• Title/Summary/Keyword: AM1

Search Result 2,277, Processing Time 0.031 seconds

Effect of Vehicles and Enhancers on the in vitro Skin Penetration of Aspalatone and Its Enzymatic Degradation Across Rat Skins

  • Gwak, Hye-Sun;Chun, In-Koo
    • Archives of Pharmacal Research
    • /
    • v.24 no.6
    • /
    • pp.572-577
    • /
    • 2001
  • The feasibility of skin penetration was studied for aspalatone (AM, acetylsalicylic acid maltol ester), a novel antithrombotic agent. In this studys hairless mouse dorsal skins were used as a model to select composition of vehicle and AM. Based on measurements of solubility and partition coefficient, the concentration of PC that showed the highest flux for AM across the hairless mouse skin was found to be 40%. The cumulative amount permeated at 48 h, however, appear inadequate, even when the PC concentration was employed. To identify a suitable absorption enhancer and its optimal concentration for AM, a number of absorption enhancers and a variety of concentration were screened for the increase in transdermal flux of AM. Amongst these, linoleic acid (LOA) at the concentration of 5% was found to have the largest enhancement factor (i.e., 132). However, a further increase in AM flux was not found in the fatty acid concentration greater than 5%, indicating the enhancement effect is in a bell-shaped currie. In a study of the effect of AM concentration on the permeation, there was no difference in the permeation rate between 0.5 and 1% for AM, below its saturated concentration. At the donor concentration of 2%, over the saturated condition, the flux of AM was markedly increased. A considerable degradation of AM was found during permeation studies, and the extent was correlated with protein concentrations in the epidermal and serosal extracts, and skin homogenates. In rat dorsal skins, the protein concentration decreased in the rank order of skin homogenate > serosal extract > epidermal extract. Estimated first order degradation rate constants were $6.15{\pm}0.14,{\;}0.57{\pm}0.02{\;}and{\;}0.011{\pm}{\;}0.004{\;}h^{-1}$ for skin homogenate, serosal extract and epidermal extract, respectively. Therefore, it appeared that AM was hydrolyzed to some extent into salicylmaltol by esterases in the dermal and subcutaneous tissues of skin. taken together, our data indicated that transdermal delivery of AM is feasible when the combination of PC and LOA is used as a vehicle. However, since AM is not metabolically stable, acceptable degradation inhibitors may be nervessary to fully realize the transdermal delivery of the drug.

  • PDF

Determination of Transuranic Elements in Radwaste Samples from Nuclear Power Plant (원전발생 방사성폐기물 시료 중 초우란원소의 정량)

  • 조기수;김태현;전영신;지광용;김원호
    • Proceedings of the Korean Radioactive Waste Society Conference
    • /
    • 2003.11a
    • /
    • pp.351-357
    • /
    • 2003
  • Transuranic elements such as Pu, Am and Cm in synthetic solution of spent nuclear fuel samples were determined by electrodeposition followed by alpha-spectrometry after separation using anion exchange and extraction chromatography in order to determine the transuranic elements in radwaste samples from nuclear power plants. Plutonium was separated by 12M HC1-0.1M HI as an eluent on anion exchange column. As a second step Am and Cm were separated in a group by DTPA-Lactic acid as the eluent on HDEHP coated column. The nuclides of $^{239}Pu$, $^{241}Am$$^{244}Cm$ separated were determined by alpha-spectrometry after electrodeposition in 0.1M $NaHSo_4$-0.53M $Na_2SO_4$buffer solution as an electrolyte. The recovery yields of $^{239}Pu$, $^{241}Am$$^{244}Cm$ were 83.8%, 85.2% and 86.3%, respectively, from the synthetic solution containing uranium and non-radioactive metal elements.

