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Pesquisa : D03.066.515.530.500 [Categoria DeCS]
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[PMID]:23124661
[Au] Autor:Lopez-Avila V; Cooley J; Urdahl R; Thevis M
[Ad] Endereço:Agilent Technologies, Santa Clara, CA, 95051, USA. viorica_lopez-avila@agilent.com
[Ti] Título:Determination of stimulants using gas chromatography/high-resolution time-of-flight mass spectrometry and a soft ionization source.
[So] Source:Rapid Commun Mass Spectrom;26(23):2714-24, 2012 Dec 15.
[Is] ISSN:1097-0231
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:RATIONALE: The aim of this study was to investigate the mass spectral fragmentation of a small set of stimulants in a high-resolution time-of-flight mass spectrometer equipped with a soft ionization source using vacuum ultraviolet (VUV) photons emitted from different plasma gases. It was postulated that the use of a plasma gas such as Xe, which emits photons at a lower energy than Kr or Ar, would lead to softer ionization of the test compounds, and thus to less fragmentation. METHODS: A set of nine stimulants: cocaine, codeine, nicotine, methadone, phenmetrazine, pentylenetetrazole, niketamide, fencamfamine, and caffeine, was analyzed by gas chromatography/time-of-flight mass spectrometry (GC/TOFMS) in positive ion mode with this soft ionization source, using either Xe, Kr, or Ar as plasma gases. Working solutions of the test compounds at 0.1 to 100 ng/µL were used to establish instrument sensitivity and linearity. RESULTS: All test compounds, except methadone and pentylenetetrazole, exhibited strong molecular ions and no fragmentation with Xe-microplasma photoionization (MPPI). Methadone exhibited significant fragmentation not only with Xe, but also with Kr and Ar, and pentylenetetrazole could not be ionized with Xe, probably because its ionization energy is above 8.44 eV. The Kr- and Ar-MPPI mass spectra of the test compounds showed that the relative intensity of the molecular ion decreased as the photon energy increased. CONCLUSIONS: When coupled to a TOF mass spectrometer this soft ionization source has demonstrated signal-to-noise (S/N) ratios from 7 to 730 at 100 pg per injection (depending on the compound), and a dynamic range of three orders of magnitude (100 pg to 100 ng) for some of the test compounds.
[Mh] Termos MeSH primário: Estimulantes do Sistema Nervoso Central/análise
Cromatografia Gasosa-Espectrometria de Massas/instrumentação
[Mh] Termos MeSH secundário: Cafeína/análise
Cocaína/análise
Codeína/análise
Inibidores da Captação de Dopamina/análise
Desenho de Equipamento
Antagonistas GABAérgicos/análise
Estimulantes Ganglionares/análise
Íons/química
Metadona/análise
Entorpecentes/análise
Nicotina/análise
Niquetamida/análise
Norbornanos/análise
Pentilenotetrazol/análise
Fenmetrazina/análise
Sensibilidade e Especificidade
[Pt] Tipo de publicação:EVALUATION STUDIES; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Central Nervous System Stimulants); 0 (Dopamine Uptake Inhibitors); 0 (GABA Antagonists); 0 (Ganglionic Stimulants); 0 (Ions); 0 (Narcotics); 0 (Norbornanes); 368IVD6M32 (Nikethamide); 3G6A5W338E (Caffeine); 6M3C89ZY6R (Nicotine); I5Y540LHVR (Cocaine); NME1I5IGBK (fencamfamine); Q830PW7520 (Codeine); UC6VBE7V1Z (Methadone); WM5Z385K7T (Pentylenetetrazole); XA501VL3VR (Phenmetrazine)
[Em] Mês de entrada:1304
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:121106
[St] Status:MEDLINE
[do] DOI:10.1002/rcm.6398


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[PMID]:21402138
[Au] Autor:Wu XY; Zhao JL; Zhang M; Li F; Zhao T; Yang LQ
[Ad] Endereço:School of Chemistry and Chemical Engineering, Jiangsu University, Zhenjiang 212013, China.
