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Pesquisa : B01.050.150.900.649.313.992.635.505.700.550.408 [Categoria DeCS]
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[PMID]:29190552
[Au] Autor:Jiang Q; Yu S; Li X; Ma C; Li A
[Ad] Endereço:Department of Anesthesiology, Huaihe Hospital of Henan University, Kaifeng, Henan, China.
[Ti] Título:Evaluation of local anesthetic effects of Lidocaine-Ibuprofen ionic liquid stabilized silver nanoparticles in Male Swiss mice.
[So] Source:J Photochem Photobiol B;178:367-370, 2018 Jan.
[Is] ISSN:1873-2682
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:A simple approach for the synthesis of Lidocaine-Ibuprofen ionic liquid stabilized silver nanoparticles (IL-AgNPs) was reported in this work. The shape, size and surface morphology of the Lidocaine-Ibuprofen ionic liquid stabilized AgNPs were characterized by using spectroscopic and microscopic techniques such as Ultraviolet-visible spectroscopy (UV-Visible), X-ray diffraction (XRD) analysis, Selected area electron diffraction (SAED), Transmission electron microscopy (TEM). TEM analysis showed the formation of 20-30nm size of IL-AgNPs with very clear lattice fringes. SAED pattern confirmed the highly crystalline nature of fabricated IL stabilized AgNPs. EDS results confirmed the formation of nanosilver. The fabricated IL-AgNPs were studied for their local anesthetic effect in rats. The results of local anesthetic effect showed that the time for onset of action by IL-AgNPs is 10min, which is significantly higher than that for EMLA. Further, tactile test results confirmed the stronger and faster local anesthetic effect of IL-AgNPs when compared to that of EMLA.
[Mh] Termos MeSH primário: Ibuprofeno/química
Líquidos Iônicos/química
Lidocaína/química
Nanopartículas Metálicas/química
Prata/química
[Mh] Termos MeSH secundário: Anestésicos/química
Anestésicos/farmacologia
Animais
Ibuprofeno/farmacologia
Lidocaína/farmacologia
Masculino
Nanopartículas Metálicas/toxicidade
Camundongos
Microscopia Eletrônica de Transmissão
Limiar da Dor/efeitos dos fármacos
Tamanho da Partícula
Ratos
Ratos Pelados
Espectrofotometria Ultravioleta
Difração de Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anesthetics); 0 (Ionic Liquids); 3M4G523W1G (Silver); 98PI200987 (Lidocaine); WK2XYI10QM (Ibuprofen)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180212
[Lr] Data última revisão:
180212
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171201
[St] Status:MEDLINE


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[PMID]:28506834
[Au] Autor:Sugino M; Hatanaka T; Todo H; Mashimo Y; Suzuki T; Kobayashi M; Hosoya O; Jinno H; Juni K; Sugibayashi K
[Ad] Endereço:Faculty of Pharmaceutical Sciences, Josai University, 1-1 Keyakidai, Sakado, Saitama 350-0295, Japan.
[Ti] Título:Safety evaluation of dermal exposure to phthalates: Metabolism-dependent percutaneous absorption.
[So] Source:Toxicol Appl Pharmacol;328:10-17, 2017 Aug 01.
[Is] ISSN:1096-0333
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Phthalates, known as reproductive toxicants and endocrine disruptors, are widely used as plasticizers in polyvinyl chloride products. The present study was conducted for risk identification of dermal exposure to phthalates. When dibutyl phthalate was applied to the skin of hairless rats and humans, only monobutyl phthalate appeared through the skin, and the permeability of the skin was higher than that after the application of the monoester directly. The inhibition of skin esterases made the skin impermeable to the metabolite following dermal exposure to dibutyl ester, whereas removal of the stratum corneum from the skin did not change the skin permeation behavior. Similar phenomena were observed for benzyl butyl phthalate. The skin permeability of monobenzyl phthalate was higher than that of monobutyl phthalate in humans, although the reverse was observed in rats. Species difference in skin permeation profile corresponded to the esterase activity of the skin homogenate. Di(2-ethylhexyl) phthalate, which was not metabolized by esterases in the skin, was not transported across the skin. These results suggest that highly lipophilic phthalates may be transported easily across the stratum corneum lipids. The water-rich viable layer may become permeable to these phthalates by their metabolism into monoesters, which are relatively hydrophilic. Skin metabolism is essential to the percutaneous absorption of phthalates. Because esterase activity has large inter-individual differences, further study will be needed for individual risk identification of dermal exposure to phthalates.
