• Title/Summary/Keyword: Lovastatin acid

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Preparation and release characteristics of PVP-based solid dispersion capsules containing solubilizers

  • Cao, Qing-Ri;Kim, Tae-Wan;Choi, Choon-Young;Lee, Beom-Jin
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.412.1-412.1
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    • 2002
  • Purpose. To prepare PVP-based solid dispersions containing lovastatin (LOS) and solubilizers (sodium lauryl sulfate. Tween80. oleic acid) to enhance dissolution of practically insoluble LOS. Methods. Solid dispersions containing LOS were prepared by dissolving two different organic solvent systems (acetone/ethanol or acetonitrile/ethanol). Results. The stickiness and flowability of solid dispersion powders were dependent on the composition and ratio of the solubilizers. (omitted)

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Quantitation of Mevinolinic Acid in Human Plasma by HPLC (고속액체크로마토그래피를 이용한 사람 혈장중 메비놀린 산의 정량)

  • Oh, Han-Suk;Park, Dong-Young;Seo, Sung-Hoon;Kim, Young-Gwan;Hong, Seon-Pyo;Choi, Young-Wook;Lee, Kyung-Tae
    • Journal of Pharmaceutical Investigation
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    • v.30 no.4
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    • pp.279-282
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    • 2000
  • Simple and precise high-performance liquid chromatographic (HPLC) assay was developed and validated for the determination of a HMG-CoA reductase inhibitor, $lovastatin^{TM}$ and its active metabolite (mevinolinic acid) in human plasma. The method involved solid phase extraction of mevinolinic acid and internal standard using Sep-Pak Cartridge. Samples were analyzed by reversed-phase HPLC using $Capcell-Pak\;C_{18}$ column with ultraviolet detection at 238 nm. The quantitation limit of mevinolinic acid was 2 ng/ml and the calibration curve was linear over the range of 2-50 ng/ml $(r^2>0.999)$ with human plasma. The analyses of quality control samples indicated that the normal values could be predicted with an accuracy >97%. The intra- and inter-day coefficients of variation for the analyses were <10%. The average recoveries were similar (79%) for mevinolinic acid and methylmevinolinic acid. The method described has been successfully applied to the quantification of mevinolinic acid in about 1,000 human plasma samples over six-month period.

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Improved mevinolic acid (MA) production by the immobilized cells, and the establishment of on-line measurement system for fermentation parameters using vent gas analyzer

  • Song, Seong-Gi;Kim, Gyeong-Hui;Kim, Myeong-Jin;Lee, Sang-Jong;Jang, Yong-Geun;Jeong, Yeon-Ho;Jeong, Yong-Seop;Jeon, Gye-Taek
    • 한국생물공학회:학술대회논문집
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    • 2003.04a
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    • pp.223-227
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    • 2003
  • Mevinolic acid (MA), a secondary metabolite produced by a filamentous fungus Aspergillus terreus, is acidic form of lovastatin which has been identified as a powerful cholesterol-lowering agent in humans. When immobilized cell culture was performed, MA production was about 5.3-fold higher than the parallel suspended cell culture. Although the immobilized cells proliferated slowly during exponential in comparison with the suspended cells, oxygen uptake rate and oxygen mass transfer coefficient of the immobilized cell culture were about 1.3- and 2.5- fold higher respectively than those of the parallel suspended cell culture. From these results, it was concluded that MA biosynthesis was closely dependent on the cell growth rate, morphology and oxygen availability.

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Preparation and Dissolution of Polyvinylpyrrolidone(PVP)-Based Solid Dispersion Systems Containing Solubilizers (가용화 조성물을 함유한 PVP형 고체분산체의 제조 및 특성)

  • Cao, Qing-Ri;Kim, Tae-Wan;Choi, Choon-Young;Kwon, Kyoung-Ae;Lee, Beom-Jin
    • Journal of Pharmaceutical Investigation
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    • v.33 no.1
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    • pp.7-14
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    • 2003
  • The PVP-based solid dispersion systems (SDs) containing lovastatin (LOS) and solubilizers (sodium lauryl sulfate, tween 80 and oleic acid) were prepared to enhance dissolution rate of practically water insoluble LOS using solvent evaporation method. Two different organic cosolvents either acetone/ethanol or acetonitrile/ethanol were used for the preparation of SDs. The LOS contents were highly decreased when acetone/ethanol cosolvents were used. The decrease of LOS contents was not caused by acetonitrile or acetone, based on HPLC data. The surface morphology as investigated by scanning electron microscope (SEM) and angle of repose as an index of flowability of SDs were highly dependent on the type and amount of solubilizers used. Based on differential scanning calorimetry (DSC) and X-ray powder diffraction data, the SDs made crystalline LOS into amorphous structure or partially eutectic mixtures. The simultaneous use of the solubilizers in SDs was also useful to increase dissolution rate of LOS in gastric or intestinal fluid. The SDs containing solubilizers reached 76% and 60% in gastric and intestinal fluid, respectively but the commercial tablet gave only less than 4%. These solubilizers in SDs could be also applicable for enhancing dissolution and bioavailability of poorly water-soluble drugs.