[Ti] Título:Sedative, hypnotic and anticonvulsant activities of the ethanol fraction from Rhizoma Pinelliae Praeparatum.
[So] Source:J Ethnopharmacol;135(2):325-9, 2011 May 17.
[Is] ISSN:1872-7573
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:ETHNOPHARMACOLOGICAL RELEVANCE: Rhizoma Pinelliae Praeparatum is the product of raw Rhizoma Pinellia processed with alkaline solution and Licorice, which had been widely used for treatment of insomnia in traditional Chinese medicine. The present study aimed to investigate the sedative, hypnotic and anticonvulsant activities of ethanol fraction from Rhizoma Pinelliae Praeparatum (EFRP) and to determine whether these effects were related to GABAergic mechanism. MATERIALS AND METHODS: The sedative, hypnotic and anticonvulsant activities of EFRP were investigated with locomotion activity, pentobarbital-induced sleeping and nikethamide (NKTM)-induced convulsion tests, respectively. Additionally, the effects of flumazenil (an antagonist of GABA(A) receptor) and L-malic acid (blocker of synthetic enzyme for GABA) on the hypnotic activity of EFRP were evaluated. RESULTS: EFRP at dose of 12 g/kg significantly inhibited the locomotion activity of mice. EFRP showed synergic effect on pentobarbital-induced sleeping by increased numbers of mice falling asleep, reduced the sleep latency and prolonged the sleeping time. L-malic acid and flumazenil inhibited the augment effects of EFRP on pentobarbital-induced sleeping. EFRP promoted a significant protection to NKTM-induced convulsion, by prolonged the death latency and decreased mortality. CONCLUSION: EFRP possessed sedative, hypnotic and anticonvulsant activities and these activities may be related to the GABAergic system.
[Mh] Termos MeSH primário: Anticonvulsivantes/farmacologia
Hipnóticos e Sedativos/farmacologia
Pinellia/química
Extratos Vegetais/farmacologia
[Mh] Termos MeSH secundário: Animais
Anticonvulsivantes/uso terapêutico
Etanol/química
Locomoção/efeitos dos fármacos
Camundongos
Camundongos Endogâmicos ICR
Niquetamida/administração & dosagem
Pentobarbital/administração & dosagem
Convulsões/induzido quimicamente
Convulsões/tratamento farmacológico
Sono/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anticonvulsants); 0 (Hypnotics and Sedatives); 0 (Plant Extracts); 368IVD6M32 (Nikethamide); 3K9958V90M (Ethanol); I4744080IR (Pentobarbital)
[Em] Mês de entrada:1109
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:110316
[St] Status:MEDLINE
[do] DOI:10.1016/j.jep.2011.03.016


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[PMID]:18425309
[Au] Autor:Qian ZB; Wu ZH
[Ad] Endereço:Department of Physiology, Southern Medical University, Guangzhou 510515, China.
[Ti] Título:[Role of 5-HT(2A) receptor in increase in respiratory-related rhythmic discharge activity by nikethamide in neonatal rat transverse medullary slices].
[So] Source:Sheng Li Xue Bao;60(2):216-20, 2008 Apr 25.
[Is] ISSN:0371-0874
[Cp] País de publicação:China
[La] Idioma:chi
[Ab] Resumo:To investigate the effects of nikethamide on the generation and modulation of rhythmic respiration of neonatal rats and the role of 5-HT(2A) receptor in this course, experiments were performed on the transverse medullary slices of neonatal rats (both sexes, 1-3 d) in vitro. The slices containing the medial region of the nucleus retrofacialis (mNRF) with the hypoglossal nerve rootlets were prepared in which the respiratory-related rhythmic discharge activity (RRDA) was recorded from the hypoglossal nerve rootlets by suction electrode. The possible role of nikethamide on RRDA was investigated by administration of an agonist of 5-HT(2A) receptor, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI), and an antagonist of 5-HT(2A) receptor, ketanserine, dissolved in modified Krebos solution (MKS). Thirty slices were randomly divided into five groups: Group 1: the slices were perfused with different concentrations of nikethamide (0.5, 1, 3, 5, 7, 10 µg/mL), and the most effective concentration was selected; Group 2: the slices were perfused with DOI (40 µmol/L); Group 3: the slices were perfused with ketanserine (40 µmol/L); Group 4: the slices were perfused with ketanserine + DOI; Group 5: the slices were perfused with nikethamide, then perfused with nikethamide + ketanserine after washout of nikethamide. Nikethamide increased RRDA in transverse medullary slices at 0.5-7 µg/mL, and 5 µg/mL was the most effective concentration. DOI increased RRDA with prolonged inspiratory time (TI), increased integral amplitude (IA), and shortened respiratory cycle (RC). Ketanserine decreased RRDA with shortened TI, decreased IA and prolonged RC. Ketanserine + DOI had no significant effects on RRDA. The effects of nikethamide on RC and IA were totally and partially reversed by additional application of ketanserine, but the effect of nikethamide on TI was not influenced by ketanserine. It is proposed that nikethamide increases RRDA partly via 5-HT(2A) receptors.
