\textrm{cm}^2$, the drug release and skin permeation rates increased linearly. At loading dose of 1.19 mg/$\textrm{cm}^2$, the flux reached 35.6 $\mu$g/$\textrm{cm}^2$/hr. New LP plasters showed a good adhesive property onto skin, and showed no crystal formation. The AU $C_{0-24hr}$ and $C_{max}$ after dermal application of LP plaster (60 mg/70 $\textrm{cm}^2$) were found to be 6951$\pm$230 ng.hr/ml and 400$\pm$44 ng/ml, respectively. And the plasma concentration maintained above 300 ng/ml up to 24 hr period. In the carrageenan-induced rat paw edema test, LP plaster showed similar inhibition rate with marketed ketoprofen (Ketoto $p^{R}$) plaster.aster.r.

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Effects of Cryoprotectants and Equilibration Time on the Viability of Frozen-thawed Porcine Oocytes (동결-융해된 돼지난포란의 생존성에 대한 항동해제와 평형시간의 영향)

  • 이장희;김창근;박충생
    • Journal of Embryo Transfer
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    • v.12 no.3
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    • pp.315-324
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    • 1997
  • This study was undertaken in an effort to develop a cryopreservation system of immature and mature porcine oocytes. For this aim, the experiments were designed to examine the effect of cryoprotectants and equdibration time on the viability of frozen-thawed oocytes by using trypan blue(TB) and fluorescene diacetate(FDA) test. The viability of frozen immature oocytes evaluated by TB test was slightly higher than that of frozen mature oocytes. The viability(25.O%) after IVM of frozen-thawed immature oocytes greatly decreased that(42.9%) of oocytes just after thawing, but it was higher than frozen-thawed mature oocytes(15.8%). When immature oocytes were equilibrated for 10, 20 and 30 minutes before freezing the oocyte viability was 20.0, 31.3 and 42.9%, respectively. There was a tendency for long equilibration before oocyte freezing to be more effective for the immature oocytes and a short equilibration time for mature oocytes. Although there was no difference in viability index of frozen oocytes hetween the viability test methods, the index of TB test was slightly higher than that of FDA test. The viability(FDA test) of frozen-immature oocytes with 3 different crtoprotectants was 22.2% for propylene glycol(PG), 9.3% for polyehtylene glycol(PEG) and 65.6% for PG+PEG, in which PG+PEG was more protective against freezing effect.

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Solubilization of CPD, a Novel Antivirus Compound Containing Pirimidine Structure, in Aqueous Solution (신규 피리미딘 구조를 함유한 항바이러스성 화합물 CPD의 수용액중 가용화)

  • Song Sukgil;Kweon Ho-Seok;Chung Youn Bok
    • YAKHAK HOEJI
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    • v.50 no.1
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    • pp.1-7
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    • 2006
  • The purpose of the present study was to formulate the aqueous solution of 1-cyclopent-3-enylmethyl-6(3,5-dimethyl-benzoyl)-5-ethyl-1H-pyrimidine-2,4-dione (CPD), a novel antivirus compound containing pirimidine structure. For this purpose, the effects of various solubilization agents such as cosolvents [ethanol, propylene glycol (PG), polyethylene glycol 300 (PEG 300), polyethylene glycol 400 (PEG 400), glycerin], surfactants (Tween 80, Cremophor$^{(R)}$ RH40, Cremophor$^{(R)}$ EL, Poloxamer 407, Poloxamer 188) and a complexation agent [hydroxypropyl-${\beta}$-cyclodextrin (HPBCD)] , on the solubility of CPD in aqueous solution were evaluated. The solubility of CPD in water was under $1\;{\mu}g/ml$ at $20^{\circ}C$. Cosolvents such as ethanol, PG, PEG 300, PEG 400 and glycerin did not enhance the solubility of CPD at the $0{\sim}40\%$ concentration range. The solubility of CPD was significantly elevated by the addition of cosolvents over the $80\%$ concentration range. On the other hand, tween 80, Cremophor$^{(R)}$ L, Cremophor$^{(R)}$ RH40, and HPBCD showed enhanced effects on the solubility of CPD. The enhanced effects of Poloxamer 407 or Poloxamer 188 on the CPD solubility were less pronounced compared with tween 80, Cremophor$^{(R)}$ L or Cremophor$^{(R)}$ RH40. As a results, tween 80 aqueous solution was selected as an optimum solvent system. The aqueous solutions containing $20\%$ tween 80 were formulated as a dosing solution containing CPD for its intraperitoneal and intrahypodermic administration, respectively, The formular showed physical stability after stored for 7 days at $4^{\circ}C$.

