• Title/Summary/Keyword: pharmaceutical ingredient

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Therapeutic Duplication Criteria Development of Respiratory System Drugs (호흡기계 작용 약물의 치료군 중복처방 평가기준 개발)

  • Choi, Kyung-Eob;Sohn, Hyun-Soon;Kim, Nam-Hyo;Shin, Hyun-Taek;Lee, Young-Sook
    • YAKHAK HOEJI
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    • v.56 no.2
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    • pp.126-135
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    • 2012
  • Purpose: To develop therapeutic duplication criteria for the drugs used for respiratory diseases. Method: Therapeutic duplication was defined as "more than 2 drug ingredient-usage in which each has the same therapeutic effect and combination therapy does not confer additional therapeutic benefit". Respiratory system drugs approved in Korea were examined for the study. The WHO's Anatomical Therapeutic Chemical Classification System was used for grouping of the corresponding drug ingredients. The principles and recommendations on combination usage or multiple drug regimens were reviewed by using the clinical practice guidelines, textbooks, product labelings, and clinical articles. Clinical expert group consultation was performed and expert opinions were incorporated into the final criteria. Results: Nine hundred sixty two drug products with Korean Food and Drug Administration classification codes of 141, 149, 222, and 229 were evaluated, of which 87 active ingredients were composed. The drug ingredients were classified into 12 groups (antihistamines, oral nasal decongestants, leukotriene receptor antagonists, inhaled anticholinergics, inhaled corticosteroids, oral ${\beta}2$-agonists, long-acting ${\beta}2$-agonists, short-acting ${\beta}2$-agonists, xanthines, antiallergics, mucolytics and cough suppressants). The use of more than 2 drug ingredients including the same group was therapeutic duplication, and thus combination should be recommended not to be used. Conclusion: Twelve drug groups were identified as therapeutic duplication criteria. Combination therapy within each group should not be used otherwise therapeutic benefits outweigh potential risks.

Biosynthesis of ceramide by deletion mutant of Saccharomyces cerevisiae (Saccharomyces cerevisiae deletion mutant의 세라마이드 생합성)

  • Kim, Se-Kyung;Noh, Yong-Ho;Yun, Hyun-Shik
    • KSBB Journal
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    • v.24 no.1
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    • pp.25-29
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    • 2009
  • Ceramide is important not only for the maintenance of the barrier function of the skin but also for the water-binding capacity of the stratum corneum. Though the effectiveness of ceramide is not understood fully, ceramide has become a widely used ingredient in cosmetic and pharmaceutical industries. However, ceramide production from Saccharomyces cerevisiae has not been widely studied and the quantity are very low. Gene deletion in the cell is used frequently to investigate the function of gene and verification research of drug target. Specially, deletion mutant library is useful for a large amount functional analysis of gene. In this study, deletion mutants of genes on the metabolic pathway of ceramide synthesis in S. cerevisiae were grown in a batch culture and the cellular content of ceramide was measured. The ceramide content was highest in ${\triangle}$ydc1 mutant and 6 mg ceramide/g cell was obtained.

Synthesis and Properties of 5-Aminosalicyl-taurine as a Colon-specific Prodrug of 5-Aminosalicylic Acid

  • Jung, Yun-Jin;Kim, Hak-Hyun;Kong, Hye-Sik;Kim, Young-Mi
    • Archives of Pharmacal Research
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    • v.26 no.4
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    • pp.264-269
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    • 2003
  • 5-Aminosalicylic acid (5-ASA) is an active ingredient of therapeutic agents used for Crohn s disease and ulcerative colitis. Because it is absorbed rapidly and extensively in the upper intestine, delivery of the agent specifically to the colon is necessary. We selected taurine as a colon-specific promoiety and designed 5-aminosalicyltaurine (5-ASA-Tau) as a new colon-specific prodrug of 5-aminosalicylic acid (5-ASA). It was expected that introduction of taurine would restrict the absorption of the prodrug and show additive effect to the anti-inflammatory action of 5-ASA after hydrolysis. 5-ASA-Tau was prepared in good yield by a simple synthetic route. The apparent partition coefficient of 5-ASA-Tau in 1-octanol/pH 6.8 phosphate buffer or $CHCl_3$/pH 6.8 phosphate buffer was 0.10 or 0.18, respectively, at $37^{\circ}C$. To determine the chemical and biochemical stability in the upper intestinal environment, 5-ASA-Tau was incubated in pH 1.2 and 6.8 buffer solutions, and with the homogenates of tissue and contents of stomach or small intestine of rats at $37^{\circ}C$. 5-ASA was not detected from any of the incubation medium with no change in the concentration of 5-ASA-Tau. On incubation of 5-ASA-Tau with the cecal and colonic contents of rats, the fraction of the dose released as 5-ASA was 45% and 20%, respectively, in 8 h. Considering low partition coefficient and stability in the upper intestine, 5-ASA-Tau might be nonabsorbable and stable in the upper intestine. After oral administration, it would be delivered to the colon in intact form and release 5-ASA and taurine. These results suggested 5-ASA-Tau as a promising colon-specific prodrug of 5-ASA.

