• Title/Summary/Keyword: Enhancers

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Evaluation or various vehicles and O/W Microemulsions of Flurbiprofen as Transdermal Delivery System (경피제제로서 수종의 플루비프로펜 Vehicle과 O/W 마이크로에멀젼의 평가)

  • Lee, Gye-Won;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
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    • v.28 no.3
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    • pp.141-149
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    • 1998
  • In order to reduce systemic side effects following administration, flurbiprofen was formulated as O/W microemulsion consisting of the surfactant, oil phase and aqueous phase. Particle size distribution, apparent viscosity, solubility and skin permeation of flurbiprofen in various vehicles and microemulsion were evaluated. The domain of O/W microemulsion s phase diagram had difference between oil types and the area of O/W microemulsion was wide distributed by adding to PG and cosurfactant than that of water alone. As increasing 10, 15 and 20% of Brij 97 content and 1, 2.5, 5% of oil content, the solubility of flurbiprofen in O/W microemulsions and various vehicles was $400{\sim}1,000$ and $10{\sim}500$ times higher than that of control. Also, apparent viscosity of soybean oil microemulsions was higher than that of IPM microemulsions and that of vehicle were increased as increasing vehicle content. Since skin permeation of flurbiprofen decreased as increasing viscosity, in each vehicle, it was not affected 2% ${\beta}-CD$ and decreased as increasing PG content and to 2, 5 and 10% of $HP-{\beta}-CD$. In O/W microemulsion, 5% soybean oil. 20% Brij 97 and 75% water(A-1) with high viscosity showed low skin penetration.

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Development of Clotrimazole Gels for Enhanced Transdermal Delivery

  • Cho, Hwa-Young;Kim, Dal-Keun;Park, ung-Chan;Kang, Chung;Oh, In-Joon;Kim, Seong-Jin;Shin, Sang-Chu
    • Journal of Pharmaceutical Investigation
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    • v.39 no.6
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    • pp.437-443
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    • 2009
  • To develop a topical bioadhesive formulation of clotrimazole for enhanced transdermal delivery, hydroxypropyl methylcellulose gel containing permeation enhancer was formulated and permeation studies were carried out. The release characteristics of the drug from the gel formulation were examined according to the receptor medium, drug concentration, and temperature. The rate of drug release from the gel increased with increasing drug concentration and temperature. The activation energy (Ea) of drug permeation, which was calculated from the slope of log P versus 1/T plots, was 14.41kcal/mol for a 1%(w/w) loading dose. The enhancer, such as saturated, unsaturated fatty acids, pyrrolidones, propylene glycol derivatives, glycerides, and non-ionic surfactants, were incorporated onto the gels to increase the amount of drug permeation into the skin. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the highest level of enhancement. These results show that clotrimazole gels containing polyoxyethylene 2-oleyl ether could be used for the enhanced transdermal delivery of clotrimazole.

Formulation and Evaluation of Transdermal Patch Containing Sibutramine

  • Subedi, Robhash Kusam;Jang, Jun-Ho;Kim, Jae-Il;Park, Young-Joon;Choi, Hoo-Kyun
    • Journal of Pharmaceutical Investigation
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    • v.40 no.1
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    • pp.33-38
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    • 2010
  • Sibutramine is a serotonin-norepinephrine reuptake inhibitor indicated for the management of obesity in conjunction with a reduced calorie diet. The oral administration of sibutramine is followed by its dose-related side effects. In this study, sibutramine was formulated into drug in adhesive (DIA) patches in an attempt to overcome these problems. The effects of different formulation variables including pressure-sensitive adhesive (PSA), loading amount of drug, thickness of matrix and enhancer on the skin permeation of the drug were evaluated using excised hairless mouse skin. In the acrylic adhesive with carboxyl functional group, low release of sibutramine was observed due to the strong interaction between carboxyl group of adhesive and amine group of sibutramine. The acrylic adhesive without functional group provided good adhesion force and allowed high drug loading. Changing drug load as well as thickness of the matrix was found to alter permeation rate. $Crovol^{(R)}$ PK40 and $Crovol^{(R)}$ A40, were found to be effective enhancers for sibutramine. The optimized patch contained 20% sibutramine, and 5% $Crovol^{(R)}$ A40 as permeation enhancer, in $80\;{\mu}m$ thick Duro-$Tak^{(R)}$ 87-9301 matrix.