  • PDF

Permeation and Enzymatic Degradation of Aspalatone in Gastrointestinal Tract of Rabbit (아스팔라톤의 토끼 위장관 점막 투과 및 효소적 분해)

  • Chun, In-Koo;Gwak, Hye-Sun
    • Journal of Pharmaceutical Investigation
    • /
    • v.31 no.1
    • /
    • pp.27-35
    • /
    • 2001
  • To evaluate the site-specific permeation of aspalatone (acetylsalicylic acid maltol ester, AM) through gastrointestinal tract, the enzymatic degradation and permeation studies were carried out using gastric, duodenal and jejunal mucosae of rabbits. It was found that $15.2{\pm}11.4%$, $11.6{\pm}5.2$ and $0.8{\pm}0.6%$ of the donor dose of AM, salicylmaltol (SM) and aspirin (ASA) permeated through the upper gastric mucosa after 8 hr of permeation, respectively. After 8 hr of AM permeation, SM and ASA were measured to be $15.0{\pm}1.7$ and $2.6{\pm}0.8%$ of the dose in the donor solutions, respectively, and salicylic acid (SA) was not detected even after 6 hr, suggesting a very low gastric damage. For the gastric mucosa, the increase of donor dose from 100 to $1,000\;{\mu}g/ml$ increased the permeation flux dose-dependently (r=0.9905). For the duodenal and jejunal mucosae, however, AM was fully degraded into SM and SA due to the esterase activities within 30 min. AM and ASA were not detected in the receptor solution. This result indicates that AM is not a prodrug of ASA. Addition of potassium fluoride (0.5%) into the donor solution delayed the degradation of AM, but did not allow the permeation through duodenal mucosa even by the inhibition of esterase activity. The addition of $dimethyl-{\beta}-cyclodextrin$ and $2-hydroxypropyl-{\beta}-cyclodextrin$ (5%) into the donor solutions also did not show favorable effects on the permeation of AM through various mucosae. In comparison of permeation rates of AM and ASA through the upper gastric mucosa, the flux of ASA was 4.2 times faster than AM based on the molar concentration. ASA also was fully degraded in the donor solutions faced with duodenal and jejunal mucosae within 2 hr, and was not detected in the receptor solution, suggesting a slower metabolism compared with AM.

  • PDF

Complexation of Amphotericin B With Egg Phosphatidylcholine Liposomes

  • Kim, Jin-Chul;Lee, Eun-Ok;Yang, Ji-Won;Choe, Tae-Boo;Kim, Jong-Duk
    • Archives of Pharmacal Research
    • /
    • v.18 no.2
    • /
    • pp.84-89
    • /
    • 1995
  • The complexation and physical characteristics of egg phosphatidylcholine (PC) liposome containing amphotericin B(AmB) were investigated through circular dichrosim(CD) spectra, the size distribution, the turbidity change, and the calcein release. CD spectra of AmB-containing egg PC mxture exhibited a positive peak around 330 nm indicative of complexation of AmB and four negative peaks. The positive peak increased up to $2.2{\;}millidegree/{\mu}g$ AmB as AmB contents increased up to 12% (w/w), suggesting that AmB-phospholipid complexation was promoted by the antibiotics. The effective diameter of liposomesa by dynamic light scattering decreased from 450 nm to 220 nm as the amount of AmB in liposomes increased from o to 30% (w/w). The complexation may be responsible for the reduction in size. On the other hand, at around 1 mN deoxycholate (DOC), the reltive turbidities of 5 and 10% (w/w) AmB-containing liposome suspension were less than 1 probably due to the soblubilization of the complex, while those of pure PC liposome suspension were larger than 1 at the same concentration. Deoxycholate-induced release of liposomes, indicating the intercalation of the drug into the bilayers. Therefore, it is concluded that in AmB/eggPC/water system, AmB-phospholipid complexcoexists with AmB-containing liposomes.