[Mh] Termos MeSH primário: Poluentes Ambientais/toxicidade
Ácidos Ftálicos/toxicidade
Absorção Cutânea
[Mh] Termos MeSH secundário: Animais
Dibutilftalato
Dietilexilftalato/administração & dosagem
Dietilexilftalato/farmacocinética
Dietilexilftalato/toxicidade
Exposição Ambiental
Poluentes Ambientais/farmacocinética
Esterases/antagonistas & inibidores
Feminino
Seres Humanos
Técnicas In Vitro
Masculino
Meia-Idade
Ácidos Ftálicos/administração & dosagem
Ácidos Ftálicos/farmacocinética
Plastificantes/administração & dosagem
Plastificantes/farmacocinética
Plastificantes/toxicidade
Ratos
Ratos Pelados
Medição de Risco
Pele/enzimologia
Especificidade da Espécie
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Environmental Pollutants); 0 (Phthalic Acids); 0 (Plasticizers); 2286E5R2KE (Dibutyl Phthalate); C42K0PH13C (Diethylhexyl Phthalate); EC 3.1.- (Esterases); YPC4PJX59M (butylbenzyl phthalate); ZI46LWZ45G (monobutyl phthalate)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170517
[St] Status:MEDLINE


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[PMID]:27836753
[Au] Autor:Monti D; Egiziano E; Burgalassi S; Chetoni P; Chiappe C; Sanzone A; Tampucci S
[Ad] Endereço:Department of Pharmacy, University of Pisa, Via Bonanno 33, I-56126, Pisa, Italy. Electronic address: daniela.monti@unipi.it.
[Ti] Título:Ionic liquids as potential enhancers for transdermal drug delivery.
[So] Source:Int J Pharm;516(1-2):45-51, 2017 Jan 10.
[Is] ISSN:1873-3476
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The aim of this study was to verify the effect of several cyclic onium based ionic liquids (ILs), including mono- and dicationic derivatives of 1,4-diazabicyclo[2.2.2]octane (DABCO), a dialkyl morpholinium salt and a Brønsted acidic IL, as enhancers of the in vitro transdermal permeation and skin retention of diltiazem through and into hairless rat skin. The drug was used as both the hydrochloride salt (DZHCl) and the free base (DZB) to highlight the relationship between the enhancement effect and the physico-chemical characteristics of the active agent. Permeation tests were carried out using Gummer-type diffusion cells and excised rat skin with a 0.005M aqueous solution of diltiazem hydrochloride or diltiazem free base with and without the addition of 1% w/w ionic liquids. At the end of the permeation experiments with diltiazem hydrochloride, a suitable extraction procedure allowed for the determination of the drug content retained in the skin. Depending on the ionic liquid structure, a significant enhancement in diltiazem hydrochloride levels in the receiving phase was observed, and the transdermal permeation of the diltiazem free base was markedly increased by treatment with all of the ionic liquids. N-dodecyldabco bromide was the best enhancer for both salified and free base drug forms, even though it showed a certain toxicity. On the other hand, N-methyl-N-decylmorpholinium bromide showed a good balance between enhancer activity and cytotoxicity.
[Mh] Termos MeSH primário: Bloqueadores dos Canais de Cálcio/administração & dosagem
Diltiazem/administração & dosagem
Sistemas de Liberação de Medicamentos
Líquidos Iônicos/química
[Mh] Termos MeSH secundário: Administração Cutânea
Animais
Bloqueadores dos Canais de Cálcio/farmacocinética
Química Farmacêutica/métodos
Diltiazem/farmacocinética
Excipientes/química
Masculino
Permeabilidade
Ratos
Ratos Pelados
Pele/metabolismo
Absorção Cutânea
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Calcium Channel Blockers); 0 (Excipients); 0 (Ionic Liquids); EE92BBP03H (Diltiazem)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170509
[Lr] Data última revisão:
170509
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161113
[St] Status:MEDLINE


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[PMID]:27644893
[Au] Autor:Flo A; Cambras T; Díez-Noguera A; Calpena A
[Ad] Endereço:Departament de Farmàcia i Tecnologia Farmacèutica, Facultat de Farmàcia i Ciències de la Alimentació, Universitat de Barcelona, Av. Joan XXIII s/n, 08028 Barcelona, Spain.