Antioxidant, Anti-acetylcholinesterase and Composition of Biochemical Components of Russian Deer Velvet Antler Extracts

  • Je, Jae-Young;Park, Pyo-Jam;Lim, Dong-Hwan;Jeon, Byong-Tae;Kho, Kang-Hee;Ahn, Chang-Bum
    • Food Science of Animal Resources
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    • v.31 no.3
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    • pp.349-355
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    • 2011
  • Russian deer velvet antlers were divided into three parts and subjected to a extraction process using hot water at 100, 110, and $120^{\circ}C$ or an extraction with 70% ethanol. Each extract was analyzed for its biochemical components, including uronic acid, sulfated-glycosaminoglycans (sulfated-GAGs), and sialic acid, and the antioxidant and anti-acetylcholinesterase activities were investigated. Different levels of uronic acid and sulfated-GAGs were observed in the extracts according to the water temperature used for the extraction, and contents decreased with increasing extraction temperature. The upper layer of each extract showed high amounts of uronic acid and sulfated-GAGs, followed by the middle and base layers. Ethanol extraction was more effective for recovering uronic acid than sulfated-GAGs. Sialic acid content was the highest in the $110^{\circ}C$ extracts but was not observed in the ethanol extracts. Velvet antler extracts showed strong antioxidant activities against DPPH and hydrogen peroxide as well as strong reducing power in a dose-dependent manner. However, the antioxidant activities were different in each layer and according to the extraction method. Additionally, velvet antler extracts exhibited inhibitory activity against acetylcholinesterase, which is associated with Alzheimer's disease, in a dose-dependent manner. These results suggest that velvet antler extracts are useful as a functional food ingredient and/or a pharmaceutical.

Solubillzation and Extraction Of Antioxidant Astaxanthin by Micelle Formation from Phaffia rhodozyma Cell Homogenate (Phaffia rhodozyma 세포파쇄액으로부터 항산화제 Astaxanthin의 미셀 형성을 통한 가용화 및 추출)

  • Kim, Young-Beom;Ryu, Kang;Lim, Gio-Bin;Lee, Eun-Kyu
    • KSBB Journal
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    • v.17 no.2
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    • pp.176-181
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    • 2002
  • Astaxanthin (3,3'-dihydroxy-${\beta}$, ${\beta}$-carotene-4-4'-dione), a natural pigment of pink to red color, is widely distributed in nature particularly in the skin layer of salmonoids and the crust of shrimp, lobster, etc. Recently, it was produced from the yeast culture of Phaffia rhodozyma. Because of its high thermal stability and antioxidant functionality, its applications can be extended into food, cosmetics, and pharmaceutical ingredient beyond the traditional feed additive. Because of its very high lipophilicity, astaxanthin has been extracted traditionally by strong organic solvents such as chloroform, petroleum ether, acetone, etc. In this study, we developed a surfactant-based solubillization system for astaxanthin, and used it to extract astaxanthin from disrupted yeast cells. Among Tween 20, Triton X-100 and SDS, Tween 20 was identified as the most suitable surfactant in terms of extraction capacity and safety. The ethylene oxide group of Tween 20 was identified as the most significant factor to increase the HLB value that determined the extraction capacity. The effects of micelle formation condition, such as the molar ratio of astaxanthin and Tween 20, pH, and ionic strength were also investigated. pH and ionic strength showed no significant effects. The optimal molar ratio between astaxanthin and Tween 20 was 1 : 12. Antioxidant activity of astaxanthin was higher than ${\beta}$-carotene and ${\alpha}$-tocopherol. Astaxanthin in the crude extract from the yeast cell was more resistant to air and/or light degradation than pure astaxanthin, probably because of the presence of other carotenoids and lipids.