  • PDF

Studies on Tolerance Level Against Antheraea mylitta Cytoplasmic Polyhedrosis Virus (AmCPV) in Different Eco-races of Tropical Tasar Silkworm, Antheraea Mylitta Drury

  • Singh, G.P.;Zeya, S.B.;Srivastava, A.K.;Ojha, N.G.;Suryanarayana, N.
    • International Journal of Industrial Entomology and Biomaterials
    • /
    • v.17 no.1
    • /
    • pp.153-155
    • /
    • 2008
  • Pathogenic infection in tasar silkworm, Antheraea mylitta Drury is common and there is a breed specific response regarding tolerance. Hence, the tolerance level of three eco-races of tasar silkworm viz. Daba, Sarihan and Raily to Antheraea mylitta cytoplasmic polyhedrosis virus (AmCPV) infection was tested. The survival of Daba, Sarihan and Raily eco-races was significantly different (p<0.05) when challenged with the same concentration ($1{\times}10^5$ polyhedra/ml) of AmCPV. Daba eco-race was more tolerant to the AmCPV infection having higher survival (65.7%) and $LC_{50}$ values (1000893.17 polyhedra/ml) of AmCPV followed by Sarihan eco-race (50.7% survival and $LC_{50}$ value of AmCPV 187203.6168 polyhedra/ml) and Raily eco-race (24.3% survival and $LC_{50}$ value of AmCPV 5176.37 polyhedra/ml). The tolerance level of Daba and Sarihan eco-races against AmCPV was more than two times than Raily eco-race.

Antioxidant Effect of Atractylodes macrocephala Koidzumi in DSS-induced Ulcerative Colitis Model (백출(白朮)의 항산화 효과가 DSS 유발 궤양성 대장염 모델에 미치는 영향)

  • Park, Seok Man;Lee, Se Hui;Jeong, Da un;Cho, Su-Jung;Shin, Mi-Rae;Park, Hae-Jin;Roh, Seong-Soo
    • The Korea Journal of Herbology
    • /
    • v.37 no.1
    • /
    • pp.19-29
    • /
    • 2022
  • Objectives : Although the pharmacological effects of anti-inflammatory and antioxidant action of Atractylodes macrocephala Koidzumi water extract (AM) have been proven from many studies, reports on the antioxidant effect of AM on ulcerative colitis (UC) are scarce. Therefore, we aimed at evaluating the anti-oxidant effect of AM on the DSS-induced UC model. Methods : To induce ulcerative colitis, 8-week-old male Balb/c mice received 5% DSS in drinking water for 1 week. After 1 week of adaptation, mice were divided into four groups (n=8 each) for use as normal (Normal), DSS Control (Control), DSS + AM 100 mg/kg (AM100)-treatment, DSS + AM 200 mg/kg (AM200)-treatment. After 1 week of the experiment, the animals were sacrificed, and the extracted colon tissue was analyzed for protein through western blot. Results : As a result of confirming the macroscopic changes in colon tissues to confirm the therapeutic effects of AM, the decrease in colon length was suppressed in the AM treatment group compared to the control group. In addition, as a result of biochemical analysis, AM administration significantly reduced serum glutamic oxalacetic transaminase, glutamic pyruvate transaminase levels and tissue malondialdehyde levels. As a result of confirming the protein expression level through western blot, AM administration significantly decreased the expression of NADPH-related proteins such as NOX2, p22phox, and iNOS, but significantly increased the expression of SOD, catalase, and GPx-1/2. Conclusions : AM may improve DSS-induced UC in mice by modulating NADPH and antioxidant-related proteins. In conclusion, AM showed an antioxidant effect through the improvement of oxidative stress on UC.

