• Title/Summary/Keyword: Simvastatin

Search Result 72, Processing Time 0.032 seconds

Effects of Unripe Black Raspberry Water Extract on Lipid Metabolism and Oxidative Stress in Mice (복분자 미숙과 물 추출물이 마우스의 지질대사 및 산화적 스트레스에 미치는 영향)

  • Choi, Hye Ran;Lee, Jung-Hyun;Lee, Su Jung;Lee, Min Jung;Jeong, Jong Tae;Lee, Tae-Bum
    • Korean Journal of Food Science and Technology
    • /
    • v.46 no.4
    • /
    • pp.489-497
    • /
    • 2014
  • We examined the effects of unripe black raspberry water extract (UBR-W) on lipid metabolism and oxidative stress in mice. C57BL/6J mice were divided into 4 groups: those administered a control diet (CTL), high-fat diet (HFD), UBR-W and simvastatin for 12 weeks. In the HFD group, LDL cholesterol were significantly higher than in the CTL group. However, the UBR-W treated group showed dose-dependent reduction of plasma LDL levels. Hepatic total lipid, TC, and malondialdehyde were significantly increased in hyperlipidemic mice. However, supplementation with either UBR-W or simvastatin effectively reduced these lipid profiles and lipid peroxidation. UBR-W increased mRNA expression of the LDL receptor, sterol regulatory element binding protein 2 (SREBP2), 3-hydroxy-3-methylglutaryl (HMG)-CoA reductase and ATP-binding cassette transporter A1 (ABCA1) compared to that observed in the HFD group. In addition, UBR-W and simvastatin showed significantly reduced oxidized LDL uptake by the scavenger receptor CD36. These results suggest that UBR-W is useful for treatment and prevention of hyperlipidemia and lipid peroxidation.

Solubilization of poorly water-soluble drugs using solid dispersions

  • Kim, Tae-Wan;Choi, Choon-Young;Cao, Qing-Ri;Lee, Beom-Jin
    • Proceedings of the PSK Conference
    • /
    • 2002.10a
    • /
    • pp.412.2-413
    • /
    • 2002
  • Purpose. To prepare polymer based physical mixtures or solid dispersions containing solubilizing compositions using a spray-dryer. Methods. Lovastatin.simvastatin.aceclofenac and cisapride were selected as poorly water-soluble drugs. Dextrin. poly(vinylalcohol). poly(vinylpyrrolidone)and polyethylene glycol were chosen as solubilizing carriers for solid dispersions. The solid dispersions containing solubilizing compositions without drug were prepared without using organic solvents or tedious changes of formulation compositions. (omitted)

  • PDF

Implementation of Biopharmaceutics Classification System Concepts in Developing Dissolution Tests (용출규격 설정을 위한 생물약제학적분류체계 개념 활용)

  • Sah, Hong-Kee;Lee, Kyung-Sin;Baek, Min-Sun
    • Journal of Pharmaceutical Investigation
    • /
    • v.36 no.3
    • /
    • pp.161-167
    • /
    • 2006
  • The objective of this study was to investigate the dissolution patterns of variety of orally administered drug products available on the market. It aimed to understand their dissolution behaviors on the basis of the biopharmaceutics classification system (BCS) concept. On the tenets of BCS, several active pharmaceutical ingredients were selected: fluoxetine hydrochloride (class I), naproxen sodium (class ll), pyridostigmine bromide (class III), furosemide (class IV) and simvastatin (class IV). Typical dissolution media used in this study were pH 1.2, pH 4 & 6.8 phosphate buffers, and water. In cases, particular dissolution media specified in the KP and/or USP were used. Dissolution patterns of fluoxetine hydrochloride and pyridostigmine bromide products were characterized by their rapid release In addition, their dissolution characteristics were relatively unaffected by the type of a dissolution medium. Similar dissolution patterns were observed with pH 1.2, pH 4 & 6.8 phosphate buffers and water. By sharp contrast, poor dissolution patterns were noticed with naproxen sodium products, when pH 1.2 and pH 4 phosphate buffer were used. Improvements in its dissolution were achieved by switching the dissolution media to pH 6.8 phosphate buffer or water. Unsatisfactory dissolution data also were observed with a simvastatin product, when it was subject to dissolution tests by use of a surfactant-free pH 1.2, pH 4 & 6.8 phosphate buffers and water. All the release patterns reported in this study were best understood when BCS concepts were implemented. Our results demonstrated that a BCS-based drug classification should be considered first to choose a dissolution test/method and set up dissolution specification.