The Ginsenoside-Rb2 lowers cholesterol and triacylglycerol levels in 3T3-L1 adipocytes cultured under high cholesterol or fatty acids conditions

  • Kim, Eun-Ju;Lee, Hyun-Il;Chung, Kyung-Jin;Noh, Yun-Hee;Ro, Young-Tae;Koo, Ja-Hyun
    • BMB Reports
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    • v.42 no.4
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    • pp.194-199
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    • 2009
  • The effects of the ginsenoside Rb2 (Rb2) on lipid metabolism were characterized in 3T3-L1 adipocytes to evaluate their utility for treating obesity. While the amounts of total cholesterol and triacylglycerol (TAG) were markedly increased in the adipocytes treated with high amounts of cholesterol and fetal bovine serum (FBS), the test groups treated with Rb2 showed levels that were close to normal. The effect of Rb2 on these cells was comparable to that of lovastatin. Rb2 enhanced the expression of the sterol regulated element binding protein (SREBP) mRNA whereas treatment with cholesterol and FBS led to a reduction in the abundance of this transcript. The activity of fatty acid synthetase (FAS) was lower in the cholesterol group compared to the Rb2 treatment group suggesting that the observed decrease in cholesterol levels and activated SREBP was mediated by Rb2. Treatment with Rb2 also resulted in a decrease in TAG levels in adipocytes cultured under high fatty acid conditions. This effect was mediated by stimulating the expression of SREBP and Leptin mRNA, suggesting that Rb2 might be a valuable component capable of lowering the levels of lipids.

Effect of Yacon on Platelet Function in Hypercholesterolemic Rabbits

  • Lim, Yong;Son, Dong-Ju;Kim, Yun-Bae;Hwang, Bang-Yeon;Yun, Yeo-Pyo;Hwang, Seock-Yeon
    • Biomolecules & Therapeutics
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    • v.19 no.4
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    • pp.472-476
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    • 2011
  • Hypercholesterolemia indirectly increases the risk of arterial and venous thrombosis by enhancing the ability of platelets to aggregate. Yacon (Smallanthus sonchifolius) is composed of fructooligosaccharides, proteins, minerals and phenolic compounds, and has potential benefits for the management of diabetes. This study investigated whether the consumption of yacon in the diet inhibits platelet aggregation under hypercholesterolemic conditions. Male New Zealand white rabbits were fed one of five dietary interventions: a normal control diet, 0.5% cholesterol diet, 0.5% cholesterol diet+a low dose of yacon (0.5 g/kg body weight given orally each day), 0.5% cholesterol diet+a high dose of yacon (2.5 g/kg body weight given orally each day), or a 0.5% cholesterol diet+lovastatin (2 mg/kg body weight given orally each day). After 8 weeks, blood was collected to measure the amount of collagen- and thrombin-induced platelets present. Yacon inhibited the platelet aggregation induced by low doses of agonists (0.5 ${\mu}g/mL$ collagen and 0.02 units/ml thrombin) in a concentration-dependent manner. In addition, yacon concentration-dependently inhibited collagen-induced arachidonic acid liberation. Moreover, n-hexane, chloroform and ethyl acetate fractions showed a marked and selective inhibition of the platelet aggregation induced by collagen, again in a dose-dependent manner. These fractions, especially that of chloroform, significantly suppressed platelet aggregation. The results of this study demonstrate that when yacon is added to a cholesterol-enriched diet, cholesterol-induced platelet aggregation returns to control levels. This may also be beneficial in preventing atherosclerosis and reducing risk factors for coronary artery disease and stroke.

Effects of Seomaeyakssuk (Artemisia argyi H.) Vinegar on Lipid Metabolism in Rats Fed a High-Fat and High-Cholesterol Diet (섬애약쑥 식초가 고지방-고콜레스테롤 급이 흰쥐의 체내 지질대사에 미치는 영향)

  • Shin, Jeong Yeon;Kang, Jae Ran;Shin, Jung Hye;Seo, Weon Taek;Byun, Hee Uk;Choi, Jin Sang;Kang, Min Jung
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.46 no.7
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    • pp.779-789
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    • 2017
  • The effects of orally administered Seomaeyakssuk (Artemisia argyi H.) vinegar on lipid metabolism in Sprague-Dawley rats fed a high-fat and high-cholesterol (HFC) diet were analyzed. The experimental animals were divided into five groups: a normal diet group (normal, N), HFC diet group (control, C), HFC diet with lovastatin at 20 mg/kg body weight (B.W.) group (positive control, PC), HFC diet with malt vinegar group (TM), and HFC diet with Seomaeyaksuk vinegar group (TS) (2 mL/kg B.W.). After 4 weeks of feeding rats the experimental diet, contents of serum total lipids and total cholesterol levels of TM and TS groups were significantly lower than those of the PC group. Triglyceride contents of the TM and TS groups were not significantly different from those of the PC group but significantly lower than those of the C group. Content of serum high density lipoprotein-cholesterol was significantly lower than that of the N group but higher than that of the C group. Low density lipoprotein-cholesterol content of serum was 190.68 mg/dL in the TS group, which was the lowest except for the N group. Aspartate transaminase and albumin transaminase activities as a measurement of liver damage index were not significantly different between the TM, TS, and C groups. Serum thiobarbituric acid reactive substance content of the TS group was reduced to a similar level as the N group but was lower than that of the C group in the liver and significantly higher than that of the N group. Antioxidant activity of the TS group was 55.69% in serum, which was a similar to that of the N group, and was 52.39% in the liver, which was not significantly different than that of the C group. From these results, we conclude that Seomaeyakssuk vinegar improves serum lipid content as a result of the complex action of vinegar, an active ingredient of Seomaeyakssuk and a product of the fermentation process.

