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Id: biblio-1283487
Autor: Kyeong Kang, Min; Park, Jin-Won.
Título: Amplification of urea detection based on pH-sensitive liposomes
Fonte: Electron. j. biotechnol;52:30-34, July. 2021. ilus, tab, graf.
Idioma: en.
Resumo: BACKGROUND: This study aimed to develop an amplification method of urea detection based on pHsensitive liposomes. RESULTS: The urease covalently immobilized on the magnetic particles and the pH-sensitive liposomes encapsulating ferricyanide were added to the cyclic-voltammeter cell solution where urea was distributed. The conversion of urea into carbonic acid seemed to induce a pH decrease that caused a reduction in the electrostatic repulsion between the headgroups of weakly acidic 1,2-dipalmitoyl-sn-glycero3-succinate. The reduction induced the liposomes to release potassium ferricyanide that was encapsulated inside. The effects of urea concentration and pH value were investigated. A specific concentration (0.5 mg/mL) of the urea solution was set to observe the response. The activity of urease was reversible with respect to the pH change between 7 and 5. The sensitivity of this detection was almost identical to the comparable techniques such as an enzyme-linked immunosorbent assay and a field-effect transistor. CONCLUSIONS: In summary, the methodology developed in this study was feasible as a portable, rapid, and sensitive method.
Descritores: Ureia/análise
Lipossomos/química
-Urease/química
Ensaio de Imunoadsorção Enzimática
Enzimas Imobilizadas
Concentração de Íons de Hidrogênio
Responsável: CL1.1 - Biblioteca Central


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ANDRADE JUNIOR, Heitor Franco de
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Id: lil-782098
Autor: Borborema, Samanta Etel Treiger; Osso Junior, João Alberto; Andrade Junior, Heitor Franco de; Nascimento, Nanci do.
Título: Antimonial drugs entrapped into phosphatidylserine liposomes: physicochemical evaluation and antileishmanial activity
Fonte: Rev. Soc. Bras. Med. Trop;49(2):196-203, Mar.-Apr. 2016. tab, graf.
Idioma: en.
Projeto: Conselho Nacional de Desenvolvimento Científico e Tecnológico.
Resumo: Abstract: INTRODUCTION: Leishmaniasis is a disease caused by the protozoan Leishmania that resides mainly in mononuclear phagocytic system tissues. Pentavalent antimonials are the main treatment option, although these drugs have toxic side effects and high resistance rates. A potentially alternative and more effective therapeutic strategy is to use liposomes as carriers of the antileishmanial agents. The aims of this study were to develop antimonial drugs entrapped into phosphatidylserine liposomes and to analyze their biological and physicochemical characteristics. METHODS: Liposomes containing meglumine antimoniate (MA) or pentavalent antimony salt (Sb) were obtained through filter extrusion (FEL) and characterized by transmission electron microscopy. Promastigotes of Leishmania infantum were incubated with the drugs and the viability was determined with a tetrazolium dye (MTT assay). The effects of these drugs against intracellular amastigotes were also evaluated by optical microscopy, and mammalian cytotoxicity was determined by an MTT assay. RESULTS: Liposomes had an average diameter of 162nm. MA-FEL showed inhibitory activity against intracellular L. infantum amastigotes, with a 50% inhibitory concentration (IC50) of 0.9μg/mL, whereas that of MA was 60μg/mL. Sb-FEL showed an IC50 value of 0.2μg/mL, whereas that of free Sb was 9μg/mL. MA-FEL and Sb-FEL had strong in vitro activity that was 63-fold and 39-fold more effective than their respective free drugs. MA-FEL tested at a ten-times higher concentration than Sb-FEL did not show cytotoxicity to mammalian cells, resulting in a higher selectivity index. CONCLUSIONS: Antimonial drug-containing liposomes are more effective against Leishmania-infected macrophages than the non-liposomal drugs.
Descritores: Compostos Organometálicos/farmacologia
Fosfatidilserinas/farmacologia
Macrófagos Peritoneais/parasitologia
Leishmania infantum/efeitos dos fármacos
Gluconato de Antimônio e Sódio/farmacologia
Meglumina/farmacologia
Antiprotozoários/farmacologia
-Compostos Organometálicos/química
Fosfatidilserinas/química
Cricetinae
Gluconato de Antimônio e Sódio/química
Concentração Inibidora 50
Testes de Sensibilidade Parasitária
Relação Dose-Resposta a Droga
Antimoniato de Meglumina
Lipossomos
Meglumina/química
Camundongos
Camundongos Endogâmicos BALB C
Antiprotozoários/química
Limites: Animais
Responsável: BR1.1 - BIREME