[Mh] Termos MeSH primário: Bulbo/fisiologia
Niquetamida/farmacologia
Receptor 5-HT2A de Serotonina/metabolismo
Respiração/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Animais Recém-Nascidos
Feminino
Técnicas In Vitro
Masculino
Bulbo/efeitos dos fármacos
Ratos
Ratos Sprague-Dawley
Centro Respiratório/fisiologia
Serotonina
[Pt] Tipo de publicação:ENGLISH ABSTRACT; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Receptor, Serotonin, 5-HT2A); 333DO1RDJY (Serotonin); 368IVD6M32 (Nikethamide)
[Em] Mês de entrada:1505
[Cu] Atualização por classe:080421
[Lr] Data última revisão:
080421
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080422
[St] Status:MEDLINE


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[PMID]:18359677
[Au] Autor:Qian ZB; Qi Y; Wu ZH
[Ad] Endereço:Department of Physiology, Southern Medical University, Guangzhou 510515, China. qianzb@fimmu.com
[Ti] Título:[GABA A receptor participates in respiratory enhancement induced by nikethamide in neonatal rats].
[So] Source:Nan Fang Yi Ke Da Xue Xue Bao;28(3):301-4, 2008 Mar.
[Is] ISSN:1673-4254
[Cp] País de publicação:China
[La] Idioma:chi
[Ab] Resumo:OBJECTIVE: To investigate the role of GABA A receptor in nikethamide-induced respiratory enhancement in the medullary slices of neonatal rats. METHODS: Ex vivo medullary slices of neonatal rats (1 to 3 days old) containing the medial region of the nucleus retrofacialis with the hypoglossal nerve rootlets were prepared and perfused with modified Kreb's solution to record respiration-related rhythmic discharge activity (RRDA) from the hypoglossal nerve rootlets using suction electrodes. Thirty RRDA-positive slices were randomized into 5 equal groups and perfused with nikethamide (at concentrations of 0.5, 1, 3, 5, 7, and 10 microg/ml with the optimal nikethamide concentration determined), GABA (at 10, 20, 40, and 60 micromol/ to determine the optimal concentration), 10 micromol/ bicuculline, 10 micromol/ bicuculline plus 40 micromol/L GABA, and 5 microg/ml nikethamide followed by 5 microg/ml nikethamide plus 10 micromol/ bicuculline after wash out, respectively. RESULTS: Nikethamide increased RRDA at the concentrations of 0.5-7 microg/ml, and 5 microg/ml nikethamide showed the most distinct effect on the inspiratory time (TI), integral amplitude (IA), and respiratory cycle (RC). GABA at 40 micromol/ showed the most effective inhibition of RRDA in terms of TI, IA, and RC. Bicuculline at 10 micromol/ could increase the IA, TI and RC, but the combination of 10 micromol/ bicuculline and 40 micromol/ GABA had no significant effects on RRDA. Compared with nikethamide used alone, nikethamide plus bicuculline significantly increased TI and IA without affecting RC. CONCLUSION: Nikethamide can enhance RRDA of the hypoglossal nerve rootlets in the medullary slices of neonatal rats, and the effect can be partially mediated by the GABA A receptor.