Release Characteristics to Vitamin $B_{2}$ of Chitosan Ointments In vitro (In vitro에서 키토산 연고의 비타민 $B_{2}$ 방출 특성)

  • Oh, Se-Young;Hwang, Sung-Kwy;Hwang, Yong-Hyun
    • Journal of the Korean Applied Science and Technology
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    • v.17 no.1
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    • pp.43-48
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    • 2000
  • Drug delivery system(DDS) applied to various fields, such as medicine, cosmetics, agriculture and necessities of life. Among these application fields, DDS is often used as the method of drug dosage into the epidermic skin. We investigated characters of transdermal therapeutic system(TTS) and the skin permeability of that with applying DDS. Chitosan was selected as material of TTS. We investigated the permeation of chitosan ointment containing drug in rat skin using horizontal membrane cell model. Permeation properties of materials were investigated for water-soluble drug such as riboflavin in vitro. We used glycerin, PEG 600 and oleic acid as enhancers. Since dermis has more content water(hydration) than the stratum corneum, skin permeation rate at steady state was highly influenced when glycerin was used in water-soluble drug. The permeation rate of content enhancer and drug was found to be faster than that of content water-soluble drug only. These results showed that skin permeation rate of drug across the composite was manly dependent on the property of ointment base and drug. Proper selection of the polymeric materials which resemble and enhance properties of the delivering drug was found to be important in controlling the skin permeation rate.

Preparation and Evaluation of $PGE_1$ Urethral Suppositories ($PGE_1$ 요도좌제의 제조 및 평가)

  • Park Somin;Choi Myeongsin;Han Kyuwon;Kim Kil-Soo
    • YAKHAK HOEJI
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    • v.49 no.4
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    • pp.260-267
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    • 2005
  • [ $PGE_1$ ] is an endogenous substance of potent vasodialator as well as inhibitor of platelet aggregation. It has been used therapeutically in peripheral arterial occlusive disease and impotence. Intracavernous injection of $PGE_1$ for erectile dysfunction has been established for several years as a treatment option for erectile dysfunction of diverse etiologies, but this mode of administration is limited by penile discomfort, pain at the injection site, inconvenience and noncompliance. As the matter of worse, the $\beta-hydroxy$ moiety of $PGE_1$ is extremely susceptible to dehydration in solution to give inactive $PGA_1$ and $PGB_1$. For the improvement of stability, rapid absorption at action site and the convenience of application, $PGE_1$ was formulated as urethral suppositories of three types of formulations, such as PEG, witepsol, and the mixture of PEG and witepsol. The stability test of $PGE_1$ and the release test in urinary suppositories were performed. Futhermore, the effect of enhancers and vehicle composition on the penetration of $PGE_1$ through excised rat skin was evaluated by permeability coefficient and enhancement ratio.

Health Functional Peptides From Milk Products (유제품의 기능성 펩타이드)

  • Lee, Hyong-Joo
    • 한국유가공학회:학술대회논문집
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    • 1998.05a
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    • pp.22-29
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    • 1998
  • Various peptides derived from food are among the most potent physiologically active agents known, and include anticancer peptides, angiotensin converting enzyme(ACE) inhibitor exhibiting antihypertension action, opioid peptides, antithrombotic peptides, hypocholesterolemic peptides, immunomodulators, calcium absorption enhancers, and other peptides. Hydrophobic peptides extracted from a Cheddar-type cheese slurry were fractionated by gel chromatography and repeated HPLC. A peptide fraction from HPLC showed high cytotoxicity on the tumor cell lines such as a human colon carcinoma, and comprised of Tyr, Ser, Leu, Gly, and others. Hypocholesterolemic peptides were isolated from peptic hydrolyzates of casein and soy proteins. Macropeptides of 1,000${\sim}$5,000 dalton were effective on reducing the cholesterol level of mouse serum. Peptides showing high Krigbaum hydrophobicity and ANS surface hydrophobicity resulted in high hypocholesterolemic effect and fecal steroid concentrations. Caseinomacropeptides (CMP) were isolated from whey powder and treated with soluble and immobilized trypsin to obtain antithrombotic peptides. One fraction from the CMP hydrolyzed with immobilized trypsin for 24h exhibited high antithrombotic activity with 52.5% inhibition of platelet aggregation. These results suggested that peptides from various milk products could be utilized as a good bioactive agents for developing health functional foods.

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Mass production and application of activation tagged hairy root lines for functional genomic of secondary metabolism in ginseng

  • Choi, Dong-Woog;Chung, Hwa-Jee;Ko, Suk-Min;In, Dong-Soo;Song, Ji-Sook;Woo, Sung-Sick;Liu, Jang R.
    • Journal of Plant Biotechnology
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    • v.36 no.3
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    • pp.294-300
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    • 2009
  • Activation tagging that uses T-DNA vectors containing multimerized transcriptional enhancers from the cauliflower mosaic virus (CaMV) 35S gene is a powerful tool to determine gene function in plants. This approach has been successfully applied in screening various types of mutations and cloning the corresponding genes. We generated an activation tagged hairy root pool of ginseng (Panax ginseng C.A. Meyer) in an attempt to isolate genes involved in the biosynthetic pathway of ginsenoside (triterpene saponin), which is known as the major active ingredient of the root. Quantitative and qualitative variation of ginsenoside in activation tagged hairy root lines were profiled using LC/MS. Metabolic profiling data enabled selection of a specific hairy root line which accumulated ginsenoside at a higher level than other lines. The relative expression level of several genes of triterpene biosynthetic pathway in the selected hairy root line was determined by real time RT-PCR. Overall results suggest that the activation tagged ginseng hairy root system described in this study would be useful in isolating genes involved in a complex metabolic pathway from genetically intractable plant species by metabolic profiling.