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Texto completo SciELO Chile
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Id: biblio-950859
Autor: Cao, Xuebing; Hou, Dongzhi; Wang, Lei; Li, Sai; Sun, Shengang; Ping, Qineng; Xu, Yan.
Título: Effects and molecular mechanism of chitosan-coated levodopa nanoliposomes on behavior of dyskinesia rats
Fonte: Biol. Res;49:1-9, 2016. ilus, graf.
Idioma: en.
Projeto: National Natural Science Foundation of China; . National Natural Science Foundation of China.
Resumo: BACKGROUND: Chitosan, the N-deacetylated derivative of chitin, is a cationic polyelectrolyte due to the presence of amino groups, one of the few occurring in nature. The use of chitosan in protein and drug delivery systems is being actively researched and reported in the literature RESULTS: In this study, we used chitosan-coated levodopa liposomes to investigate the behavioral character and the expression of phosphorylated extracellular signal-regulated kinase (ERK1/2), dopamine- and cAMP-regulated phos-phoprotein of 32 kDa (DARPP-32) and FosB/AFosB in striatum of rat model of levodopa-induced dyskinesia (LID). We found that scores of abnormal involuntary movement (AIM) decreased significantly in liposome group (P < 0.05), compared with levodopa group. Levels of phospho-ERK1/2, phospho-Thr34 DARPP-32 and FosB/AFosB in striatum decreased significantly in liposome group lesion side compared with levodopa group (P < 0.05). However, both of two groups above have significantly differences compared with the control group (P < 0.05). CONCLUSION: Chitosan-coated levodopa liposomes may be useful in reducing dyskinesias inducing for Parkinson disease. The mechanism might be involved the pathway of signaling molecular phospho-ERK1/2, phospho-Thr34 DARPP-32 and AFosB in striatum
Descritores: Dopaminérgicos/farmacologia
Levodopa/farmacologia
Proteínas Proto-Oncogênicas c-fos/metabolismo
Quitosana/farmacologia
Discinesia Induzida por Medicamentos/metabolismo
Discinesia Induzida por Medicamentos/prevenção & controle
Fosfoproteína 32 Regulada por cAMP e Dopamina/metabolismo
-Doença de Parkinson/tratamento farmacológico
Fosforilação/efeitos dos fármacos
Materiais Biocompatíveis/farmacologia
Imuno-Histoquímica
Distribuição Aleatória
Western Blotting
Reprodutibilidade dos Testes
Resultado do Tratamento
Proteínas Proto-Oncogênicas c-fos/análise
Proteínas Proto-Oncogênicas c-fos/efeitos dos fármacos
Ratos Sprague-Dawley
Corpo Estriado/efeitos dos fármacos
Sistema de Sinalização das MAP Quinases
MAP Quinases Reguladas por Sinal Extracelular/análise
MAP Quinases Reguladas por Sinal Extracelular/efeitos dos fármacos
Discinesia Induzida por Medicamentos/etiologia
Fosfoproteína 32 Regulada por cAMP e Dopamina/análise
Fosfoproteína 32 Regulada por cAMP e Dopamina/efeitos dos fármacos
Nanopartículas
Lipossomos
Limites: Animais
Masculino
Tipo de Publ: Estudo de Avaliação
Responsável: CL1.1 - Biblioteca Central


