• 제목/요약/키워드: Poloxamer

검색결과 117건 처리시간 0.023초

산마늘 기능성 활성물질 탐색 및 자원화 (Effect of Allium victorialis var.platyphyllum Leaves on Triton WR-1339-induced and Poloxamer-407-induced hyperlipidemic Rats and on Diet-Induced Obesity Rats)

  • 박희준
    • 한국자원식물학회:학술대회논문집
    • /
    • 한국자원식물학회 2005년도 춘계 학술발표대회
    • /
    • pp.5-16
    • /
    • 2005
  • The herb of Allium victorialis var. platyphyllum (Liliaceae) has been used as an edible wild herb and to treat heart failure and gastritis. We have already reported antihyperlipidemic anti-tumor effects of this plant. To enlarge the commercial availability of this food, it was investigated whether the extracts of A. victorialis var.platyphyllum reduce hyperlipidemia and obesity or not. The plants tested in this experiment were collected from two eco-types of IS. Ullung and Mt. Odae cultivated at Pyongchang. Extracts were prepared by extracting the fresh leaves and those dried at $36^{\circ}C$ and $90^{\circ}C$, respectively. Pretreatment with the ethanolic extracts for two weeks (p.o.) reduced serum triglyceride-, total cholesterol- and LDL-cholesterol contents in rats induced by Triton WR-1339, respectively. Furthermore, oral administration of the extracts also inhibited the hyperlipidemia induced with oral diet of 30% corn oil. In the other attempt to find to alleviate the obesity, the model rats with obesity were induced by the high fat-diet for six weeks. Post-treatment with the extracts for two weeks significantly reduced the hyperlipidemia. Retroperitoneal-, epidymal- and total abdominal fat pad weights were considerably reduced at 100 mg/kg oral administration of the extracts. Increased feces lipid contents were also found in the rat treated with the extracts. The extract of Mt. Odae eco-type showed more potent activity than that of Is. Ullung one. These results suggest that use of the fresh leaves may lead to the higher activity in treatment of hyperlipidemia and obesity than of the dried one.

  • PDF

생체내 예측 및 흰쥐를 이용한 니코틴 패취의 약물동력학적 평가 (In Vivo Prediction and Biopharmaceutical Evaluation of Nicotine Transdermal Patch)

  • 이우영;백승희;박은석;지상철
    • Journal of Pharmaceutical Investigation
    • /
    • 제35권4호
    • /
    • pp.273-278
    • /
    • 2005
  • Nicotine transdermal therapeutic systems $(TTS_S)$ have been regarded as an effective mean to aid smoking cessation. However, most of nicotine $TTS_S$ in the market have some problems such as unpleasant side effects and skin irritation due to the excess amount of the drug permeated and the properties of the additives employed. In order to solve these problems, new nicotine $TTS_S$ were formulated using biocompatible additives. The optimized formula of the drug layer consisted of nicotine, propylene glycol and poloxamer 188 at the ratio of 1.2: 17.0: 2.0. The drug layer had the sickness of $1,250\;{\mu}m$, the pH of 8.12. The skin permeation rate of nicotine from optimized nicotine patch (NP) was $21.5\;{\mu}g/cm^2/h$. Transdermal administration of nicotine patch has been carried out for the determination of pharmacokinetic parameters in rats. Steady-state plasma concentration of nicotine following transdermal application of NP (area of patch = $15\;cm^2$) on the dorsal skin of rats was 143.2 ng/ml and AUC for 24 hrs was 3,022 ng h/ml. In case of $EXODUS^{\circledR}$ and Nicotinell $TTS^{\circledR}$, the steady-state plasma concentration of nicotine and ACU for 24 hrs were 428.9 ng/ml, $9,121\;ng{\cdot}hr/ml$ and 155.3 ng/ml, $3,152\;ng{\cdot}h/ml$, respectively. NP showed the experimental plasma nicotine concentration profile was very similar to the simulated one and had an appropriate skin permeation rate and a steady-state concentration of nicotine, which can show therapeutic blood levels of the drug for 24 hrs without severe side effects.