Hypolipemic Effect of 'Saengjinyanghyul-tang' water extracts in the Streptozotocin-induced Hyperlipemic SD Rat (생진양혈탕(生津養血湯) 물 추출물의 Streptozotocin 유발 고지혈증에 대한 효과)

  • Hur, Hyun;Kim, Dae-Jun;Byun, Joon-Seok;Choi, Bin-Hye
    • The Journal of Internal Korean Medicine
    • /
    • v.27 no.2
    • /
    • pp.444-458
    • /
    • 2006
  • In the Present study, the therapeutic hypolipemic effect of water extract of Saengjinyanghyl-tang (SJYHT), a herbal extract mixture for treatment of diabetes in oriental medicine was tested in Streptozotocin-induced diabetic hyperlipemic SD rats. For detect the therapeutic effects, the test articles were once a day dosed for 28 days by gastric gavage at a dosage 1000, 500 and 250mg/kg from 25 days after STZ-dosing, and the changes on body weight and gains, serum LDL, HDL, Triglyceride and Total Cholesterol levels were observed In addition, the effects of test articles were compared to that of Simvastatin, a well known hypolipemic agents 10mg/kg-dosing group. Base on these results, although no meaningful effects were detected on the serum HDL levels, it is concluded that Saengjinyanghyul-tang water extracts have relatively good favorable effect treatment of STZ-induced diabetic hyperlipemia because they showed clear evidences inhibit the increase of serum LDL, Triglyceride and Total Cholesterol levels. Therefore, it is expected that Saengjinyanghyul-tang extract has favorable potency to development hypolipemic drugs. In addition, about 1000mg/kg of Saengjinyanghyul-tang extracts have similar effect compared to that of Simvastatin 10mg/kg. The effective dosage of Saengjinyanghyul-tang water extracts in the present study was considered as below 250mg/kg.

  • PDF

Lipid Lowering and Antioxidant Effects of Newly Synthesized 4-[(Butylsulfinyl)methyl]-1,2-benzenediol (SMBD) in Diet-induced Hypercholesterolemic Rabbits

  • Kim, Hyun-Ju;Noh, Jeong-Sook;Kwon, Myung-Ja;Song, Su-Hee;Suh, Hong-Suk;Kim, Mi-Jeong;Song, Yeong-Ok
    • Bulletin of the Korean Chemical Society
    • /
    • v.31 no.11
    • /
    • pp.3327-3332
    • /
    • 2010
  • We investigated the effects of newly synthesized 4-[(butylsulfinyl)methyl]-1,2-benzenediol (SMBD) on the prevention of atherosclerosis in hypercholesterolemic rabbits. SMBD exhibited stronger inhibition of $Cu^{2+}$-induced low-density lipoprotein oxidation than that of ascorbic acid or simvastatin. Three-month-old rabbits were fed an atherogenic diet containing 0.5% cholesterol and 10% coconut oil, while other two groups were given an atherogenic diet with intravenous injection of either simvastatin or SMBD (0.33 mg/kg/day) for 4 weeks. The concentrations of plasma cholesterol and thiobarbituric acid reactive substances were significantly decreased in SMBD groups, compared to the control group. Also, aortic lipid level in the SMBD group significantly lower than that in the control group. Furthermore, compared with the control group, the SMBD group significantly inhibited the increase of aortic intimal thickness by 36% via reducing of aortic reactive oxygen species and cyclooxygenase-2 protein levels. We conclude that raised antioxidant effect of SMBD results in significant prevention against hypercholesterolemia.

Policosanol Reduces Blood Cholesterol Levels by Inhibiting Sterol Regulatory Element-binding Proteins-1c and Fatty Acid Synthase (Sterol regulatory element-binding proteins-1c와 지방산 합성효소의 억제를 통한 폴리코사놀의 혈중 콜레스테롤 감소)

  • Min Jung Park;Byeong Min An;Dongjun Lee;Ji Myung Choi;Yung Hyun Choi;Bo Sun Joo
    • Journal of Life Science
    • /
    • v.33 no.4
    • /
    • pp.315-324
    • /
    • 2023
  • The underlying action of policosanol in lowering cholesterol level has not yet been clearly elucidated. Several recent studies have suggested that sterol regulatory element-binding proteins (SREBP)-1c play a role in the regulation of cholesterol synthesis via the fatty acid synthesis pathway. To date, no study has evaluated the effects of policosanol on SREBP-1c-mediated fatty acid synthesis. Therefore, this study aimed to investigate whether the SREBP-1c-mediated fatty acid biosynthetic pathway is associated with the cholesterol-lowering effects of policosanol. Seven-week-old C57BL/6 male mice were randomly divided into 7 groups (n=7 per group) and treated for 8 weeks as follows: 1) normal diet (normal control), 2) high-fat diet (HFD), 3) HFD+ethanol (Pol-0), 4) HFD+policosanol 1 mg/kg (Pol-1), 5) HFD+policosanol 2 mg/kg (Pol-2), 6) HFD+policosanol 4 mg/kg (Pol-4), and 7) HFD+simvastatin 50 ㎍/kg (positive control). Policosanol and simvastatin were administered at the same time every day while maintaining the HFD. Body weight and food intake were measured weekly for 8 weeks. After 8 weeks, serum cholesterol levels were measured, histological analysis was carried out, and the expressions of SREBP-1c and fatty acid synthase (FAS) in the liver tissues were examined. Policosanol reduced body weight and the amount of food intake in a dose-dependent manner. Serum cholesterol levels were significantly lowered in the Pol-1 and Pol-4 groups. The expression of SREBP-1c and FAS was also significantly decreased in the Pol-4 group. These results suggest that the cholesterol-lowering effects of policosanol can occur due to the inhibition of the expression of SREBP-1c and FAS.