Network Pharmacology: Prediction of Astragalus Membranaceus' and Cornus Officinalis' Active Ingredients and Potential Targets to Diabetic Nephropathy (네트워크 약리학을 통한 당뇨병성 신병증에서의 황기와 산수유의 활성 성분 및 잠재 타겟 예측)

  • Lee, Keun-Hyeun;Rhee, Harin;Jeong, Han-Sol;Shin, Sang Woo
    • Journal of Physiology & Pathology in Korean Medicine
    • /
    • v.31 no.6
    • /
    • pp.313-327
    • /
    • 2017
  • The purpose of this study is to predict the effects of macroscopic and integrative therapies by finding active ingredients, potential targets of Astragalus membranaceus (Am) and Cornus officinalis (Co) for diabetic nephropathy. We have constructed network pharmacology-based systematic and network methodology by system biology, chemical structure, chemogenomics. We found several active ingredients of Astragalus membranaceus (Am) and Cornus officinalis (Co) that were speculated to bind to specific receptors which had been known to have a role in the progression of diabetic nephropathy. Four components of Am and eleven components of Co could bind to iNOS; two ingredients of Am and six ingredients of Co could docking to cGB-PDE; one component of Am and nine components of Co could bind to ACE; three ingredients of Co with neprilysin; three components of Co with ET-1 receptor; four ingredients of Am and fourteen ingredients of Co with mineralocorticoid receptor; one component of Am and seven components of Co with interstitial collagenase; one ingredient of Am and ten ingredients of Co with membrane primary amine oxidase; one component of Am and four components of Co with JAK2; two ingredients of Am and one ingredient of Co with MAPK 12; one component of Am and five components of Co could docking to TGF-beta receptor type-1. From this work we could speculate that the possible mechanisms of Am and Co for diabetic nephropathy are anti-inflammatory, antioxidant and antihypertensive effects.

Determination of $^{241}$Am and $^{241}$Cm in Radwaste Samples (방사성폐기물 시료 중 $\^{241}$Am과 $\^{244}$Cm의 정량)

  • Joe Kih Soo;Kim Tae Hyun;Jeon Young Shin;Jee Kwsng Yong;Kim Won Ho
    • Journal of Nuclear Fuel Cycle and Waste Technology(JNFCWT)
    • /
    • v.3 no.1
    • /
    • pp.1-7
    • /
    • 2005
  • Anion exchange chromatography and HDEHP extraction chromatography using DTPA-lactic acid as an eluent were applied in series for the separation of $^{241}$Am and $^{244}$Cm in radwaste samples. The separated elements were determined by electrodeposition at the sodium hydrogen sulfate-sodium sulfate buffer solution followed by alpha-spectrometry. The recovery yields of $^{241}$Am and $^{244}$Cm were 85.2$\pm$$15.3\%$, respectively, from the synthetic solution of spent nuclear fuel sample. The amounts of 241Am and 2440m determined in radwaste sample solutions of condensate bottoms were at the range of 1.5-1.9 Bq/g and -1.7 Bq/g, respectively.

  • PDF

The Stability of Aspalatone and Aspirin in Buffered Aqueous Solution (완충 수용액중 아스파라톤 및 아스피린의 안정성)