비만유도 흰쥐에 대한 방풍통성산가미방 (防風通聖散加味方)의 항고지혈 효과 및 항산화 효과 (Hypolipidemic and Antioxidative Effects of Bangpoongtongsungsankamibang on Diet-Induced Obesity Rats)

  • 정승희;이경태;안홍식;이진용;최종원;김덕곤
    • 생약학회지
    • /
    • 제37권3호
    • /
    • pp.190-195
    • /
    • 2006
  • Obesity is associated with a number of pathological disorders such as non-insulin-dependent diabetes, hypertension, hyperlipidemia, and cardiovascular diseases. Bangpoongtongsungsankamibang (BTSK) has been widely used in the oriental medicine for the treatment of several diseases associated with inflammatory abnormalities in cardiovascular and nervous system. The BTSK is the modified prescription of Bangpoongtongsungsankamibang in which sea tangle (Laminaria japonica) were added. This study was carried out to detemine the anti-obestic effects of BTSK. Pretreatment with the BTSK at daily dose of 100 or 200 mg/kg (p.o.) far 4 weeks reduced serum triglyceride, total cholesterol contents in rat induced by Poloxamer-407 or Triton WR-1339, respectively. Furthermore, post-treatment with BTSK far four weeks also inhibited body weight gain, adipose tissue mass and hyperlipidemia induced by the high fat diet for six weeks. The BTSK shifted serum total-, HDL- and LDL-cholesterol levels toward the values of normal group, suggesting that BTSK has hypolipldemlc effects. The rats fed BTSK reduced lipid peroxide and hydroxy radical in the rat blood and increased superoxide dismutase (SOD) activity compared to the control group. Taken together, these results superoxide that BTSK improve hyperlidemia and obesity via the upregulation of anti-oxidative mechanism.

다양한 표면개질을 이용한 폴리에테르설폰 막의 친수성 향상 (Enhanced Hydrophilicity of Polyethersulfone Membrane by Various Surface Modification Methods)

  • 박소정;황준석;최원길;이형근;허강무
    • 폴리머
    • /
    • 제38권2호
    • /
    • pp.205-212
    • /
    • 2014
  • 본 연구에서는 폴리에테르설폰(polyethersulfone, PES)을 연소배가스에 포함된 수증기를 분리 및 회수하기 위한 고분자 분리막 소재로 사용하기 위해 다양한 물리 화학적 표면개질 방법을 사용하여 PES 평막 표면의 친수성을 향상시키고자 하였다. 균일한 PES 평막을 제조한 후 친수성 향상을 위한 개질 방법으로 산처리, 블렌딩 및 플라즈마 처리를 통해 표면개질을 하였고, 표면 특성을 비교하였다. PES 평막 표면의 특성 변화는 ATR-FTIR, XPS, SEM 및 접촉각 측정을 통해 관찰하였다. 황산을 이용한 산처리 방법과 양친매성 고분자를 이용한 블렌딩 방법에 의해 개질된 PES 평막에서는 접촉각의 변화가 크지 않았다. Ar 플라즈마 처리를 한 경우, 플라스마 처리 시간이 증가함에 따라 PES 표면의 친수성이 크게 증가하는 것을 확인할 수 있었다. 본 결과를 통해 다양한 표면개질 방법 중 플라즈마 방법을 적용하여 PES 표면을 처리하는 것이 PES 막 표면의 친수성 향상에 가장 효과적임을 확인하였다.

The antihyperlipidemic effect of alginate-free residue from sea tangle in hyperlipidemic rats

  • Yim, Mi-Jin;Lee, Jeong Min;Choi, Grace;Cho, Soon-Yeong;Lee, Dae-Sung
    • Fisheries and Aquatic Sciences
    • /
    • 제22권11호
    • /
    • pp.27.1-27.6
    • /
    • 2019
  • Background: In order to assess the high value-added use of the alginate-free residue of sea tangle, an animal study was performed to evaluate the functional activities and key compounds present. In the animal study, sea tangle and the alginate-free residue demonstrated good anti-hyperlipidemic and anti-arteriosclerotic abilities. Results: The functional compounds in the alginate-free residue of the sea tangle were effectively extracted by supercritical fluid extraction (SFE). The optimum extraction temperature and pressure were 40 ℃ and 6500 psi (M1) in the SFE, a better method in comparison to the conditions of 70 ℃ and 4500 psi (M2), respectively. The anti-atherosclerotic effects of the alginate-free residue of sea tangle (M1, M2) were investigated in Sprague-Dawley rats treated with poloxamer 407, Triton WR 1339, corn oil, and a high-fat diet. The M1 fraction reduced the serum lipid levels with greater efficacy than the M2 fraction. In the hyperlipidemic rats, treatment with M1 decreased the serum triglyceride (TG), total cholesterol (TC), and low-density lipoprotein-cholesterol (LDL-C) levels when compared to the levels in normal rats. Conclusion: Our results demonstrated that the alginate-free residue of sea tangle reduces serum TC, TG, and LDL-C. These results suggest that the alginate-free residue of sea tangle contains physiologically active components, such as fucosterol, that may exert beneficial effects in the prevention of atherosclerosis.