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Magalhäes, Nereide Stela Santos
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Id: biblio-973857
Autor: Ferreira, Kaline Sandrelli Amorim; Santos, Bruna Marília Alves dos; Lucena, Nelise de Paiva; Ferraz, Milena Sales; Carvalho, Rafaela de Siqueira Ferraz; Duarte Júnior, Anivaldo Pereira; Magalhães, Nereide Stela Santos; Lira, Rodrigo Pessoa Cavalcanti.
Título: Ocular delivery of moxifloxacin-loaded liposomes / Perfil de liberação ocular de lipossomas contendo moxifloxacino
Fonte: Arq. bras. oftalmol;81(6):510-513, Nov.-Dec. 2018. graf.
Idioma: en.
Resumo: ABSTRACT Purpose: To determine the release profile of moxifloxacin encapsulated in liposomes in the aqueous humor as a controlled release system for intracameral application. Methods: Liposomes containing moxifloxacin were obtained using the lipid film hydration method and were characterized by particle size and encapsulation efficiency. Female rabbits were used for the in vivo profile release study. Liposomes containing moxifloxacin was injected into the anterior chamber of the right eye of each animal. The rabbits were divided into five groups, and a sample of aqueous humor was collected 2, 4, 8, 24, and 48 h after administration of liposomes containing moxifloxacin administration. Moxifloxacin concentrations in the aqueous humor were analyzed using high-performance liquid chromatography. Results: The average size of the liposomes containing moxifloxacin was 60.5 ± 0.72 nm with a particle size distribution of 0.307. The encapsulation efficiency of moxifloxacin in liposomes was 92.24 ± 0.24%. The results of an in vivo release study of liposomes containing moxifloxacin, showed that the maximum moxifloxacin concentration was achieved within the first 2 h after administration (5.27 ± 1.09 mg/mL) and was followed by a decrease in intracameral concentration (0.35 ± 0.05 mg/mL) until the 24 h mark. Conclusions: The in vivo experiments resulted in liposomes containing moxifloxacin that were homogenous in size and exhibited high drug encapsulation efficiency. The results indicate that liposomes containing moxifloxacin offers a satisfactory aqueous humor release profile after intracameral application.

RESUMO Objetivo: Determinar o perfil de liberação, no humor aquoso, de moxifloxacino encapsulado em lipossomas como um sistema de liberação controlada para aplicação intracameral. Métodos: Lipossomas contendo moxifloxacino foram obtidos através do método de hidratação do filme lipídico e caracterizados por tamanho da partícula e eficiência de encapsulação. Utilizaram-se coelhos fêmeas foram para o estudo do perfil de liberação in vivo. Lipossomas contendo moxifloxacino foram injetados na câmara anterior do olho direito de cada animal. Os coelhos foram divididos em cinco grupos, e uma amostra de humor aquoso foi coletada 2, 4, 8, 24 e 48 h após a administração de lipossomas contendo moxifloxacino. As concentrações de moxifloxacino no humor aquoso foram analisadas usando cromatografia líquida de alta eficiência. Resultados: O tamanho médio dos lipossomas contendo moxifloxacino foi de 60,5 ± 0,72 nm com uma distribuição de tamanho de partícula de 0,307. A eficiência de encapsulação de moxifloxacino nos lipossomas foi de 92,24 ± 0,24. Os resultados de um estudo de liberação in vivo de lipossomas contendo moxifloxacino, mostraram que a concentração máxima de moxifloxacino foi atingida dentro das primeiras 2 h após sua administração (5,27 ± 1,09 mg/mL) e foi seguida de um decréscimo na concentração intracameral (0,35 ± 0,05 mg/mL) até a marca de 24 h. Conclusão: Os experimentos in vivo resultaram em lipossomas contendo moxifloxacino que eram homogêneos em tamanho e exibiam alta eficiência de encapsulação do fármaco. Os resultados indicam que lipossomas contendo moxifloxacino oferecem um perfil de liberação de humor aquoso satisfatório após a aplicação intracameral.
Descritores: Humor Aquoso
Sistemas de Liberação de Medicamentos/métodos
Moxifloxacina/administração & dosagem
Antibacterianos/administração & dosagem
-Disponibilidade Biológica
Cromatografia Líquida de Alta Pressão
Modelos Animais
Injeções Intraoculares
Moxifloxacina/análise
Moxifloxacina/farmacocinética
Lipossomos
Antibacterianos/análise
Antibacterianos/farmacocinética
Limites: Animais
Feminino
Ratos
Responsável: BR1.1 - BIREME