Inhibition of Lipid Accumulation in 3T3-L1 Adipocytes by Different Enzymatic Hydrolysates of Dried Red Sea Cucumber Stichopus japonicus (건조 방법에 따른 홍해삼(Stipchopus japonicus) 효소 가수분해물의 지방 축적 억제 효과)

  • Kim, Seo-Young;Oh, Jae-Young;Kim, Eun-A;Heo, Soo-Jin;Kim, Kil-Nam;Jeon, You-Jin
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.53 no.5
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    • pp.707-716
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    • 2020
  • Red sea cucumber Stichopus japonicus, was dried using three methods-far-infrared ray, vacuum, and freeze drying and then enzymatically hydrolyzed using nine proteases: Alcalase, Flavourzyme, Kojizyme, Neutrase, Protamex, trypsin, α-chymotrypsin, and papain. In addition, the potential ability of hydrolysates to inhibit lipid accumulation in 3T3-L1 adipocytes was evaluated. The yield of hydrolysates from red sea cucumbers dried using each method was higher than that of the distilled water extract, and protein contents were either similar or higher. The hydrolysates that exhibited inhibitory effects on lipid accumulation, as demonstrated via Oil red O staining, were those obtained by far-infrared ray drying coupled with Alcalase, Flavourzyme, Kojizyme, or Neutrase treatment. In addition to the advantages of far-infrared drying and the characteristics of Flavourzyme, the Flavourzyme hydrolysate of far-infrared-dried red sea cucumber showed the highest inhibitory effect on lipid accumulation. In addition, this hydrolysate significantly decreased the expression of the protein factor fatty acid-binding protein 4, which is related to the late differentiation of 3T3-L1 adipocytes. Taken together, these results suggest that Flavourzyme hydrolysates from farinfrared-dried red sea cucumber may be used as a functional food and/or a pharmaceutical ingredient for the inhibition of lipid accumulation.

In vitro and In vivo Activities Studies of Chois Mastic Using Self-microemulsifying Drug Delivery System (SMEDDS) against Helicobactor pylori (자가미세유화시스템을 이용한 매스틱의 헬리코박터파일로리 대한 In vitro 및 In vivo 활성 연구)

  • Kim, Su-Ji;Jeong, Sang-Young;Gil, Young-Sig;Shin, Byung-Cheol;Hwang, Sung-Joo;Cho, Sun-Hang
    • YAKHAK HOEJI
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    • v.55 no.1
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    • pp.1-10
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    • 2011
  • Mastic is a bleed resin formed in pistacia lentiscus tree extract form the anacatdiaceae family. Mastic is used as a food ingredient in the Mediteraanean resin, and has been used by local inhabitants as a traditional medicine for relief of upper abdominal discomfort, dyspepsiaand peptic ulcer. Clinically, mastic has been effective in the treatment of benign gastric and duodenal, ulcers, giving symptomatic relief and endoscopically proven healing. In this study, to enhance activiteies of poorly water soluble Mastic with oils, surfactants and cosurfactants and then the mixure was microemulsified in aqueous media under condition of gentle agitation and digestive motility that would be encountered in the gastrointestinal tract. Formulation development and screening were based on phase diagrams and characteristics of resultant microemulsion. For optimum mastic formulation, microemulsions with various ratio (w/w%) of mastics, oils, surfactants and cosurfactants were prepared and their solubility was evaluated by monitoring particles size in their buffer through visual asessment and electrophoretic light scattering spectrophotomerter (ELS). In vitro activity of self microemulsified mastic (SME mastic) was determined by minimum ingibition concentration (MIC) test against a panel of Helicobacter pylori (H. pylori) clinical strains. Additionally, in vivo activity of SME masitc was investigated us mouse infected by CH275 of H. pylori. The mean diameter of SME mastic was less then 100 nm in water and SME mastic was showed similar antiboisis effect compared to tometronidazole, clarithromycin and omeproazole. Consequently, SME mastic would be effective system to exterminate H. pylori. If mastic were dose with combined treatment, mastic might augur well for effect of H. pylori eradication as good remedy.

