• Title/Summary/Keyword: Stearate

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Enhanced Dissolution and Permeation of Biphenyl Dimethyl Dicarboxylate Using Solid Dispersions (고체분산체로부터 비페닐디메칠디카르복실레이트의 용출 및 투과 증전)

  • Moon, Jee-Hyun;Chun, In-Koo
    • Journal of Pharmaceutical Investigation
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    • v.29 no.3
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    • pp.227-234
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    • 1999
  • Solid dispersions were prepared to increase the dissolution rate of biphenyl dimethyl dicarboxylate (DDB) using water-soluble carriers such as povidone, copolyvidone, $2-hydroxypropyl-{\beta}-cyclodextrin (HPCD)$, sodium salicylate or sodium benzoate by solvent evaporation method. Solid dispersions were characterized by infrared spectrometry, differential scanning calorimetry (DSC) and powder X-ray diffractometry, dissolution and permeation studies. DDB tablets (7.5 mg) were prepared by compressing the powder mixtures composed of solid dispersions, lactose, com starch, crospovidone and magnesium stearate using a single-punch press. DDB capsules (7.5 mg) were also prepared by filling the mixtures in empty hard gelatin capsules (size No.1). From the DSC and powder x-ray diffractometric studies, it was found that DDB was amorphous in the HPCD or copolyvidone solid dispersions. Dissolution rates after 10 min of DDB alone and solid dispersions (1 : 10) in sodium benzoate, sodium salicylate and copolyvidone were 11.8, 23.5, 22.8 and 82.5%, respectively. Dissolution rates of DDB after 30 min from 1 : 10 and 1 : 20 copolyvidone solid dispersions were 80.5 and 95.0%, respectively. For the DDB tablets prepared using solid dispersions (1 : 20), the initial dissolution rate was dependent on carrier material, and was ranked in order, $Kollidon\;30\;{\ll}$ copolyvidone < HPCD. For the HPCD solid dispersion tablets, dissolution rate reached 97.4% after 15 min, but thereafter slowly decreased to 80.7% after 2 hr due to the precipitation of DDB. However, in the case of copolyvidone solid dispersion tablets, dissolution increased linearly and reached 93.4% after 2 hr. Reducing the volume of test medium from 900 to 300 ml markedly decreased the dissolution rate of the tablets containing 1 : 20 HPCD solid dispersions and 1 : 10 copolyvidone solid dispersion. For 1 : 20 copolyvidone solid dispersion tablets, there was no significant change in dissolution rate up to 1 hr with different volumes of test medium. Preparation of the copolyvidone solid dispersion (1 : 20) in capsules markedly delayed the dissolution (31.2 % after 2hr) due to the limited diffusion within capsules. The permeation rate $(13.4\;g/cm^2\;after\;8\;hr)$ of DDB through rabbit duodenal mucosa from copolyvidone solid dispersion (1 : 10) was markedly enhanced, when compared with drug alone or physical mixtures. From overall findings, DDB formulations containing copolyvidone solid dispersions (1 : 20) could be used to remarkably improve the dissolution rate in dosage form of powders and tablets.

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Validation of HPLC Methods for Ascorbic Acid and Its Derivatives in Foods (식품 중 아스코르빈산 유래 산화방지제의 HPLC 분석법 검증 및 개선)

  • Jeong, Min Kyu;Park, Chan Uk;Park, Min Hee;Yeo, JuDong;Park, SeungKwan;Kim, SoHee;Shin, Tae-Sun;Baek, Hyung Hee;Lee, JaeHwan
    • Food Engineering Progress
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    • v.15 no.1
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    • pp.75-79
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    • 2011
  • Analytical methods for food antioxidants including ascorbic acid, erythorbic acid, ascorbyl palmitate (AP), and ascorbyl stearate (AS), were validated using high performance liquid chromatography. Validation parameters such as linearity, limit of detection (LOD), limit of quantification (LOQ), and recovery were tested using lard and cider as food model systems. Linearity of ascorbic acid and erythorbic acid were both higher than ($R^2$> 0.99), LOD of these compounds were 0.46 and 0.48 ${\mu}g/mL$, respectively and LOQ were 1.39 and 1.45 ${\mu}g/mL$, respectively. The recovery rates of these compounds were 86.35-94.78% and 84.76-95.02%, respectively. However, the concentration of AP and AS decreased in methanol stock solution. Four other solvents including ethanol, acetonitrile, mixture of methanol and acetonitrile, and mixture of ethanol and acetonitrile were tested to increase the stability of AP and AS under room temperature and refrigerated temperature. Ethanol provided better stability of AP and AS under both room and refrigerated temperature. This study can help to accurately analyze the content of ascorbic acid and its derivatives in processed foods.