[Mh] Termos MeSH primário: Bulbo/fisiologia
Niquetamida/farmacologia
Receptores de GABA-A/fisiologia
Centro Respiratório/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Animais Recém-Nascidos
Estimulantes do Sistema Nervoso Central/farmacologia
Feminino
Técnicas In Vitro
Masculino
Distribuição Aleatória
Ratos
Ratos Sprague-Dawley
Respiração/efeitos dos fármacos
Centro Respiratório/fisiologia
[Pt] Tipo de publicação:ENGLISH ABSTRACT; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Central Nervous System Stimulants); 0 (Receptors, GABA-A); 368IVD6M32 (Nikethamide)
[Em] Mês de entrada:0904
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080325
[St] Status:MEDLINE


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[PMID]:17289323
[Au] Autor:Chen L; Liao L; Zuo Z; Yan Y; Yang L; Fu Q; Chen Y; Hou J
[Ad] Endereço:West China School of Preclinical Medicine and Forensic Medicine, Sichuan University, No. 17, Section 3, Renmin Nan Road, Chengdu 610041, PR China.
[Ti] Título:Simultaneous determination of nikethamide and lidocaine in human blood and cerebrospinal fluid by high performance liquid chromatography.
[So] Source:J Pharm Biomed Anal;43(5):1757-62, 2007 Apr 11.
[Is] ISSN:0731-7085
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Nikethamide and lidocaine are often requested to be quantified simultaneously in forensic toxicological analysis. A simple reversed-phase high performance liquid chromatography (RP-HPLC) method has been developed for their simultaneous determination in human blood and cerebrospinal fluid. The method involves simple protein precipitation sample treatment followed by quantification of analytes using HPLC at 263 nm. Analytes were separated on a 5 microm Zorbax Dikema C18 column (150 mm x 4.60 mm, i.d.) with a mobile phase of 22:78 (v/v) mixture of methanol and a diethylamine-acetic acid buffer, pH 4.0. The mean recoveries were between 69.8 and 94.4% for nikethamide and between 78.9 and 97.2% for lidocaine. Limits of detection (LODs) for nikethamide and lidocaine were 0.008 and 0.16 microg/ml in plasma and 0.007 and 0.14 microg/ml in cerebrospinal fluid, respectively. The mean intra-assay and inter-assay coefficients of variation (CVs) for both analytes were less than 9.2 and 10.8%, respectively. The developed method was applied to blood sample analyses in eight forensic cases, where blood concentrations of lidocaine ranged from 0.68 to 34.4 microg/ml and nikethamide ranged from 1.25 to 106.8 microg/ml. In six cases cerebrospinal fluid analysis was requested. The values ranged from 20.3 to 185.6 microg/ml of lidocaine and 8.0 to 72.4 microg/ml of nikethamide. The method is simple and sensitive enough to be used in toxicological analysis for simultaneous determination of nikethamide and lidocaine in blood and cerebrospinal fluid.
[Mh] Termos MeSH primário: Cromatografia Líquida de Alta Pressão/métodos
Lidocaína/sangue
Lidocaína/líquido cefalorraquidiano
Niquetamida/sangue
Niquetamida/líquido cefalorraquidiano
[Mh] Termos MeSH secundário: Adulto
Idoso
Anestésicos Locais/sangue
Anestésicos Locais/líquido cefalorraquidiano
Estimulantes do Sistema Nervoso Central/sangue
Estimulantes do Sistema Nervoso Central/líquido cefalorraquidiano
Cromatografia Líquida de Alta Pressão/instrumentação
Evolução Fatal
Medicina Legal/métodos
Seres Humanos
Masculino
Meia-Idade
Padrões de Referência
Reprodutibilidade dos Testes
Estudos Retrospectivos
Sensibilidade e Especificidade
[Pt] Tipo de publicação:CASE REPORTS; COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anesthetics, Local); 0 (Central Nervous System Stimulants); 368IVD6M32 (Nikethamide); 98PI200987 (Lidocaine)
[Em] Mês de entrada:0706
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:070210
[St] Status:MEDLINE


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[PMID]:16490330
[Au] Autor:Elkharraz K; Faisant N; Guse C; Siepmann F; Arica-Yegin B; Oger JM; Gust R; Goepferich A; Benoit JP; Siepmann J
[Ad] Endereço:College of Pharmacy, Freie Universitaet Berlin, Kelchstr. 31, 12169 Berlin, Germany.