고체분산체로부터 비페닐디메칠디카르복실레이트의 용출 특성 및 토끼의 십이지장 점막 투과 (Dissolution Characteristics of Biphenyl Dimethyl Dicarboxylate from Solid Dispersions and Permeation through Rabbit Deuodenal Mucosa)

  • 현진;전인구
    • Journal of Pharmaceutical Investigation
    • /
    • 제24권2호
    • /
    • pp.57-65
    • /
    • 1994
  • To increase the dissolution rate of practically insoluble biphenyl dimethyl dicarboxylate (DDB), various solid dispersions were prepared with water soluble carriers, such as povidone (PVP K-30), poloxamer 407, sodium deoxycholate (SDC) and polyethylene glycol (PEG) 6000, at drug to carrier ratios of 1:3, 1:5 and 1:10 (w/w) by solvent or fusion method. Dissolution test was performed by the paddle method. The dissolution rate of DDB tablets (25 mg) on market was found to be very low (11.44, 9.02 and 6.42% at pH 1.2, 4.0 and 6.5 after 120 min, respectively). However, dissolution rates of DDB from various solid dispersions were very fast and reached supersaturation within 10 min. DDB-PEG 6000 solid dispersion appeared to be better in enhancing the in vitro dissolution rate than others. Furthermore, the incorporation of DDB and phosphatidylcholine (PC) into ${\beta}-cyclodextrin$ at ratios of 1:2:20, 1:5:20 and 1:10:20 resulted in a 4.9-, 11.2- and 19.6-fold increase in DDB dissolution after 120 min as compared with the pure drug, respectively. This might be attributed to the formation of lipid vesicles which entrapped a certain concentration of DDB during dissolution. On the other hand, the permeation of DDB through rabbit duodenal mucosa was examined using some enhancers such as SDC, sod. glycocholate (SGC) and glycyrrhizic acid ammonium salt (GAA). Only trace amounts of DDB were found to permeate through deuodenal mucosa in the absence of enhancer. SDC was found to markedly decrease the permeation flux of DDB, however, SGC and GAA (5 mM) enhanced the flux of DDB 1.6 and 2.4 times higher as compared with no additive, respectively.

  • PDF

아스코르빈산 팔미테이트를 함유한 리포겔의 피부 투과 및 잔류 특성 (Skin Penetration and Localization Characteristics of Lipogel Containing Ascorbyl Palmitate)

  • 이상길;우혜승;이연아;권용남;최영욱
    • Journal of Pharmaceutical Investigation
    • /
    • 제31권4호
    • /
    • pp.225-232
    • /
    • 2001
  • The present study was carried out to observe the effect of liposome dispersed gel formulation (Lipogel) on topical delivery of ascorbyl palmitate (AsP). Neutral and negatively charged MLV liposomes containing AsP were prepared with dimyristoylphosphadtidylcholine (DMPC) and dicetyl phosphate (DCP), and dispersed to poloxamer gel matrix. In the hydrolysis study in rat's skin homogenates, AsP hydrolyzed to ascorbic acid (AsA) according to the first-order kinetics with the rate constant of $2.46{\times}10^{-2}\;min^{-1}$. In the passive skin penetration study using Franz diffusion cell, lipogel systems exhibited the greater values in the flux $(J_s)$ and the amount penetrated $(Q_p)$ compared to control hydrogels containing diethyleneglycol monoethyl ether $(Transcutol^{\circledR})$ as a solubilizing agent and a penetration enhancer for AsP. The total amount penetrated $(Q_{Total})$, which is expressed as a summation of $Q_P\;and\;Q_L$, for lipogel system was about 1.4 times higher in average than that of control hydrogel. However the amount localized in the skin $(Q_L)$ was similar in both formulations. As a result, lipogel system enhanced the skin penetration of AsP, possibly due to the increase in local concentration of AsP by preferential adsorption of liposome to the skin and the enhancing effect of phospholipid in liposome composition. Moreover it was expected that the penetrated AsP would generate AsA during skin penetration by the skin esterase. In conclusion, lipogel formulation was considered as a good candidate for topical delivery of AsP.

  • PDF

Protective effects of alginate-free residue of sea tangle against hyperlipidemic and oxidant activities in rats