Inhibitory effects of Saiko-ka-Ryukotsu-Borei-To on the migration and proliferation of vascular smooth muscle cell and suppression of carotid intimal thickness after balloon injury in rats

  • Chung, Hwa-jin;Maruyama Ikuro;Tani Tadato;Lee, Sang-Kook
    • Proceedings of the PSK Conference
    • /
    • 2003.10b
    • /
    • pp.207.3-208
    • /
    • 2003
  • Objectives:We have reported that oral administration of Saiko-ka-Ryukotsu-Borei-To (SRB), a traditional Chinese formulation, inhibited the intimal thickening in carotid artery after balloon injury in cholesterol-fed rats. To elucidate its mechanism, the effects of SRB on migration and proliferation of vascular smooth muscle cell (VSMC) were examined in vivo and in vitro.Methods: < In vivo-study> Rats were fed on diet containing 1% cholesterol and SRB 3 days before and 4 days after denudation. Simvastatin was used as a positive control. (omitted)

  • PDF

Biodegradation of Blood Lipid Lower Agents (BLLAs) in Biological Activated Carbon (BAC) Process (BAC 공정에서의 고지혈증 치료제 생물분해 특성)

  • Yoom, Hoon-Sik;Son, Hee-Jong;Ryu, Dong-Choon;Yoo, Pyung-Jong
    • Journal of Korean Society of Environmental Engineers
    • /
    • v.39 no.3
    • /
    • pp.124-131
    • /
    • 2017
  • In this study, We investigated the effects of water temperature and empty bed contact time (EBCT) on the biodegradability of 8 blood lipid lower agents (BLLAs) in biological activated carbon (BAC) process. Experiments were conducted at three water temperatures ($8^{\circ}C$, $16^{\circ}C$ and $24^{\circ}C$) and three EBCTs (5 min, 10 min and 15 min). Increasing water temperature and EBCT increased the biodegradation efficiency of BLLAs in BAC process. Simvastatin and fenofibrate were the highest biodegradation efficiency, but atorvastatin and clofibric acid were the lowest. The kinetic analysis suggested a pseudo-first-order reaction model for biodegradation of 8 BLLAs at various water temperatures and EBCTs. The pseudo-first-order biodegradation rate constants ($k_{bio}$) of clofibric acid and atorvastatin were $0.0075min^{-1}$ and $0.0122min^{-1}$ at $8^{\circ}C$, and were $0.0540min^{-1}$ and $0.0866min^{-1}$ at $24^{\circ}C$, respectively. By increasing the water temperature from $8^{\circ}C$ to $24^{\circ}C$, the biodegradation rate constants ($k_{bio}$) were increased 7.1~7.2 times.

Evaluation of the Bioequivalence of Simvastatin 20mg Tablets in Healthy Volunteers (조코 정에 대한 엘바스타 정의 생물학적 동등성 평가)