[Ti] Título:Paclitaxel-loaded microparticles and implants for the treatment of brain cancer: preparation and physicochemical characterization.
[So] Source:Int J Pharm;314(2):127-36, 2006 May 18.
[Is] ISSN:0378-5173
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The aim of this study was to prepare different types of paclitaxel-loaded, PLGA-based microparticles and lipidic implants, which can directly be injected into the brain tissue. Releasing the drug in a time-controlled manner over several weeks, these systems are intended to optimize the treatment of brain tumors. The latter is particularly difficult because of the blood-brain barrier (BBB), hindering most drugs to reach the target tissue upon systemic administration. Especially paclitaxel (being effective for the treatment of ovarian, breast, lung and other cancers) is not able to cross the BBB to a notable extent since it is a substrate of the efflux transporter P-glycoprotein. Both, biodegradable microparticles as well as small, cylindrical, glycerol tripalmitate-based implants (which can be injected using standard needles) were prepared with different paclitaxel loadings. The effects of several formulation and processing parameters on the resulting drug release kinetics were investigated in phosphate buffer pH 7.4 as well as in a diethylnicotinamide (DENA)/phosphate buffer mixture. Using DSC, SEM, SEC and optical microscopy deeper insight into the underlying drug release mechanisms could be gained. The presence of DENA in the release medium significantly increased the solubility of paclitaxel, accelerated PLGA degradation, increased the mobility of the polymer and drug molecules and fundamentally altered the geometry of the systems, resulting in increased paclitaxel release rates.
[Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/química
Neoplasias Encefálicas/tratamento farmacológico
Portadores de Fármacos
Implantes de Medicamento
Paclitaxel/química
[Mh] Termos MeSH secundário: Antineoplásicos Fitogênicos/uso terapêutico
Composição de Medicamentos
Cinética
Ácido Láctico/química
Microesferas
Niquetamida/química
Paclitaxel/uso terapêutico
Ácido Poliglicólico/química
Polímeros/química
Solubilidade
Tecnologia Farmacêutica
Triglicerídeos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents, Phytogenic); 0 (Drug Carriers); 0 (Drug Implants); 0 (Polymers); 0 (Triglycerides); 0 (polylactic acid-polyglycolic acid copolymer); 26009-03-0 (Polyglycolic Acid); 33X04XA5AT (Lactic Acid); 368IVD6M32 (Nikethamide); D133ZRF50U (tripalmitin); P88XT4IS4D (Paclitaxel)
[Em] Mês de entrada:0708
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:060224
[St] Status:MEDLINE


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[PMID]:15212332
[Au] Autor:Baek N; Lee J; Park K
[Ad] Endereço:Department of Pharmaceutics and Biomedical Engineering, Purdue University School of Pharmacy, Room G22, 575 Stadium Mall Drive, West Lafayette, IN 47907-2051, USA.
[Ti] Título:Aqueous N,N-diethylnicotinamide (DENA) solution as a medium for accelerated release study of paclitaxel.
[So] Source:J Biomater Sci Polym Ed;15(4):527-42, 2004.