Development of a novel combination tablet containing silodosin and solifenacin succinate for the treatment of urination disorder (배뇨 장애 치료를 위한 실로도신과 솔리페나신 숙신산염 함유한 새로운 복합 정제 개발)

  • Choi, Hyung-Joo;Lee, Jeong-Gyun;Kim, Kyeong Soo
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.22 no.3
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    • pp.323-332
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    • 2021
  • This study was undertaken to develop a new combination tablet containing silodosin and solifenacin succinate for treating urination disorders, for which a simultaneous analytical method of silodosin and solifenacin succinate was established. The aqueous solubility of silodosin and solifenacin succinate was determined to be higher than 1 mg/ml in various buffers, and dissolution of the silodosin and solifenacin succinate commercial products was accomplished within 30 minutes. The drug-excipients compatibility test was subsequently evaluated using differential scanning calorimetry. Excipients without compatibility were selected, and various combination formulations were prepared applying the wet granulation method. Of these, the formulation comprising silodosin, solifenacin succinate, lactose hydrate, MCC PH101, sodium lauryl sulfate (SLS), Povidone K30, crospovidone and magnesium stearate, having a weight ratio of 8/10/56/112/2/6/6/2, respectively, showed equivalence comparative to the dissolution achieved with the commercial products of silodosin (Thrupas tab) and solifenacin succinate (Vesicare tab). Thus, we propose that compared to the currently available commercial products, this novel combination tablet containing silodosin and solifenacin succinate is an effective alternative for the treatment of urination disorders.

Evaluation on Pharmacological Effects and Compound Contents of Hwangryunhaedok-tang formulation for Tablet (황련해독탕을 함유하는 정제 개발과 성분함량 및 약리효과 평가)

  • Lee, Ji-Beom;Choi, Hye-Min;Kim, Jong-Bum;Kim, Jung-Ok;Moon, Sung-Ok;Lee, Hwa-Dong
    • The Korea Journal of Herbology
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    • v.33 no.2
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    • pp.9-18
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    • 2018
  • Objectives : Hwangryunhaedok-tang (HRHDT) is one of the well-known prescription herbal drugs of Korean herbal medicine, which has been widely used for the treatment of various bacterial and inflammatory diseases. This study was conducted in order to develop the tablet formulations of HRHDT and compare its efficacy with the other commercial formulations. Methods : Corresponding herbal medicines comprising of HRHDT were extracted with water for 3 hr at $95{\sim}100^{\circ}C$ and then vacuum dried. Subsequently, some pharmaceutical excipients such as microcrystalline cellulose, croscarmellose sodium, magnesium stearate, etc were used to prepare the HRHDT tablets. The contents with characterizing components of HRHDT tablet was compared with the HRHDT decoction. The contents of characterizing components were analyzed with HPLC. Furthermore, we investigated the anti-inflammatory and anti-oxidative abilities of two different commercial HRHDT granules (HJP-1 and HJP-2) and were compared with that of the formulated HRHDT tablets. The anti-oxidant properties of HRHDR were studied using the 1,1-diphenyl-2-picryhydrazyl (DPPH) radical, contents of total flavonoid and polyphenol. In addition, based on this result the anti-inflammatory effects have verified by mechanism from LPS- treated Raw264.7 macrophages. Results : The results demonstrated that HRHDT tablets showed more anti-inflammatory and anti-oxidative effects than HJP-1, HJP-2. Moreover, it showed more superior effects in terms of dose, usability and stability than the granules. Conclusion : Hence, we concluded that in order to improve the quality and efficacy of the Korean herbal medicine, it is necessary to develop appropriate methods and establish standardized techniques for the development of good formulations.