[Ti] Título:Melatonin pharmacokinetics after transdermal administration changes according to the time of the day.
[So] Source:Eur J Pharm Sci;96:164-170, 2017 Jan 01.
[Is] ISSN:1879-0720
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Melatonin is a neurohormone with multiple and different actions, such as chronobiotic or antioxidant. Melatonin is usually orally administered, but dermal administration is also useful in dermatological diseases or as adjuvant to certain skin treatments. Here, we studied the variability of the pharmacokinetics of melatonin and its metabolite AFMK, when melatonin is transdermally administered to Hairless rat at two different times of day (Zeitgeber Time 4 (ZT4) and ZT16). Moreover, in order to obtain the bioavailability, kinetics after intravenous administration was also studied. In addition, a permeation study was carried out, at both ZTs, to test the amount of melatonin retained in the skin after transdermal administration. Results showed that pharmacokinetic parameters of melatonin administered exogenously depended on the time of the day. When intravenous data were fitted to a compartmental model, the extrapolated plasma concentration at time 0 and the area under the curve were higher at ZT4, while clearance, volumes of central and peripheral compartments and volume of distribution at the steady state were higher at ZT16. Transdermal administration was best fitted to a one-compartment model and t , half-life of absorption and area under the curve showed higher values at ZT4, while the absorption rate and constant of absorption were higher at ZT16. AFMK was detected in all cases, but no differences between the two ZTs were observed. Transdermal administration showed better bioavailability also at ZT4. Results indicate that time of day is a variable that should be taken into account when melatonin is transdermally administered.
[Mh] Termos MeSH primário: Melatonina/administração & dosagem
Melatonina/farmacocinética
[Mh] Termos MeSH secundário: Administração Cutânea
Animais
Antioxidantes/administração & dosagem
Antioxidantes/farmacocinética
Disponibilidade Biológica
Fenômenos Cronobiológicos
Cronoterapia Farmacológica
Meia-Vida
Injeções Intravenosas
Masculino
Melatonina/sangue
Modelos Biológicos
Ratos Pelados
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); JL5DK93RCL (Melatonin)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170904
[Lr] Data última revisão:
170904
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160921
[St] Status:MEDLINE


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[PMID]:27521610
[Au] Autor:Matsumoto M; Todo H; Akiyama T; Hirata-Koizumi M; Sugibayashi K; Ikarashi Y; Ono A; Hirose A; Yokoyama K
[Ad] Endereço:Division of Risk Assessment, National Institute of Health Sciences, Tokyo, Japan; Department of Epidemiology and Environmental Health, Juntendo University, Faculty of Medicine, Tokyo, Japan. Electronic address: mariko@nihs.go.jp.
[Ti] Título:Risk assessment of skin lightening cosmetics containing hydroquinone.
[So] Source:Regul Toxicol Pharmacol;81:128-135, 2016 Nov.
[Is] ISSN:1096-0295
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Following reports on potential risks of hydroquinone (HQ), HQ for skin lightening has been banned or restricted in Europe and the US. In contrast, HQ is not listed as a prohibited or limited ingredient for cosmetic use in Japan, and many HQ cosmetics are sold without restriction. To assess the risk of systemic effects of HQ, we examined the rat skin permeation rates of four HQ (0.3%, 1.0%, 2.6%, and 3.3%) cosmetics. The permeation coefficients ranged from 1.2 × 10 to 3.1 × 10 cm/s, with the highest value superior than the HQ aqueous solution (1.6 × 10 cm/s). After dermal application of the HQ cosmetics to rats, HQ in plasma was detected only in the treatment by highest coefficient cosmetic. Absorbed HQ levels treated with this highest coefficient cosmetic in humans were estimated by numerical methods, and we calculated the margin of exposure (MOE) for the estimated dose (0.017 mg/kg-bw/day in proper use) to a benchmark dose for rat renal tubule adenomas. The MOE of 559 is judged to be in a range safe for the consumer. However, further consideration may be required for regulation of cosmetic ingredients.