[Is] ISSN:0920-5063
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:N,N-Diethylnicotinamide (DENA) was identified as an excellent hydrotropic agent for paclitaxel (PTX) in our previous studies. The aqueous solubility of PTX was increased by several orders of magnitude in the presence of DENA. Because of such a high hydrotropic property, DENA was used as a release medium providing a sink condition for the release of PTX from poly(lactic-co-glycolic acid) (PLGA) matrices. The release profiles of PTX from PLGA matrices into DENA, serum and phosphate-buffered saline (PBS) were compared. The stability of PTX in DENA and the degradation of PLGA molecules in DENA were examined. The degradation rate constant of PTX in 2 M DENA was similar to those in other aqueous solutions. The use of 2 M DENA as a release medium allowed differentiation of the release profiles of PTX from PLGA matrices made of different PLGA compositions. The PTX release from PLGA matrices was much faster in DENA solution than in serum or PBS, and the concentration of DENA affected the PTX release rate. The presence of DENA in the release medium increased the hydrolysis rate of PLGA polymers. The faster release of PTX from PLGA matrices in DENA solution may be due to the high PTX solubility and faster degradation of PLGA polymers in the presence of DENA. Our study suggests that the aqueous DENA solution can be used for the accelerated release study of PTX from PLGA matrices.
[Mh] Termos MeSH primário: Portadores de Fármacos/química
Niquetamida/farmacologia
Paclitaxel/administração & dosagem
[Mh] Termos MeSH secundário: Animais
Estabilidade de Medicamentos
Glicolatos
Cinética
Ácido Láctico
Paclitaxel/farmacocinética
Ácido Poliglicólico
Soro
Solubilidade
Soluções
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.; RESEARCH SUPPORT, U.S. GOV'T, P.H.S.
[Nm] Nome de substância:
0 (Drug Carriers); 0 (Glycolates); 0 (Solutions); 0 (polylactic acid-polyglycolic acid copolymer); 26009-03-0 (Polyglycolic Acid); 33X04XA5AT (Lactic Acid); 368IVD6M32 (Nikethamide); P88XT4IS4D (Paclitaxel)
[Em] Mês de entrada:0503
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:040624
[St] Status:MEDLINE


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[PMID]:14636718
[Au] Autor:Ooya T; Lee J; Park K
[Ad] Endereço:School of Materials Science, Japan Advanced Institute of Science and Technology, Tatsunokuchi, Ishikawa 923-1292, Japan.
[Ti] Título:Effects of ethylene glycol-based graft, star-shaped, and dendritic polymers on solubilization and controlled release of paclitaxel.
[So] Source:J Control Release;93(2):121-7, 2003 Dec 05.
[Is] ISSN:0168-3659
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:New methods and pharmaceutical compositions were developed to increase the aqueous solubility of paclitaxel (PTX), a poorly water-soluble drug. Graft and star-shaped graft polymers consisting of poly(ethylene glycol) (PEG400) graft chains increased the PTX solubility in water by three orders of magnitude. Polyglycerol dendrimers (dendriPGs) dissolved in water at high concentrations without significantly increasing the viscosity and, at 80 wt.%, were found to increase the solubility of PTX 10,000-fold. The solubilized PTX was released from graft polymers, star-shaped graft polymers, and the dendriPGs into the surrounding aqueous solution. The release rate was a function of the star shape and the dendrimer generation. The availability of the new graft, star and dendritic polymers having ethylene glycol units should permit development of novel delivery systems for other poorly water-soluble drugs.
[Mh] Termos MeSH primário: Preparações de Ação Retardada/farmacocinética
Etilenoglicol/farmacocinética
Estrutura Molecular
Paclitaxel/farmacocinética
Polímeros/farmacocinética
Solubilidade/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Bovinos
Portadores de Fármacos/farmacocinética
Etilenoglicol/química
Sangue Fetal
Glicerol/análogos & derivados
Glicerol/química
Peso Molecular
Niquetamida/química
Niquetamida/farmacocinética
Paclitaxel/sangue
Paclitaxel/química
Polietilenoglicóis/química
Polietilenoglicóis/metabolismo
Polímeros/química
Relação Quantitativa Estrutura-Atividade
Fatores de Tempo
Viscosidade/efeitos dos fármacos
Água/química
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, U.S. GOV'T, P.H.S.