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Id: lil-619656
Autor: Reimão, Juliana Quero.
Título: Estudo da atividade Anti-Leishmania e Anti-Trypanosoma Cruzi de bloqueadores de canal de cálcio, furazolidona e buparvaquona: reposicionamento, associações de fármacos e formulações lipossomais / Study of the antileishmanial and Anti-Trypanosoma cruzi activity of calcium channel blockers, furazolidone and buparvaquone: drug repurposing, drug combinations and liposomal formulations.
Fonte: São Paulo; s.n; 2012. [248] p. ilus, tab, graf.
Idioma: pt.
Tese: Apresentada a São Paulo(Estado) Secretaria da Saúde. Coordenadoria de Controle de Doenças. Programa de Pós Graduação em Ciências para obtenção do grau de Doutor.
Resumo: A pesquisa de medicamentos mais eficazes e que atendam aos padrões atuais de segurança é considerada uma prioridade para o tratamento da leishmaniose e doenças de Chagas. Os principais objetivos do presente trabalho foram: avaliar a atividade anti-Leishmania in vitro e in vivo de bloqueadores de canal de cálcio (BCC) e dos fármacos buparvaquona e furazolidona; realizar combinações de BCC com os principais fármacos usados na clínica da leishmaniose visceral (LV); desenvolver formulações lipossomais de buparvaquona, furazolidona e nimodipino e desenvolver um protocolo de PCR em tempo real (qPCR) visando quantificar a carga parasitária de hamsteres infectados com L. (L.) infantum chagasi após tratamento experimental. Buparvaquona, furazolidona e doze dos treze BBC testados (anlodipino, azelnidipino, bepridil, cilnidipino, fendilina, lercanidipino, lidoflazina, mibefradil nicardipino, nifedipino, nimodipino e nitrendipino) apresentaram atividade in vitro contra diferentes espécie de Leishmania e contra Trypanosoma cruzi, com moderada a baixa citotoxicidade contra células de mamíferos. O estudo de QSAR das 1,4-diidropiridinas permitiu a predição de dois análogos com possível atividade antiprotozoária. Anlodipino, bepridil, fendilina e nimodipino não apresentaram redução na carga parasitária de hamteres infectados com...
Descritores: Modelos Animais
Combinação de Medicamentos
Doença de Chagas
Leishmaniose
Lipossomos
Reação em Cadeia da Polimerase em Tempo Real
Limites: Animais
Responsável: BR91.2 - Centro de Documentação
BR91.2; W4, R363es, 2012


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Id: lil-507806
Autor: Tempone, André Gustavo; Andrade Jr, Heitor Franco.
Título: Nanoformualations of pentavalent abtimony entrapped in phosphatidyserine-liposomes demonstrate highest efficacy aginst experimental visceral leishmaniasis
Fonte: Rev. Inst. Adolfo Lutz;67(2):131-136, maio-ago. 2008. ilus.
Idioma: en.
Resumo: Leishmaniasis is an endemic and tropical disease that afflicts mainly the developing . The limited and highly toxic therapeutic arsenal for leishmaniasis..
Descritores: Antimônio
Leishmania
Lipossomos
Responsável: BR91.2 - Centro de Documentação