  • 곽혜선;전인구
    • Proceedings of the Korean Society of Applied Pharmacology
    • /
    • 1995.04a
    • /
    • pp.130-130
    • /
    • 1995
  • AM, SM 및 ASA는 수용액중에서 겉보기 1차반응에 따라 분해되었으며 보존온도가 높을수록 분해가 촉진되는 온도 의존성을 나타내었다. AM의 분해경로는 pH 1.22 및 pH 7.0 이상에서는 AM$\longrightarrow$ SM $\longrightarrow$ SA의 경로로 주로 분해되었으며 pH 2.01 - 6.08의 범위에서는 AM $\longrightarrow$ASA$\longrightarrow$SA의 경로로 분해되는 양상을 보였다. 또 pH가 분해에 미치는 영향을 pH-rate profile로 나타낸 결과 AM, SM 및 ASA의 최대안정 pH는 각각 4.0, 3.0, 2.0 부근이 있고 이 조건에서의 분해 반감기는 114, 168, 113 hr로 나타났다. 전체적으로 보면 pH 2.0 이하에서는 ASA가 AM 보다 약간 안정한 편이나 pH 2.0-8.0 사이에서는 AM의 분해속도가 ASA보다 현저히 낮았다. 또 AM은 pH 7.0 이상에서, SM은 pH 6.0 이상에서, ASA는 9.0 이상에서 특수염기촉매반응에 따라 분해가 이루어지는 것을 알 수 있었다. 이온강도($\mu$)의 영향으로는 pH 7.0에서 이온강도가 0.115에서 1.0으로 증가할수록 $\mu$$^{1}$2/에 대해 AM의 분해속도정수가 직선적으로 완만하게 감소되었다. 또 완충수용액 중 AM의 가수분해 억제효과를 검토하기 위해 시클로덱스트린류를 첨가하였을 때, $\beta$-시클로덱스트린과 히드록시프로필기-$\beta$-시클로덱스트린은 AM의 분해를 각각 1.6배 및 1.1배 촉진시켜 촉매적으로 작용하였으며 디메칠-$\beta$-시클로덱스트린은 약 3.2배 분해속도를 억제시켜 안정화제로 작용하였다.Zn^{2+}$, soybean trypsin inhibtor에 의해 25~50% 정도, serine proteinase inhibitor인 phenylmethylsulfonyl floride에 의해 80%정도 활성이 억제되는 특성이 있음을 규명하였다.면역환성 (immunoreactivity)이 나타났고 pyramidal cell layer (PCL)와 glia에 SOD-1이 강하게 염색되었다. APT 병용 투여로 상당수의 경련이 일어나지 않은 흰쥐는 해마의 DG에 FRA가 경미하게 염색되었고, PCL에 SOD-1도 경미하게 나타났으나, 경련이 나타난 쥐에서는 KA만을 투여한 흰쥐와 구별되지 않았다. 이상의 APT의 항산화 효과는 KA로 인한 뇌세포 변성 개선에 중요한 인자로 작용할 것으로 사료되나, 보다 명확한 APT의 기전을 검색하고 직접 임상에 응응하기 위하여는 보다 다양한 실험 조건이 보완되어야 찰 것으로 생각된다. 항우울약들의 항혈소판작용은 PKC-기질인 41-43 kD와 20 kD의 인산화를 억제함에 기인되는 것으로 사료된다.다. 것으로 사료된다.다.바와 같이 MCl에서 작은 Dv 값을 갖는데, 이것은 CdCl$_{4}$$^{2-}$ 착이온을 형성하거나 ZnCl$_{4}$$^{2-}$ , ZnCl$_{3}$$^{-}$같은 이온과 MgCl$^{+}$, MgCl$_{2}$같은 이온종을 형성하기 때문인것 같다. 한편 어떠한 용리액에서던지 NH$_{4}$$^{+}$의 경우 Dv값이 제일 작았다. 바. 본 연구의 목적중의 하나인 인체유해 중금속이온인 Hg(II), Cd(II)등이 NaCl같은 염화물이 함유된 시료용액에 공해이온으로 존재할 경우 흡착에 의한 제거가 가능하다. 한편 이같

  • PDF

Qualitative Mapping of Ambient Intelligence Characteristics to Operating System Features in Smart Environment

  • Choo, Young-Yeol
    • International Journal of Contents
    • /
    • v.2 no.4
    • /
    • pp.1-7
    • /
    • 2006
  • The goal of Ambient Intelligence (AmI) is to build a smart environment for users where they are supported in some of their activities by many interaction mechanisms. The diversity of AmI characteristics requires special support from Operating Systems (OSes). In this paper, in order to support a conscious choice of an operating system for any specific AmI application, features requested by AmI systems were characterized and defined considering various applications. Then, characteristics of existing Operating Systems have been investigated in the context of AmI application support to relate their key characteristics to the typical requirements of AmI systems. Qualitative mapping table between AmI characteristics and as features has been proposed with an illustration of how to use it. As no as completely covers the range of characteristics required by AmI systems, challenging issues are summarized for the development of a new as and a product line of OSes.

  • PDF