The effect of pretreated Lithospermum erythrorhizon derived-naphthoquinone on anxiety, depression in mice (지치 유래 naphthoquinone을 전처치한 생쥐에서 우울 및 불안 조절 효과)

  • Je, Hyun Dong;Min, Young Sil
    • Journal of Convergence for Information Technology
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    • v.10 no.7
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    • pp.116-121
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    • 2020
  • This study was undertaken to investigate the influence and related mechanisms that have yet to be clearly demonstrated of Lithospermum erythrorhizon derived-naphthoquinone (shikonin) on the anxiety, insomnia, depression in rats. We hypothesized that naphthoquinone, the primary ingredient of Lithospermum erythrorhizon, plays a role in the modulation of insomnia evoked by stress, depression evoked by forced swimming or anxiety evoked by elevated plus maze. Male ICR (Institute of Cancer Research) mice were used and the immobility or swimming time, the duration of sleep, the duration and entry frequency into open arms were measured and recorded. The administration of naphthoquinone (10, 30 and 100 mg/kg) potentiated barbiturate-induced sleep suggesting the activation of GABAA receptor. It also potentiated the time spent in open arms of the maze and decreased the immobility time in forced swimming. In conclusion, naphthoquinone has anxiolytic, hypnotic and anti-depressant properties and is a potential therapeutic for anxiety, insomnia and depression.

Anti-oxidant and Anti-aging Activities of Sericinjam Gland Hydrolysate Extract in Human Dermal Fibroblasts (사람 섬유아세포에서 세리신잠 실샘가수분해물(Sericinjam Gland Hydrolysate)의 항산화 및 항노화 효과)

  • Cheon, Yuri;Hwang, Jung Wook;Lee, Heui Sam;Yun, Seiyoung;Choi, Yong-Soo;Kang, Sangjin
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.39 no.1
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    • pp.9-17
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    • 2013
  • We studied the anti-oxidant and anti-aging activities of Sericinjam Gland Hydrolysate (SJGH) in the human dermal fibroblasts. SJGH effectively defended cell death and ROS generation under high H2O2 in human dermal fibroblasts. Moreover SJGH reduced the expression of SA-${\beta}$-Gal and MMP-1 under low concentration of $H_2O_2$ whereas biosynthesis of procollagen-I was increased. This results demonstrate the anti-oxidant and anti-aging activities of SJGH. SJGH could be a good candidate for anti-aging cosmetics ingredient.

New Anti-Inflammatory Formulation Containing Synurus deltoides Extract

  • Choi, Yong-Hwan;Son, Kun-Ho;Chang, Hyeun-Wook;Bae, Ki-Hwan;Kang, Sam-Sik;Kim, Hyun-Pyo
    • Archives of Pharmacal Research
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    • v.28 no.7
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    • pp.848-853
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    • 2005
  • Synurus deltoides was previously found to possess significant anti-inflammatory activity especially against chronic inflammation, and strong analgesic activity in vivo. In this study, new anti-inflammatory formulation containing S. deltoides extract as a major ingredient was prepared and in vivo activity was evaluated. The plausible action mechanism was also investigated. The new formulation (SAG) contains 1 part of S. deltoides extract, 0.9 part of Angelica gigas extract and 0.9 part of glucosamine sulfate (w/w). SAG inhibited dose-dependently edematic response of arachidonic acid (AA)- and 12-O-tetradecanoyl 13-acetate (TPA)-induced ear edema in mice, which is an animal model of acute inflammation. SAG showed 44.1 % inhibition of AA-induced ear edema at an oral dose of 50 mg/kg. In an animal model of chronic inflammation, SAG clearly reduced the edematic response of 7 -day model of multiple treatment of TPA (38.1 % inhibition at 200 mg/kg/day). Furthermore, SAG (50-800 mg/kg/day) as well as S. deltoides extract (285 mg/kg/day) significantly inhibited prostaglandin $E_2$ production from the skin lesion of the animals of 7-day model. These results were well correlated with in vitro finding that SAG as well as S. deltoides extract reduced cyclooxygenase (COX)-1- and COX-2-induced prostanoid production, measured in mouse bone marrow-derived mast cells. Therefore, these results suggest that SAG possesses anti-inflammatory activity in vivo against acute as well as chronic inflammatory animal models at least in part by inhibition of prostaglandin production through COX-1/COX-2 inhibition. And COX inhibition of SAG is possibly contributed by S. deltoides extract among the ingredients. Although the anti-inflammatory potencies of SAG were less than those of currently used anti-inflammatory drugs, this formulation may have beneficial effect on inflammatory disorders as a neutraceutical.