[Mh] Termos MeSH primário: Hidroquinonas/toxicidade
Absorção Cutânea
Preparações Clareadoras de Pele/toxicidade
Pigmentação da Pele/efeitos dos fármacos
Pele/metabolismo
Testes de Toxicidade/métodos
[Mh] Termos MeSH secundário: Administração Cutânea
Administração Intravenosa
Animais
Benchmarking
Simulação por Computador
Relação Dose-Resposta a Droga
Seres Humanos
Hidroquinonas/administração & dosagem
Hidroquinonas/sangue
Hidroquinonas/farmacocinética
Masculino
Modelos Teóricos
Nível de Efeito Adverso não Observado
Permeabilidade
Ratos Pelados
Medição de Risco
Preparações Clareadoras de Pele/administração & dosagem
Preparações Clareadoras de Pele/metabolismo
Testes de Toxicidade/normas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Hydroquinones); 0 (Skin Lightening Preparations); XV74C1N1AE (hydroquinone)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170324
[Lr] Data última revisão:
170324
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160814
[St] Status:MEDLINE


  6 / 151 MEDLINE  
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[PMID]:27477646
[Au] Autor:Goto N; Morita Y; Terada K
[Ad] Endereço:Honjo Reserch Section Drug Development Technology Center, Customer Joy Department Eisai Japan, Eisai Co., Ltd.
[Ti] Título:Deposits from Creams Containing 20% (w/w) Urea and Suppression of Crystallization (Part 2): Novel Analytical Methods of Urea Accumulated in the Stratum Corneum by Tape stripping and Colorimetry.
[So] Source:Chem Pharm Bull (Tokyo);64(8):1092-8, 2016.
[Is] ISSN:1347-5223
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:The transfer of urea from a urea formulation to the stratum corneum varies with the formulation base and form, and impacts the formulation's therapeutic effect. Consequently, determining the amount of urea transferred is essential for developing efficient formulations. This study assessed a simple method for measuring the amount of urea accumulated in the stratum corneum. Conventional methods rely on labeling urea used in the formulation with radiocarbon ((14)C) or other radioactive isotopes (RIs), retrieving the transferred urea from the stratum corneum by tape stripping, then quantitating the urea. The handling and use of RIs, however, is subject to legal regulation and can only be performed in sanctioned facilities, so methods employing RIs are neither simple nor convenient. We therefore developed a non-radiolabel method "tape stripping-colorimetry (T-C)" that combines tape stripping with colorimetry (urease-glutamate dehydrogenase (GLDH)) for the quantitative measurement of urea. Urea in the stratum corneum is collected by tape stripping and measured using urease-GLDH, which is commonly used to measure urea nitrogen in blood tests. The results indicate that accurate urea measurement by the T-C method requires the application of 1400 mg (on hairless rats) of a 20% urea solution on a 50 cm(2) (5×10 cm) area. Further, we determined the amount of urea accumulated in the stratum corneum using formulations with different urea concentrations, and the time course of urea accumulation from formulations differing in the rate of urea crystallization. We demonstrate that the T-C method is simple and convenient, with no need for (14)C or other RIs.
[Mh] Termos MeSH primário: Colorimetria/métodos
Epiderme/química
Creme para a Pele/química
Ureia/análise
[Mh] Termos MeSH secundário: Animais
Química Farmacêutica
Cristalização
Epiderme/metabolismo
Glutamato Desidrogenase/metabolismo
Masculino
Ratos
Ratos Pelados
Ureia/metabolismo
Urease/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
8W8T17847W (Urea); EC 1.4.1.2 (Glutamate Dehydrogenase); EC 3.5.1.5 (Urease)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170202
[Lr] Data última revisão:
170202
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160802
[St] Status:MEDLINE
[do] DOI:10.1248/cpb.c15-00784


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[PMID]:27166538
[Au] Autor:Ahad HA; Ishaq BM; Shaik M; Bandagisa F
[Ad] Endereço:Department of Pharmaceutics, Balaji College of pharmacy, Anantapur, Andhra Pradesh, India.
[Ti] Título:Designing and characterizing of tramadol hydrochloride transdermal patches prepared with Ficus carica fruit mucilage and povidone.
[So] Source:Pak J Pharm Sci;29(3):945-51, 2016 May.
[Is] ISSN:1011-601X
[Cp] País de publicação:Pakistan
[La] Idioma:eng
[Ab] Resumo:The purpose of this investigation was to prepare matrix type transdermal patches of Tramadol HCl using various ratios of Ficus carica fruit mucilage and Povidone. The matrix type transdermal patches were prepared using Tramadol HCl with Ficus carica fruit mucilage and Povidone. The interactions between Tramadol HCl with F. carica fruit mucilage and Povidone were performed by Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared spectroscopy (FTIR). The prepared patches were examined for physicochemical characterization and in vitro drug permeation studies (using a Keshary-Chien diffusion cell across hairless Albino rat skin), skin irritation studies and accelerated stability studies. The drug was found to be free from negligible interactions with the polymers used. The formulated patches possessed satisfactory physicochemical properties, in vitro drug permeation and devoid of serious skin irritation. The selected formulation (F-5) was retains the characteristics even after the accelerated environmental conditions. The study concludes that F. carica fruit mucilage with Povidone is a good combination for preparing transdermal patches.