  • Yim, Mi-Jin;Choi, Grace;Lee, Jeong Min;Cho, Soon-Yeong;Lee, Dae-Sung
    • Fisheries and Aquatic Sciences
    • /
    • 제20권9호
    • /
    • pp.22.1-22.6
    • /
    • 2017
  • The antihyperlipidemic and antioxidant activities of dietary supplementation of sea tangle from Goseong and the alginate-free residue of sea tangle were investigated in Sprague Dawley rats treated with a high-fat diet, streptozotocin, poloxamer 407, and bromobenzene. The alginate-free residue of Goseong sea tangle induced a significant reduction in triglycerides and total cholesterol levels, as well as a significant increase in high-density lipoprotein cholesterol levels. Alginate-free Goseong sea tangle residue reduced the activities of the phase I enzymes aminopyrine N-demethylase and aniline hydroxylase, which had been increased by intraperitoneal injection of bromobenzene. Pretreatment with Goseong sea tangle residue prevented a bromobenzene-induced decrease in epoxide hydrolase activity. Bromobenzene reduced hepatic glutathione content and increased hepatic lipid peroxide levels. Pretreatment with alginate-free Goseong sea tangle residue prevented lipid peroxidation induced by bromobenzene, but pretreatment with Goseong sea tangle did not. These results suggest that Goseong sea tangle residue exerted antihyperlipidemic and antioxidant activities that were higher than those induced by alginate-containing sea tangle. Therefore, the alginate-free residue may contain physiologically unknown active components, other than alginic acid, which may potentially be used to prevent hyperlipidemic atherosclerosis.

Androstane과 Cholestane 유도체의 진통, 소염 및 항고지혈 효과 (Antinociceptive, Antiinflammtory and Antihypercholesterolemic Effects of Androstane and Cholestane Derivatives)

  • 김학순;마은숙
    • 약학회지
    • /
    • 제51권6호
    • /
    • pp.495-499
    • /
    • 2007
  • Seven epoxy- and hydroxyandrostane derivatives ($DH-1{\sim}DH-7$) and nine epoxy- and hydroxycholestane derivatives ($CH-1{\sim}CH-9$) with unsaturation in ring A and ring B were synthesized from DHEA and cholesterol, respectively. The antinociceptive effects of all synthesized compounds were measured by hot plate method. Most of androstane derivatives except $1{\alpha},2{\alpha}$-epoxy-4,6-androstadiene-3,17-dione (DH-3), and CH-6, CH-7 and CH-9 exhibited antinociceptive effect. 1,4-Androstadiene-$3{\beta},17{\beta}$-diol (DH-5, 100 mg/kg, $35.8{\pm}7.39$), $6{\alpha},7{\alpha}$-epoxy-1,4-androstadiene-3,17-dione (DH-4, 100 mg/kg, $32.6{\pm}5.50$) and $5{\alpha},6{\alpha}$-epoxy-17-oxo-androstan-$3{\beta}$-ol (DH-1, 100 mg/kg, $32.5{\pm}2.98$) were more effective than morphine (10 mg/kg, $30.6{\pm}0.5$). The analgesic effects of androstane derivatives on acetic acid writhing in mice were lower than aspirin. The androstane derivatives were less effective than ibuprofen at inhibiting effects on the carrageenin induced paw oedema. 4,6-Cholestadien-$3{\beta}$-ol (CH-5), $1{\alpha},2{\alpha}$-epoxy-4,6-cholestadien-$3{\beta}$-ol (CH-7) and $7{\alpha}$-hydroxy4-cholesten-3-one (CH-9) showed the decrease of serum triglyceride and total cholesterol levels in poloxamer P-407 injected rat.

케토프로펜을 함유하는 고형 지질 나노파티클의 제조 및 평가 (Preparation and Evaluation of Ketoprofen-incorporated Solid Lipid Nanoparticles (SLN))

  • 백명기;이상영;지웅길
    • Journal of Pharmaceutical Investigation
    • /
    • 제26권4호
    • /
    • pp.245-256
    • /
    • 1996
  • Solid lipid nanoparticles (SLN) have been developed as a new drug delivery system. Although many particulate drug carriers, such as microsphere, liposome, niosome, emulsion, etc. have been introduced, they have some disadvantage; low efficiency of incorporation and stability, lack of reproducibility, and so on. Meanwhile, SLN as a new drug delivery system is known to entrap rugs with a high efficiency and a good reproducibility. Moreover, small size SLN can circulate in blood for a prolonged time. Although many preparation methods were introduced, microfluidization method is recommended to be the most useful. This study was attempted to prepare and evaluate ketoprofen-incorporated SLNs (keto-SLN), which were prepared by two methods, ultrasonication and microfluidization. Keto-SLN was evaluated by measurement of particle size and zeta potential, efficacy of entrapment, sedimentation volume, in virto release pattern. The mean particle size was about $0.1\;{\mu}m$, and the size was dependent on the type and the amount of emulsifier. Zeta potential was negative, $-9{\sim}-13mV$ and entrapment efficacy was very high and stability was good for at least 60 days in the respect of particle size and sedimentation volume ratio. Analgesic effect was also determined as well as pharmacokinetic parameters. The former was comparable to that of that of ketoprofen loaded suspension (keto-sus) and the latter revealed that consistent with the delayed release of keto-SLN. $T_{max}$ was longer than keto-sus. Therefore, keto-SLN was favourable dosage forms in the field of drug delivery system such as anti-cancer, analgesics and anti-inflammatory agents.

  • PDF