Candida rugosa Lipase-Catalyzed Production of Optically Pure S-(+)-Ketoprofen (Candida rugosa 리파제를 이용한 광학적으로 순수한 S-(+)-Ketoprofen의 생산)

  • 김민곤;최순자;최원아;김철호;정봉현
    • KSBB Journal
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    • v.14 no.2
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    • pp.225-229
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    • 1999
  • Enzymatic resolution reactions were investigated using Candida rugosa lipase for the production of potically pure S-(+)-Ketoprofen. When the enzymatic hydroysis (and esterification) of recemic ketoprofen esters (and recemic ketoprofen with alcohol) was investigated comparatively, aqueous media was more specific for S-enantiomer than organic media. In the enzymatic hydrolysis of racemic ketoprofen ethyl ester in aqueous media, optimal temperature and pH for enantioselectivity were $37^{\circ}C$ and 4, respectively. The stereoselectivity of the enzyme was enhanced by adding dialcohols such as ethylene glycol and propylene glycol. The enantiomeric ratio obtained in the 40 %(v/v) ethylene glycol was 2-fold higher than that without the additive. By adding $CH_2Cl_2$, $CHCl_3$ and $CCl_4$ (5%,v/v), the enantioselectivity was reversed. A dramatic increase in the stereoselectivity was achieved using lipase purified by anion exchange chromatography. The type A lipase(the first eluted lipase fraction) showed an enantiomeric ratio of >100, whereas the type B lipase(the second eluted lipase fraction) exhibited enantimomer ratio of 9.0 in the hydrolysis of racemic ketoprofen ethyl ester.

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Solubilization of IH-901, a Novel Intestinal Metabolite of Ginseng Saponin, in Aqueous Solution (인삼사포닌의 소장내 최종대사물인 IH-901의 수용액중 가용화)

  • Kwon, Oh-Seung;Chung, Youn-Bok
    • Journal of Pharmaceutical Investigation
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    • v.34 no.5
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    • pp.385-391
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    • 2004
  • The purpose of the present study was to formulate the aqueous solution of $20-O-{\beta}-D-glucopyranosyl-20(S)-protopanaxadiol\;(IH-901)$, an intestinal bacterial metabolic derivative from Ginseng protopanaxadiol saponin. For this purpose, the effects of various solubilization agents such as cosolvents [ethanol, propylene glycol (PG), polyethylene glycol 300 (PEG 300), polyethylene glycol 400 (PEG 400), glycerin], surfactants $(Tween\;80,\;Cremophor^{\circledR}\;RH40,\;Cremophor^{\circledR}\;EL,\;Poloxamer\;407,\;Poloxamer\;188)$ and a complexation agent $[hydroxypropyl-{\beta}-cyclodextrin\;(HPBCD)]$, on the solubility of IH-90l in aqueous solution were evaluated. The solubility of IH-901 in water was under $1\;{\mu}g/ml\;at\;20^{\circ}C$. Cosolvents such as ethanol, PG, PEG 300, PEG 400 and glycerin did not enhance the solubility of IH-901 at the 0 - 40% concentration range. The solubility of IH-901 was significantly elevated by the addition of cosolvents over the 80% concentration range. On the other hand, tween 80, $Cremophor^{\circledR}\;EL,\;Cremophor^{\circledR}\;RH40$ and HPBCD showed enhanced effects on the solubility of IH-901. The enhanced effects of Poloxamer 407 or Poloxamer 188 on the IH-901 solubility were less pronounced compared with $Cremophor^{\circledR}\;EL\;or\;Cremophor^{\circledR}\;RH40$. As a results, $Cremophor^{\circledR}$ aqueous solution was selected as an optimum solvent system. The aqueous solutions containing 10% $Cremophor^{\circledR}\;EL$ and 7% $Cremophor^{\circledR}\;RH40$ were formulated as dosing solutions containing 5.0 mg/ml of IH-901 for its intravenous and oral administration, respectively. The formular showed physical stability after stored for 7 days at $4^{\circ}C$.