  • Yun, Hwi-yeol;Kang, Wonku;Kwon, Kwang-il
    • Korean Journal of Clinical Pharmacy
    • /
    • v.15 no.1
    • /
    • pp.41-45
    • /
    • 2005
  • 심바스타틴은 cholesterol 생합성 과정에서 속도 조절 효소인 HMG-CoA reductase의 강력한 상경적 길항약으로서 고지혈증 치료에 널리 쓰이는 약물이다. 심바스타틴 제제인 MSD 사의 조코 20 mg정을 대조약으로 하여 시험약인 유영 제약의 엘바스타 20mg정의 생물학적 동등성 평가를 하기 위해 22명의 건강한 지원자를 모집하였다. 지원자를 두 군으로 나누어 2정씩 투여하였고 $2{\times}2$ 교차시험을 실시하였다. 심바스타틴의 혈장 중의 농도를 정량하기 위하여 발리데이션된 LC/MS/MS를 사용하였다. 채혈 시간은 투약 전 및 투약 후 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12 시간에 걸쳐 총 12시점에 걸쳐 시행하였다. 생물학적 동등성을 판정하기 위한 파라미터로 12시간까지의 혈장 중 농도곡선 하 면적 ($AUC_{12hr}$)과 최고 혈중 농도($C_{max}$)를 사용하였다. 12시간 까지의 혈중 농도 곡선 하 면적의 기하 평균은 $17.30ng{\cdot}ml/hr$(시험약)과 $17.35ng{\cdot}ml/hr$(대조약)으로 나타났다. 최고 혈중 농도의 경우 각 각 5.08 ng/ml(시험약)과 5.20 ng/ml(대조약)으로 관찰 되었다. $AUC_{12hr}$의 경우 로그변환한 평균치 차의 $90{\%}$ 신뢰구간이 log0.8510 - log1.1694이었고, $C_{max}$의 경우 log0.8176 - log1.1649로 계산되어 두 항목 모두 log0.8-log1.25이어야 한다는 식품의약품 안전청과 FDA의 기준을 모두 만족시켰다. 이상의 결과를 종합하면 시험약 엘바스타 정 20mg은 대조약 조코정 20 mg에 대하여 생물학적 동등한 것으로 판정되었다.트리머 전기비저항 탐사를 수행하였다. 이를 통해 하저에 케이블을 설치하는 방식에 비해 매우 신속하고 경제적으로 하저에 분포하는 이상대의 분포범위와 발달방향을 규명할 수 있었다.대에 대해 가장 효과적이다. 모델과 현장 적용 결과들을 통해 GRM SSM 방법을 이용하여 불규칙한 굴절면을 가진 지층들에 대해 좀 더 신뢰할 수 있는 정밀한 탄성파 속도를 산출할 수 있음을 보여주고 있다.별한 주의를 기울여야 한다.EX>$\alpha/\beta$=10인 경우 $62.0\~121.9\;Gy_{10}$ (중앙값: $93.0\;Gy_{10}$)의 분포를, ${\alpha/\beta}=3$인 경우 $93.6\~187.3\;Gy_3$ (중앙값=$137.6\;Gy_3$ )의 분포를 보였다. MD-BED $Gy_3$는 직장합병증 발생과의 관계는 통계적으로 유의하였고, 방광합병증과는 유의하지 않았다. 직장합병증과의 연관성은 MD-BED $Gy_3$보다 개별 환자의 직장전벽 총 선량 BED값인 R-BED $Gy_3$가 훨씬 더 높았다. 요도카테터 풍선의 후방지점이 대변하는 방광의 총 선량 BED값인 V-BED $Gy_3$도 방광합병증과 경향성 테스트에서 통계적 유의성을 보였다. 하지만, 어떠한 방사선선량도 골반제어율과 의미 있는 상관관계를 보이지 않았다. 본 기관에서 주치의의 선호도에 따라 강내근접치료가 외부방사선치료의 중간에 시행되는 형태인 샌드위치기법과 외부방사선치료 후반부에 시행되는 순차적 기법으로 구분하였을 때, 두 방식간 치료성적 및 합병증의 차이는 없었다. 총 치료기간에 대한 분석에서는 치료기간이 길어질수록 재발 위험이 커지는 경향을 보였으나, 나이 및 병기, 종양의 크기, MD-BED $Gy_{10}$

  • PDF

Cholesterol Improvement Effects of Co-treatment with Black Raspberry and Red Ginseng Extracts in Mice Fed a High Cholesterol Diet (고콜레스테롤 식이 투여 마우스에서 복분자 미숙과 추출물과 홍삼농축액 복합 투여의 콜레스테롤 개선 효과)

  • Lee, Min Jung;Lee, Su Jung;Choi, Hye Ran;Lee, Jung-Hyun;Jeong, Jong Tae;Choi, Kyung-Min;Cha, Jeong-Dan;Hwang, Seung-Mi;Park, Jong Hyuk;Lee, Joo Hee;Lee, Tae Bum
    • Journal of the Korean Society of Food Science and Nutrition
    • /
    • v.43 no.10
    • /
    • pp.1491-1499
    • /
    • 2014
  • We examined the effects of unripe black raspberry (UBR) and red ginseng (RG) extracts on cholesterol improvement in C57BL/6J mice fed a HCD (high cholesterol diet) for 12 weeks. Hepatic total lipid and total cholesterol contents were significantly induced in hyperlipidemic mice. However, supplementation with UBR, RG and simvastatin effectively reduced these lipid profiles. Further, UBR and co-treatment with UBR and RG increased expression of LDL receptor, SREBP2, and SR-B1 mRNA compared with HCD. The ApoB/ApoA1 ratio was reduced by co-treatment with UBR and RG compared to treatment with UBR. In addition, histopathologic evaluation showed that co-treatment with UBR and RG suppressed lipid accumulation as well as FAS and leptin expression in plasma. These results indicate that co-treatment with UBR and RG may be useful for the prevention of hypercholesterolemia.