[Mh] Termos MeSH primário: Adesivos/química
Analgésicos Opioides/administração & dosagem
Portadores de Fármacos
Ficus/química
Povidona/química
Tramadol/administração & dosagem
Adesivo Transdérmico
[Mh] Termos MeSH secundário: Adesivos/isolamento & purificação
Administração Cutânea
Analgésicos Opioides/química
Analgésicos Opioides/metabolismo
Animais
Varredura Diferencial de Calorimetria
Química Farmacêutica
Difusão
Estabilidade de Medicamentos
Frutas
Cinética
Microscopia Eletrônica de Varredura
Modelos Biológicos
Permeabilidade
Coelhos
Ratos
Ratos Pelados
Pele/metabolismo
Absorção Cutânea
Solubilidade
Espectroscopia de Infravermelho com Transformada de Fourier
Tecnologia Farmacêutica/métodos
Tramadol/química
Tramadol/metabolismo
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adhesives); 0 (Analgesics, Opioid); 0 (Drug Carriers); 39J1LGJ30J (Tramadol); FZ989GH94E (Povidone)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160512
[St] Status:MEDLINE


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[PMID]:27126240
[Au] Autor:Miller DL; Lu X; Fabiilli M; Fields K; Dou C
[Ad] Endereço:Department of Radiology, University of Michigan Health System, Ann Arbor, Michigan, USA. Electronic address: douglm@umich.edu.
[Ti] Título:Frequency Dependence of Petechial Hemorrhage and Cardiomyocyte Injury Induced during Myocardial Contrast Echocardiography.
[So] Source:Ultrasound Med Biol;42(8):1929-41, 2016 08.
[Is] ISSN:1879-291X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Myocardial contrast echocardiography (MCE) for perfusion imaging can induce microscale bio-effects during intermittent high-Mechanical Index scans. The dependence of MCE-induced bio-effects on the ultrasonic frequency was examined in rats at 1.6, 2.5 and 3.5 MHz. Premature complexes were counted in the electrocardiogram, petechial hemorrhages with microvascular leakage on the heart surface were observed at the time of exposure, plasma troponin elevation was measured after 4 h and cardiomyocyte injury was detected at 24 h. Increasing response to exposure above an apparent threshold was observed for all endpoints at each frequency. The effects decreased with increasing ultrasonic frequency, and the thresholds increased. Linear regressions for frequency-dependent thresholds indicated coefficients and exponents of 0.6 and 1.07 for petechial hemorrhages, respectively, and 1.02 and 0.8 for cardiomyocyte death, compared with 1.9 and 0.5 (square root) for the guideline limit of the mechanical index. The results clarify the dependence of cardiac bio-effects on frequency, and should allow development of theoretical descriptions of the phenomena and improved safety guidance for MCE.
[Mh] Termos MeSH primário: Morte Celular
Meios de Contraste
Ecocardiografia/efeitos adversos
Hemorragia/etiologia
Miócitos Cardíacos/patologia
[Mh] Termos MeSH secundário: Animais
Modelos Animais de Doenças
Masculino
Púrpura/etiologia
Ratos
Ratos Pelados
Troponina/sangue
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Contrast Media); 0 (Troponin)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171109
[Lr] Data última revisão:
171109
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160430
[St] Status:MEDLINE


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[PMID]:26934927
[Au] Autor:Hazama Y; Maekawa T; Miki R; Oshima S; Egawa Y; Morimoto K; Seki T
[Ad] Endereço:Faculty of Pharmaceutical Sciences, Josai University.
[Ti] Título:Effect of Physiological Changes in the Skin on Systemic Absorption of Tacrolimus Following Topical Application in Rats.
[So] Source:Biol Pharm Bull;39(3):343-52, 2016.