Effect of Heating Condition, Additives and Solvents on Rheology of Squid Meat Paste Products (오징어 연제품의 물성 개선을 위한 탄력증강제 및 용매처리 효과)

  • 배태진;김해섭;최옥수
    • The Korean Journal of Food And Nutrition
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    • v.16 no.2
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    • pp.130-137
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    • 2003
  • The squid had not been utilized for gel products because of its lower gel forming ability. The objectives of this study were as followed; 1) the optimum heating condition on squid meat paste products and 2) the optimum added level for jelly strength of squid meat paste products. Optimum heating conditions of squid meat kamaboko were as followed; setting(pre-heating) at 15$^{\circ}C$ or 55$^{\circ}C$ for 2 hours and heating at 9$0^{\circ}C$ for 60 minutes. The additives examined were as follows; 20mM EDTA, 10mM PMSF, 5 $\mu$mol/100g TGase, 0.2% potassium bromate, 2% collagen, 2% sucrose ester of stearic acid and 1% egg shell powder. The effects of additives on jelly strength were observed as follow, in descending order; 10mM of PMSF>5 $\mu$mo1/100g of TGase>0.2% of potassium bromate>20mM of EDTA. But sucrose ester of stearic acid and 1% egg shell powder were no effect. The solvents examined were as follows; n-amyl alcohol, n-butyl alcohol, n-hexyl alcohol, ethyl alcohol, ethylene glycol, propylene glycol and glycerin glycol. It showed that high jelly strength as 787gㆍcm for 3% of n-butyl alcohol and 749gㆍcm for 3% of n-amyl alcohol. To adding 5% of n-butyl alcohol and n-amyl alcohol, gave the highest jelly strength and water holding capacity(WHC). Effect of alcohol on jelly strength appeared higher value at added 5% of n-butyl alcohol than n-amyl alcohol, and flying squid product was higher than jumbo squid product.

Improvement of the heat transfer ability on the heat transfer printing (열 전사날염의 열전사성 향상에 관한 연구)

  • Lee, Mun-Soo;Song, Kyung-Hun
    • The Journal of Natural Sciences
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    • v.11 no.1
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    • pp.151-157
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    • 1999
  • The study was investigated the improved printing effect of heat transfer ability for the cotton fabric treated with disperse dyes. Some important factors were studied to determine the most optimal conditions such as concentration of dye, treated time and temperature, after treatment and before treatment using swelling agent, and molecular weight of dye. The fastness to laundering and light for heat transfer printing was measured.The optimal conditions of heat transfer printing for cotton fabric treated with disperse dye were concentration of 5% owf, treated temperature of $200^{\circ}C$, treated time of 3 minute. The diffusion of disperse dyes inside cotton fabric was accelerated as a result of swelling agent such as glycerin, ethylene glycol, tetramethylene glycol, propylene glycol using in this study. The effects of heat transfer printing were increased that the increasement of before treatment time for swelling agent, decrease of molecular weight of dye.