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Id: biblio-969463
Autor: Ramirez, ana(edt); Ruiz, Adrian(edt); Melo, Virginia(edt); Garcia, Maritza(edt).
Título: Alternativa con gel de Papaver somniferum (amapola) y Cannabis sativa (marihuana), como tratamiento de artritis reumatoide / Alternative gel Papaver somniferum (poppy) and Cannabis sativa (marihuana), as treatment of rheumatoid arthritis
Fonte: Rev. enferm. neurol;9(1), ene-jun. 2010.
Idioma: es.
Resumo: En la elaboración del presente producto farmacéutico (una formulación galénica entre el gel y la emulsión fluida), se utilizaron dos principios activos naturales considerados psicotrópicos o narcóticos: extracto alcohólico de amapola (Papaver somniferum) y extracto alcohólico de marihuana (Cannabis sativa); éstos tienen actividad biológica conocida dentro del organismo. Son excelentes analgésicos para pacientes con cáncer terminal pero también tienen propiedades antieméticas, estimulantes del apetito, relajantes oculares, bronquíticos, ansiolíticos. Se conoce que para tener una liberación prolongada de un principio activo es muy útil el uso de liposomas; por esta razón se utilizaron liposomas de extracto alcohólico de amapola, considerando que esta planta tiene mejores propiedades analgésicas que la marihuana, por lo cual el extracto de esta última integra un 40% de la formulación.
Descritores: Papaver
Lipossomos
Limites: Humanos
Tipo de Publ: Artigo Clássico
Responsável: MX380.1 - Coordianción de Investigación en Enfermería


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Texto completo SciELO Brasil
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Id: biblio-973489
Autor: Zhao, Qiao-Hong; Zhang, Xi-Shan; Wu, Kun; Zhang, Jie; Xia, Tian-Fang; Chen, Jian; Qin, Zhen-Shen; Pang, Li-Qun.
Título: Preparation of Zoledronate liposome and its impact on apoptosis of Kupffer cells in rat liver
Fonte: Acta cir. bras;33(12):1052-1060, Dec. 2018. graf.
Idioma: en.
Projeto: Huai'an Science and Technology Bureau International Cooperation Project.
Resumo: Abstract Purpose: To establish a method for the preparation of zoledronate liposome and to observe its effect on inducing the apoptosis of rat liver Kupffer cells. Methods: Zoledronate was encapsulated in liposomes, and then the entrapment rate was detected on a spectrophotometer. The prepared Zoledronate liposome (0.01 mg/mL) was injected into the tail vein of SD rats. Three days later, the number of Kupffer cells (CD68 positive) in rat liver tissue was detected by immunohistochemistry. Flow cytometry was used to detect the apoptosis rate of the isolated liver Kupffer cell cultured in vitro. Results: The entrapment rate of Zoledronate was 43.4±7.8%. Immunohistochemistry revealed that the number of Kupffer cells was 19.3±2.1 in PBS group and 5.5±1.7 in Zoledronate liposome group, with a significant difference (P<0.05). The apoptosis rate of Kupffer cells was 4.1±0.8% in PBS group, while it was 9±2.2% and 23.3±5.9% in Zoledronate liposomes groups with different concentrations of Zoledronate liposome (P<0.05). Conclusions: Zoledronate liposomes can effectively induce the apoptosis of Kupffer cells in vivo and in vitro, and the apoptosis rate is related to the concentration of Zoledronate liposome. To establish a rat liver Kupffer cell apoptosis model can provide a new means for further study on Kupffer cell function.
Descritores: Apoptose/efeitos dos fármacos
Ácido Zoledrônico/farmacologia
Macrófagos do Fígado/efeitos dos fármacos
Fígado/citologia
-Imuno-Histoquímica
Distribuição Aleatória
Contagem de Células
Reprodutibilidade dos Testes
Resultado do Tratamento
Ratos Sprague-Dawley
Composição de Medicamentos/métodos
Citometria de Fluxo
Ácido Zoledrônico/administração & dosagem
Ácido Zoledrônico/síntese química
Lipossomos/síntese química
Limites: Animais
Masculino
Responsável: BR1.1 - BIREME