Comparison of Standard and Lend Limit Test of Various Institutes on Lead Limit of Synthetic and Natural Food Additives (합성 및 천연 식품첨가물의 납함량에 대한 여러 기관의 규격기준 및 납시험법 비교)

  • Shin Dong-Hwa;Kim Yong-Suk;Jeong Do-Yeong;Lee Young-Hwan;Bang Jeong-Ho;Om Ae-Son;Shin Jae-Wook;Lee Tal-Soo;Jang Young-Mi;Hong Ki-Hyoung;Park Sung-Kwan;Park Sung-Kug;Kwon Yong-Kwan
    • Journal of Food Hygiene and Safety
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    • v.21 no.2
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    • pp.82-91
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    • 2006
  • Standard and lead limit test in general test method of Korea, Japan, Joint FAO/WHO Expert Committee of Food Additives (JECFA), USA, and EU on synthetic and natural food additives were compared. There were found that the general test methods in 'Korea Food Additives Code' were different from standards of various institutes on lead limit test. For the lead limit test of food additives, Korea used dithizone method, Japan used atomic absorption spectrophotometry, and USA used dithizone method, flame atomic absorption spectrophotometric method, atomic absorption spectrophotometric graphite furnace method, and APDC extraction method. In addition, JECFA and EU used dithizone method and atomic absorption spectrophotometric method. The dithizone methods of Korea, USA, and JECFA were nearly identical. In the case of USA, JECFA, and EU, the analytical methods for lead limit test were shown in individual monograph. Lead limit test against 13 synthetic, such as magnesium stearate and L-cystine, and 12 natural, such as gua gum and diatomaceous earth, food additives distributed in Korea were performed by the analytical method of each institute. Although all institutes use various methods for analysis of lead, contents of lead in food additives tested fell into the standard of each institute.

Relationship between Monounsaturated Fatty Acid Composition and Stearoyl-CoA Desaturase mRNA Level in Hanwoo Liver and Loin Muscle (한우 간 및 등심 조직에서 불포화지방산의 조성비율과 Stearoyl-CoA Desaturase mRNA의 발현 양상)

  • Lee, S.H.;Yoon, D.H.;Hwang, S.H.;Cheong, E.Y.;Kim, O.H.;Lee, C.S.
    • Journal of Animal Science and Technology
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    • v.46 no.1
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    • pp.7-14
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    • 2004
  • The Stearoyl-CoA Desaturase(SCD) is a key enzyme, which converting palmitic acid(16:0) and stearic acid (18:0) to pahnitoleic acid(16:1) and oleic acid(l8:1), respectively. The concentration of oleic acid(18:1) in meat of beef cattle could influence both palatability and perception of meat. This experiment has conducted to determine relationship between the compositions of monounsaturated fatty acids and the SCD mRNA level in bovine liver and loin muscle tissue. The compositions of palmitoleic acid(16:1) and oleic acid(18:1) in loin muscle were 5% and 46% of total lipid and in liver were 2% and 20% of total lipid, respectively. On the other hand, the compositions of palmitic acid(16:0) and stearic acid(18:0) in loin muscle were 25% and 45% of total lipid and in liver were 14% and 43% of total lipid, respectively. The ratio of monounsaturated to saturated fatty acids(the desaturation index) was used as a measure of SCD activity in tissues. The average desaturation index in loin muscle was higher about 3.6-fold than that in liver. The desaturation index of oleate/stearate and palmitoleatelpalmitate in loin muscle were higher 8-fold and 1.8-fold than those in liver, respectively, showing that the substrate specificity of SCD enzyme was very different between liver and muscle tissues. To determine whether the composition of monounsaturated fatty acids in liver and muscle are dependent on SCD expression, SCD mRNA level was examined by RT-PCR analysis. The SCD mRNA level in loin muscle was higher about 3-fold than that in liver. Thus, the quantitative relationship between the desaturation index of fatty acid and SCD mRNA was observed in liver and muscle. The difference in the compositions of monounsaturated fatty acids between bovine liver and muscle tissues may be due to different level of Stearoyl-CoA Desaturase mRNA.