Optimization of Culture Conditions for D-Ribose Production by Transketolase-Deficient Bacillus subtilis JY1

  • Park, Yong-Cheol;Seo, Jin-Ho
    • Journal of Microbiology and Biotechnology
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    • v.14 no.4
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    • pp.665-672
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    • 2004
  • D-Ribose is a five-carbon sugar used for the commercial synthesis of riboflavin, antiviral agents, and flavor enhancers. Batch fermentations with transketolase-deficient B. subtilis JY1 were carried out to optimize the production of D-ribose from xylose. The best results for the fermentation were obtained with a temperature of $37^{\circ}C$ and an initial pH of 7.0. Among various sugars and sugar alcohols tested, glucose and sucrose were found to be the most effective for both cell growth and D-ribose production. The addition of 15 g/l xylose and 15 g/l glucose improved the fermentation performance, presumably due to the adequate supply of ATP in the xylose metabolism from D-xylulose to D-xylulose-5-phosphate. A batch culture in a 3.7-1 jar fermentor with 14.9 g/l xylose and 13.1 g/l glucose resulted in 10.1 g/l D-ribose concentration with a yield of 0.62 g D-ribose/g sugar consumed, and 0.25 g/l-h of productivity. Furthermore, the sugar utilization profile, indicating the simultaneous consumption of xylose and glucose, and respiratory parameters for the glucose and sucrose media suggested that the transketolase-deficient B. subtilis JY1 lost the glucose-specific enzyme II of the phosphoenolpyruvate transferase system.

Transdermal Delivery of Porcine Placenta Extracts using Linolenic Acid-based Emulsion Formulations

  • Kim, Dong-Chan;Noh, Sang-Myoung;Park, Ki-Tae;Kim, Young-Bong;Baek, Kwang-Hyun;Oh, Yu-Kyoung
    • Journal of Pharmaceutical Investigation
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    • v.37 no.5
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    • pp.281-286
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    • 2007
  • For transdermal delivery of porcine placenta extract (PPE), various emulsion formulations were prepared and evaluated. Polysorbate surfactants were used as emulsifiers and various C-18 unsaturated fatty acids as enhancers. The skin permeation of PPE was tested using a cellulose nitrate membrane-loaded Franz cell apparatus. Among emulsifiers, Tween 20 provided higher penetration effect than did Tween 80. Meanwhile, of various fatty acids, linolenic acid (18:3) revealed the highest skin permeation of PPE than the other C-18 unsaturated fatty acids. Stability of PPE emulsions was determined by cycles of freezing and thawing processes. The stability of emulsions depended on the percentage of Tween 20. Minimum 20% of Tween 20 was required to stabilize emulsions at room temperature for several days. Taken together, our results suggest that Tween 20 and linolenic acids might be key components to formulate PPE emulsion to provide the desirable skin permeability and stability.

Use of Monosodium L-Glutamate and Ribonucleotide Seasoning in Korean Processed Foods (국내 가공식품 중 L-글루탐산나트륨과 핵산조미료의 사용 현황)

  • Jung, Jee Eun;Koh, Eunmi
    • Journal of the East Asian Society of Dietary Life
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    • v.26 no.4
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    • pp.308-313
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    • 2016
  • This study aimed to analyze the use of monosodium L-glutamate (MSG) and disodium 5'-ribonucleotide in processed foods manufactured in Korea. Information about MSG and disodium 5'-ribonucleotide was collected from the ingredients claimed on the food packaging. A total of 412 food items were investigated, and 76 items were found to use MSG, disodium 5'-r ibonucleotide, and/or disodium 5'-inosinate. MSG was the most frequently found in 45 items (10.9%), followed by disodium 5'-ribonucleotide in 27 items (6.6%) and disodium 5'-inosinate in three items (0.7%). Of 29 food categories classified by the Korea Food Code, MSG was used most frequently in others, meat products, seasoned food, fish products, and noodles. In comparison, disodium 5'-ribonucleotide was mostly used in noodles. These results indicate that MSG and disodium 5'-ribonucleotide have been used in various Korean processed foods as a flavor enhancers with an umami taste that intensifies the flavor of food.