[Nm] Nome de substância:
0 (Delayed-Action Preparations); 0 (Drug Carriers); 0 (Polymers); 0 (poly(ethylene glycol) methacrylate polymer); 059QF0KO0R (Water); 30IQX730WE (Polyethylene Glycols); 368IVD6M32 (Nikethamide); FC72KVT52F (Ethylene Glycol); P88XT4IS4D (Paclitaxel); PDC6A3C0OX (Glycerol)
[Em] Mês de entrada:0412
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:031126
[St] Status:MEDLINE


  9 / 268 MEDLINE  
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[PMID]:12426818
[Au] Autor:Okide GB; Odoh UE; Ajali U
[Ad] Endereço:Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences University of Nigeria, Nsukka, Nigeria.
[Ti] Título:Spectrophotometric determination of nikethamide by charge--transfer complexation with chloranilic acid.
[So] Source:Boll Chim Farm;141(4):299-303, 2002 Jul-Aug.
[Is] ISSN:0006-6648
[Cp] País de publicação:Italy
[La] Idioma:eng
[Ab] Resumo:A Spectrophotometric method is described for assay of nikethamide which was based on charge transfer complexation between it and chloranilic acid. They form a complex with stoichiometric ratio of 1:1 and showed l-max at 535 nm. Maximum complexation occurred 30 min after mixing the reactants and was stable for 12 hr. The molar absorptivity, association constant and free energy for the complex were 1.05 x 1.0(2), 4.40 x 10(-2) litre mole-1 and 1819.02 kcal respectively. Conformity to Beer's Law was within the concentration range of 1-2.5 x 10(-4), which enabled the assay of dosage forms of the drug at microquantities.
[Mh] Termos MeSH primário: Benzoquinonas/química
Estimulantes do Sistema Nervoso Central/análise
Niquetamida/análise
[Mh] Termos MeSH secundário: Dioxinas/química
Indicadores e Reagentes
Cinética
Soluções
Espectrofotometria Ultravioleta
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzoquinones); 0 (Central Nervous System Stimulants); 0 (Dioxins); 0 (Indicators and Reagents); 0 (Solutions); 290-67-5 (1,4-dioxin); 368IVD6M32 (Nikethamide); YJ8L3BB7Y4 (chloranilic acid)
[Em] Mês de entrada:0212
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:021113
[St] Status:MEDLINE


  10 / 268 MEDLINE  
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[PMID]:10776570
[Au] Autor:Bushma MI; Legon'kova LF; Zverinskii IV; Vasil'ev AV
[Ti] Título:[Disturbed functioning of enzyme systems of microsomal oxidation, glucuro-, and glutathione conjugation of xenobiotics in the liver of rats intoxicated by deoxycholate and their correction].
[Ti] Título:Narushenie funktsionirovaniia fermentnykh sistem mikrosomal'nogo okisleniia, glukuro- i glutationkon''iugatsii ksenobiotikov v pecheni krys s intoksikatsiiei dezoksikholatom i ikh korrektsiia..
[So] Source:Biull Eksp Biol Med;129(3):297-301, 2000 Mar.
[Is] ISSN:0365-9615
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Mh] Termos MeSH primário: Doença Hepática Induzida por Substâncias e Drogas/metabolismo
Ácido Desoxicólico
Glucuronídeos/metabolismo
Glutationa/metabolismo
Microssomos Hepáticos/metabolismo
Xenobióticos/metabolismo
[Mh] Termos MeSH secundário: Animais
Doença Hepática Induzida por Substâncias e Drogas/enzimologia
Doença Hepática Induzida por Substâncias e Drogas/etiologia
Colagogos e Coleréticos/farmacologia
Microssomos Hepáticos/enzimologia
Niquetamida/farmacologia
Ratos
S-Adenosilmetionina/farmacologia
Ácido Ursodesoxicólico/farmacologia
Vitamina E/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cholagogues and Choleretics); 0 (Glucuronides); 0 (Xenobiotics); 005990WHZZ (Deoxycholic Acid); 1406-18-4 (Vitamin E); 368IVD6M32 (Nikethamide); 724L30Y2QR (Ursodeoxycholic Acid); 7LP2MPO46S (S-Adenosylmethionine); GAN16C9B8O (Glutathione)
[Em] Mês de entrada:0005
[Cu] Atualização por classe:161124
[Lr] Data última revisão:
161124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:000425
[St] Status:MEDLINE



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