A Study on the Moisturizing Effect and Preparation of Liquid Crystal Structures Using Sucrose Distearate Emulsifier (슈크로오스디스테아레이트를 사용한 액정구조의 생성과 보습효과에 관한 연구)

  • Kwak, Myeong-Heon;Kim, In-Young;Lee, Hwan-Myung;Park, Joo-Hoon
    • Journal of the Korean Applied Science and Technology
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    • v.33 no.1
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    • pp.1-12
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    • 2016
  • This study is to make the liquid crystalline structure using sucrose distearate (Sucro-DS) emulsifier to create the hydrophilic type oil-in-water (O/W) emulsion, the droplets of the emulsion having a structure of a multi-lamellar structure. We have studied the physicochemical properties of Sucro-DS using those techniques. And it has been studied in the emulsion performance. In order to form the liquid crystalline structure applying 3 wt% of Sucro-DS, 5 wt% of glycerin, 5 wt% of squalane, 5 wt% of capric/caprylic triglyceride, 3wt% of cetostearyl alcohol, 1wt% of glyceryl mono-stearate, 78 wt% of pure water in mixture having the lamellar structure of stable multi-layer system was found to formed. By applying them, they were described how to create an unstable active material encapsulated cream. Further, the moisturizing cream was studied using this technique. It reported the results to the skin improvement effect by the human clinical trials. The pH range to produce a stable liquid crystal phase using a Sucro-DS was maintained in 5.2~7.5. In order to increase the stability of the liquid crystal, it was when behenyl alcohol containing 3 wt%, the hardness at this time was 13 kg/mm,min. Viscosity of the same amount was 25,000mPas/min. After a test for the effects of the emulsions, the concentration of 6 wt% Sucro-DS is that was appropriate, the particle size of the liquid crystal was 4~6mm. It was observed through a microscope analysis, reliability of the liquid crystal changes for 3 months was found to get stable at each $4^{\circ}C$, $25^{\circ}C$ and $45^{\circ}C$. In clinical trial test, before applying a moisturizing effect it was $13.4{\pm}7%$. Moisturizing cream liquid crystal was not formed in $14.5{\pm}5%$. Therefore, applying than ever before could see the moisture about 8.2% was improved. On the other hand, it was the moisturizing effect of the liquid cream is $19.2{\pm}7%$. The results showed that 43.3% improvement than that previously used. Applications fields, Sucro-DS emulsifier used liquid cream, lotion, eye cream and a variety of formulations can be developed, as well as the cosmetics industry is expected to be wide fields in the application of the external preparation for skin emulsion technology in the pharmaceutical industry and pharmaceutical industry.

Effects of Rye Silage on Growth Performance, Blood Characteristics, and Carcass Quality in Finishing Pigs (호맥 사일리지의 급여기간이 비육돈의 생산성, 혈액 성상 및 도체특성에 미치는 영향)

  • Shin, Seung-Oh;Han, Young-Keun;Cho, Jin-Ho;Kim, Hae-Jin;Chen, Ying-Jie;Yoo, Jong-Sang;Whang, Kwang-Youn;Kim, Jung-Woo;Kim, In-Ho
    • Food Science of Animal Resources
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    • v.27 no.4
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    • pp.392-400
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    • 2007
  • This experiment was conducted to evaluate effects of various periods of rye silage feeding on the growth performance, blood characteristics, and carcass quality of finishing pigs. A total of sixteen [($Landrace{\times}Yorkshire{\times}Duroc$)] pigs (90.26 kg in average initial body weight) were tested in individual cages for a 30 day period. Dietary treatments included 1) CON (basal diet), 2) S10 (basal diet for 20 days and 3% rye silage for 10 days) 3) S20 (basal diet for 10 days and 3% rye silage for 20 days) and 4) S30 (3% rye silage for 30 days). There were no significant differences in the ADG and gain/feed ratio among the treatments(p>0.05), however the ADFI was higher in pigs fed the CON diet than with pigs fed diets with rye silage (p<0.05). The DM digestibility was higher with the S20 diet than with the S30 diet (p<0.05). With regard to blood characteristics, pigs fed rye silage had a significantly reduced cortisol concentration compared to pigs fed the CON diet (p<0.05). The backfat thickness was higher with the CON diet than with the S20 or S30 diets (p<0.05). Regarding the fatty acid contents of the leans, the C18:0 and total SFA were significantly higher with the CON diet than with the other diets (p<0.05). However, the C18:1n9, total MUFA and UFA/SFA levels were significantly lower with the CON diet than the other diets (p<0.05). Regarding the fatty acid contents of fat, the levels of C18:1n9 and MUFA were similar with the S20 and S30 diets, however, these levels were higher than with the CON or S10 diets (p<0.05). In conclusion, feed intake and DM digestibility were affected by rye silage, and the cortisol concentration, backfat thickness and fatty acid composition of pork were positively affected by feeding pigs rye silage.