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Id: biblio-887013
Autor: AlGhamdi, Khalid M; Kumar, Ashok; Ashour, Abdelkader E; AL-Rikabi, Ammar C; AlOmrani, Abdullah Hasan; Ahamed, Shaik Shaffi.
Título: Vascular sclerosing effects of bleomycin on cutaneous veins: a pharmacopathologic study on experimental animals
Fonte: An. bras. dermatol;92(4):484-491, July-Aug. 2017. tab, graf.
Idioma: en.
Projeto: King Abdulaziz City for Science and Technology.
Resumo: Abstract: Background: Varicose veins and the complications of venous disease are common disorders in humans. Objective: To study the effects of bleomycin as a potential new sclerosing agent and its adverse events in treating varicose veins. Methods: Bleomycin-loaded liposomes 0.1ml was injected in the dorsal ear veins of white New Zealand rabbits. Sodium tetradecyl sulfate was used as a positive control. Normal saline was used as negative control. The blood vessels of the treated ears were photographed before and at one hour and two, eight and 45 days after treatment. Biopsies from the treated areas were obtained for histological examination. Blood samples were collected to determine any possible toxicity. Results: Bleomycin by itself was ineffective; therefore, liposomes were used as a vector to deliver bleomycin to the vein lumen. Subsequently, bleomycin started showing its sclerosing effects. Toxicity monitoring showed no apparent hematologic, pulmonary, hepatic or renal toxicities. This study revealed that bleomycin induced vasculitis, which led to vascular occlusion, which was observed on day 1 and day 8. No bleomycin-related injury was noted by histopathological examination of lung sections. The calculation of the lung/body weight coefficient indicated that edema was present in the experimental groups compared with the negative and positive controls. Study limitations: Relatively small number of experimental animals used. Conclusions: This study showed that bleomycin-loaded liposomes were able to induce vasculitis and vascular occlusion without any toxicity or complications. It might be useful, hence, to treat patients suffering from Varicose veins and other ectatic vascular diseases with this agent.
Descritores: Soluções Esclerosantes/farmacologia
Tetradecilsulfato de Sódio/administração & dosagem
Varizes/terapia
Bleomicina/farmacologia
Escleroterapia/métodos
Antibióticos Antineoplásicos/administração & dosagem
-Soluções Esclerosantes/administração & dosagem
Soluções Esclerosantes/efeitos adversos
Vasculite/induzido quimicamente
Vasculite/tratamento farmacológico
Veias/efeitos dos fármacos
Bleomicina/administração & dosagem
Modelos Animais de Doenças
Avaliação Pré-Clínica de Medicamentos
Injeções Intravenosas
Lipossomos
Limites: Animais
Coelhos
Responsável: BR1.1 - BIREME


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Id: biblio-1039075
Autor: Jarrar, Qais Bashir; Hakim, Muhammad Nazrul; Cheema, Manraj Singh; Zakaria, Zainul Amiruddin.
Título: In vitro characterization and in vivo performance of mefenamic acid-sodium diethyldithiocarbamate based liposomes
Fonte: Braz. J. Pharm. Sci. (Online);55:e17870, 2019. tab, graf.
Idioma: en.
Resumo: Mefenamic acid (MFA) is a hydrophobic drug with low dissolution rate. This study aimed to develop stable and reproducible aqueous formulations of MFA using liposomes as drug carriers. The drug entrapment, particles size and drug release profiles, and stability and reproducibility of the liposomes were determined. In addition, the maximum tolerated dose (MTD) was determined in rats via the oral and intraperitoneal routes of administration. Also, the anti-inflammatory efficacy of these liposomes was evaluated using carrageenan-induced paw edema model in rats. MFA-DDC based liposomes demonstrated a drug entrapment efficacy of 93.6%, particles size of 170.9 nm, and polydispersity index of 0.24 which were not statistically affected when stored in room and refrigerated temperatures for at least 4 weeks. The MTD of the intraperitoneally administrated MFA-loaded liposomes was 20 mg MFA/kg, whereas for those of oral administrations, it was up to 80 mg MFA/kg. Intraperitoneal dose (80 mg MFA/kg) of MFA-DDC liposomes induced extrapyramidal symptoms associated with significant elevation in serum potassium and muscle enzymes. Moreover, significant inhibition of paw edema was demonstrated by the oral and intraperitoneal routes. These findings suggest that MFA-DDC based liposomes are an effective formulation of MFA and recommend the use of bioequivalence assessments with commercial formulations.
Descritores: Ácido Mefenâmico/análise
Ditiocarb/análise
Lipossomos/agonistas
-Técnicas In Vitro
Carragenina
Limites: Animais
Feminino
Ratos
Responsável: BR40.1 - DBD - Divisão de Biblioteca e Documentacão do Conjunto das Químicas



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