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Phase Behavior Study of Fatty Acid Potassium Cream Soaps (지방산 칼륨 Cream Soaps 의 상거동 연구)

  • Noh, Min Joo;Yeo, Hye Lim;Lee, Ji Hyun;Park, Myeong Sam;Lee, Jun Bae;Yoon, Moung Seok
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.48 no.1
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    • pp.55-64
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    • 2022
  • The potassium cream soap with fatty acid called cleaning foam has a crystal gel structure, and unlike an emulsion system, it is weak to shear stress and shows characteristics that are easily separated under high temperature storage conditions. The crystal gel structure of cleansing foams is significantly influenced by the nature and proportion of fatty acids, degree of neutralization, and the nature and proportion of polyols. In order to investigate the effect of these parameters on the crystal gel structure, a ternary system consisting of water/KOH/fatty acid was investigated in this study. The investigation of differential scanning calorimeter (DSC) revealed that the eutectic point was found at the ratio of myristic acid (MA) : stearic acid (SA) = 3 : 1 and ternary systems were the most stable at the eutectic point. However, the increase in fatty acid content had little effect on stability. On the basis of viscosity and polarized optical microscopy (POM) measurements, the optimum degree of neutralization was found to be about 75%. The system was stable when the melting point (Tm) of the ternary system was higher than the storage temperature and the crystal phase was transferred to lamellar gel phase, but the increase in fatty acid content had little effect on stability. The addition of polyols to the ternary system played an important role in changing the Tm and causing phase transition. The structure of the cleansing foams were confirmed through cryogenic scanning electron microscope (Cryo-SEM), small and wide angle X-ray scattering (SAXS and WAXS) analysis. Since butylene glycol (BG), propylene glycol (PG), and dipropylene glycol (DPG) lowered the Tm and hindered the lamellar gel formation, they were unsuitable for the formation of stable cleansing foam. In contrast, glycerin, PEG-400, and sorbitol increased the Tm, and facilitated the formation of lamellar gel phase, which led to a stable ternary system. Glycerin was found to be the most optimal agent to prepare a cleansing foam with enhanced stability.

Studies on Computer Optimization Techniques for Hydrophilic Vehicle Compositions

  • Lee, Chi-Ho;Shin, Young-Hee
    • Archives of Pharmacal Research
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    • v.11 no.3
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    • pp.185-196
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    • 1988
  • The inflence of hydrophilic vehicles on percutaneous absorption rate of griseofulvin was studied using intact skin of full thickness of hairless rat. The in vitro absorption rates were used as the characteristics for deciding the optimum formula of ointment vehicles. The optimum formula of vehicle compositions for maximum absorption rate was obtained from the polynomial regression equation and the two graphical techniques, contour graph and partial derivative graph. It was composed of sodium lauryl sulfate (1.65 W /W%), white petrolatum (16.5 W /W%), propylene glycol (12.0 W /W%), and stearyl alcohol (19.6W /W%). The experimental value obtained from the optimum formula and the prediction value were 33.99 and 33.87 ${\mu}g/\sqrt{min}$, respectively. From these results, it was believed that optimum formula for semisolid dosage forms could be obtained from the application of the optimization technique used in this study.

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The Effect of Proteases on Contamination Removal (프로테아제의 오염 세정 효과)

  • Kim, Ju-Hye;Gwon, Mi-Yeon
    • Proceedings of the Korean Society of Dyers and Finishers Conference
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    • 2008.04a
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    • pp.181-183
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    • 2008
  • Four different subtilisins of protease were investigated to see their effects on the cleaning activity. The cleaning solution was formulated with various non-ionic surfactants and other additives such as propylene glycol, triethanolamine, pH balancer etc. to evaluate their effect on enzyme activity as well. Evaluation of formulated cleaning solution was carried under K0120 using pre-soiled textiles from EMPA. The results showed that the cleaning activity on soil removal was not severly influenced by surfactant but the enzyme mostly. In addition, the activity of enzymes was not much affected by the type of surfactants as long as the surfactants were non-ionic. Liquinase among the four enzymes used in this study showed the best performance on soil removal, especially blood stain.

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