Effects of Supplementation of Microbes Additive on the Fatty Acid Composition and Cholesterol Production in Meat of Pig and Chicken Broiler (미생물제제 첨가가 돈육과 계육의 지방산 조성 및 콜레스테롤 생산에 미치는 영향)

  • Kim Byung-Ki;Hong Kyu-Jin;Park Ji-Hyun;Kim Hyun-Soo
    • Food Science of Animal Resources
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    • v.24 no.4
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    • pp.399-404
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    • 2004
  • This study was conducted to determine the effect of supplemented useful microorganisim on meat quality of growing-finishing pigs for sixty days and broiler for six weeks. The pig and broiler were randomly allotted into three treatment (twenty-forty heads /treatment) ; Control (0%), T1 (supplemented with 0.2%, Aspergillus terreus koji), T2 (supplemented with 0.2%, EM-pro). The amount of stearic acid of pork was highest in T1 and T2, and oleic acid was highest in control and 71 than others (p<0.05). The amount of stearic acid of the chicken was highest in control, and oleic acid was highest in T1 and T2 than the others. Total cholesterol and HDL-cholesterol in the serum of pigs were decreased with significant difference (p<0.05) in T1 (63.77 and 111.19mg/mL, respectively) than control(101.69 and 132.37 mg/mL) and those of the chicken were decreased with lower significant difference (p<0.05) in T1 (78.50 and 143.61mg/mL) than control (119.26 and 240.43mg/mL). Total cholesterol and HDL-cholesterol in the pork were decreased with lower significant difference (p<0.05) in T1 (78.53 and 119.64 mg/mL) than control (140.55 and 150.55mg/mL), and those of the chicken were decreased with lower significant difference (p<0.05) in T1 (93.35 and 72.03mg/mL) than control (111.90 and 116.88 mg/mL). From the results, the amount of total cholesterol and HDL-cholesterol in pig and chicken was remarkably changed according to supplementation of Aspergillus terreus koji which containing the produced lovastatin.

Investigation on the occurrence and fate of micropollutants in domestic wastewater treatment plants based on full-scale monitoring and simple statistical analysis (현장 모니터링과 기초통계분석에 기반한 국내 하수처리장 미량오염물질 발생 및 거동 조사)

  • Chae, Sung Ho;Lim, Seung Ji;Lee, Jiho;Gashaw, Seid Mingizem;Lee, Woongbae;Choi, Sangki;Lee, Yunho;Lee, Woorim;Son, Heejong;Hong, Seok-Won
    • Journal of Korean Society of Water and Wastewater
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    • v.36 no.2
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    • pp.107-119
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    • 2022
  • The frequent detection and occurrence of micropollutants (MPs) in aquatic ecosystems has raised public health concerns worldwide. In this study, the behavior of 50 MPs was investigated in three different domestic wastewater treatment plants (WWTPs). Furthermore, the Kruskal-Wallis test was used to assess the geographical and seasonal variation of MPs in the WWTPs. The results showed that the concentrations of 43 MPs ranged from less than 0.1 to 237.6 ㎍ L-1, while other seven MPs including 17-ethynylestradiol, 17-estradiol, sulfathiazole, sulfamethazine, clofibric acid, simvastatin, and lovastatin were not detected in all WWTPs. Among the detected MPs, the pharmaceuticals such as metformin, acetaminophen, naproxen, and caffeine were prominent with maximum concentrations of 133.4, 237.6, 71.5, and 107.7 ㎍ L-1, respectively. Most perfluorinated compounds and nitrosamines were found at trace levels of 1.2 to 55.3 ng L-1, while the concentration of corrosion inhibitors, preservatives (parabens), and endocrine disruptors ranged from less than 0.1 to 4310.8 ng L-1. Regardless of the type of biological treatment process such as MLE, A2O, and MBR, the majority of pharmaceuticals (except lincomycin, diclofenac, iopromide, and carbamazepine), parabens (except Methyl paraben), and endocrine disruptors were removed by more than 80%. However, the removal efficiencies of certain MPs such as atrazine, DEET, perfluorinated compounds (except PFHxA), nitrosamines, and corrosion inhibitors were relatively low or their concentration even increased after treatment. The results of statistical analysis reveal that there is no significant geographical difference in the removal efficacy of MPs, but there are temporal seasonal variations in all WWTPs.