[Is] ISSN:1347-5215
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Tacrolimus (TL) ointment is a topical treatment for atopic dermatitis, a disease that exhibits various skin conditions. The effect of skin pathologies on the systemic absorption of TL and related side effects remains unknown. This study aimed to investigate factors affecting the cutaneous absorption of TL. We prepared various skin models in hairless rats by tape stripping, injection of prophlogistic material solution (PMS), and continuous subcutaneous adrenaline (Adr) infusion. In vivo absorption studies were conducted, with measurements of transepidermal water loss (TEWL) and skin blood flow as physiological parameters. Very little TL absorption was observed through intact skin. Greater TL absorption was noted in skins with high TEWL values and fully stripped skin with PMS injections. In contrast, Adr infusion, which reduced skin blood flow, resulted in decreased TL absorption through fully stripped skin. Combined use of TL and Adr on skin with PMS injections resulted in suppression of TL absorption. Our results revealed that TL absorption following topical application is affected by alterations in the skin barrier, blood flow, and vascular permeability. We propose an administration plan for TL in a flowchart as a means of preventing systemic side effects.
[Mh] Termos MeSH primário: Imunossupressores/farmacocinética
Pele/metabolismo
Tacrolimo/farmacocinética
[Mh] Termos MeSH secundário: Administração Tópica
Animais
Capilares/efeitos dos fármacos
Capilares/fisiologia
Epinefrina/farmacologia
Imunossupressores/sangue
Masculino
Ratos Pelados
Fluxo Sanguíneo Regional/efeitos dos fármacos
Pele/irrigação sanguínea
Pele/efeitos dos fármacos
Absorção Cutânea/efeitos dos fármacos
Fenômenos Fisiológicos da Pele/efeitos dos fármacos
Tacrolimo/sangue
Vasoconstrição/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Immunosuppressive Agents); WM0HAQ4WNM (Tacrolimus); YKH834O4BH (Epinephrine)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160304
[St] Status:MEDLINE
[do] DOI:10.1248/bpb.b15-00727


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[PMID]:26928401
[Au] Autor:Modepalli N; Shivakumar HN; McCrudden MT; Donnelly RF; Banga A; Murthy SN
[Ad] Endereço:The University of Mississippi School of Pharmacy, Mississippi 38677.
[Ti] Título:Transdermal Delivery of Iron Using Soluble Microneedles: Dermal Kinetics and Safety.
[So] Source:J Pharm Sci;105(3):1196-200, 2016 Mar.
[Is] ISSN:1520-6017
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Currently, the iron compounds are administered via oral and parenteral routes in patients of all ages, to treat iron deficiency. Despite continued efforts to supplement iron via these conventional routes, iron deficiency still remains the most prevalent nutritional disorder all over the world. Transdermal replenishment of iron is a novel, potential approach of iron replenishment. Ferric pyrophosphate (FPP) was found to be a suitable source of iron for transdermal replenishment. The safety of FPP was assessed in this project by challenging the dermal fibroblast cells with high concentration of FPP. The cell viability assay and reactive oxygen species assay were performed. The soluble microneedle array was developed, incorporated with FPP and the kinetics of free iron in the skin; extracellular fluid following dermal administration of microneedle array was investigated in hairless rats. From the cell based assays, FPP was selected as one of the potential iron sources for transdermal delivery. The microneedles were found to dissolve in the skin fluid within 3 hours of administration. The FPP concentration in the dermal extracellular fluid declined after complete dissolution of the microneedle array. Overall, the studies demonstrated the safety of FPP for dermal delivery and the feasibility of soluble microneedle approach for transdermal iron replenishment therapy.
[Mh] Termos MeSH primário: Difosfatos/administração & dosagem
Difosfatos/efeitos adversos
Sistemas de Liberação de Medicamentos/efeitos adversos
Ferro/administração & dosagem
Ferro/efeitos adversos
Absorção Cutânea/efeitos dos fármacos
Pele/efeitos dos fármacos
[Mh] Termos MeSH secundário: Administração Cutânea
Animais
Sobrevivência Celular/efeitos dos fármacos
Sistemas de Liberação de Medicamentos/métodos
Fibroblastos/efeitos dos fármacos
Seres Humanos
Cinética
Microinjeções/efeitos adversos
Microinjeções/métodos
Agulhas/efeitos adversos
Ratos
Ratos Pelados
Espécies Reativas de Oxigênio/metabolismo
Segurança
Pele/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Diphosphates); 0 (Reactive Oxygen Species); E1UOL152H7 (Iron); QK8899250F (ferric pyrophosphate)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:170301
[Lr] Data última revisão:
170301
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160302
[St] Status:MEDLINE



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