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Id: biblio-1283652
Autor: Zhi, Kaining; Lebo, David B.
Título: A preformulation strategy for the selection of controlled-release components to simulate a subcutaneous implant / Una estrategia de preformulación para la selección de componentes de liberación controlada para simular un implante subcutáneo
Fonte: Bol. latinoam. Caribe plantas med. aromát;19(4):344-356, 2020. tab, ilus.
Idioma: en.
Resumo: Many chronic diseases require repetitive injections as maintenance treatment. It is therefore important to investigate a possible alternative. A simulated subcutaneous implant prototype was fabricated as a polymer matrix covered by cylinder-shape tubing having a porous membrane. Sucrose, bovine serum albumin, and gelatin were selected as matrix excipients. Eight APIs with different physiochemical properties were used to investigate the releasing mechanism. Drug release was tested through an in vitrodissolution apparatus. Drug release of eight APIs followed zero-order kinetics with a minimum 12-hour duration. Release rates also showed linear correlations with the APIs' solubilities under physiological pH. For releasing mechanism studies, different combinations of matrix and membrane were investigated in detail. A 144-hour continuous zero-order release of caffeine was achieved as the best controlled simulated prototype. The results showed that drug release of our simulated prototype was primarily achieved by drug diffusion rather than dissolution.

Muchas enfermedades crónicas requieren inyecciones repetitivas como tratamiento de mantenimiento. Por lo tanto, es importante investigar una posible alternativa. Se fabricó un prototipo de implante subcutáneo simulado a partir de una matriz de polímero cubierta por un tubo en forma de cilindro que tiene una membrana porosa. La sacarosa, la albúmina de suero bovino y la gelatina se seleccionaron como excipientes matriciales. Se utilizaron ocho APIs con diferentes propiedades fisicoquímicas para investigar el mecanismo de liberación. La liberación del fármaco se probó a través de un aparato de disolución in vitro. La liberación del fármaco de las ocho APIs siguió una cinética de orden cero con una duración mínima de 12 horas. Las tasas de liberación también mostraron correlaciones lineales con las solubilidades de las APIs a pH fisiológico. Para los estudios de mecanismos de liberación, se investigaron en detalle diferentes combinaciones de matriz y membrana. El prototipo simulado con mejor control logró una liberación continua de cafeína de orden cero durante 144 horas. Los resultados mostraron que la liberación del fármaco del prototipo simulado ocurrió principalmente mediante la difusión del fármaco en lugar de la disolución.
Descritores: Preparações Farmacêuticas/administração & dosagem
Implantes de Medicamento/metabolismo
-Técnicas In Vitro
Projetos Piloto
Simulação
Cromatografia Líquida de Alta Pressão
Tela Subcutânea
Preparações de Ação Retardada
Avaliação Pré-Clínica de Medicamentos
Liberação Controlada de Fármacos
Liofilização
Responsável: CL1.1 - Biblioteca Central


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Id: biblio-906735
Autor: Silva, Guilherme Barreto Garneiro; Costa Junior, José de Ribamar; Sousa, Amanda; Sousa, José Eduardo; Abizaid, Alexandre.
Título: Stents farmacológicos: estado atual / Drug-eluting stents: state-of-the-art
Fonte: Rev. Soc. Cardiol. Estado de Säo Paulo;28(1):54-59, jan.-mar. 2018. ilus.
Idioma: en; pt.
Resumo: Stents farmacológicos foram desenvolvidos para reduzir a resposta proliferativa neointimal e consequentemente a reestenose, mais frequente limitação da intervenção coronária percutânea com balão e stents não faramcológicos. O desenvolvimento destes dispositivos baseia-se no maior entendimento da biologia da reestenose, na seleção de fármacos anti-proliferativos adequados para os diversos mecanismos envolvidos nesta complicação e no uso de plataformas/polímeros adequados para entrega do fármaco. Consequentemente o desempenho destes dispositivos depende da perfeita interação de todos estes elementos. As abordagens atuais para minimizar a reestenose são revisados neste capítulo. Embora a primeira geração dos stents farmacológicos tenha sido focada na eficácia em reduzir a reestenose, questões relacionadas à sua segurança surgiram, comprometendo seu uso mais disseminado. As novas gerações de stents farmacológicos com polímeros duráveis ou bioabsorvíveis conseguiu reduzir as taxas de nova intervenção e de trombose. Embora o modelo ideal de stent farmacológico ainda esteja em investigação, é certo que esta tecnologia já se estabeleceu como primeira linha na intervenção coronária percutânea contemporânea
Descritores: Polímeros/uso terapêutico
Sirolimo
Reestenose Coronária
Stents Farmacológicos
-Doença da Artéria Coronariana
Stents
Liberação Controlada de Fármacos/efeitos dos fármacos
Everolimo
Revascularização Miocárdica/métodos
Limites: Humanos
Masculino
Feminino
Tipo de Publ: Revisão
Responsável: BR44.1 - Serviço de Biblioteca, Documentação Científica e Didática Prof. Dr. Luiz Venere Décourt


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Id: biblio-1285516
Autor: Saraçoglu, Özlem Kislal; Uludag, Mecit Orhan; Özdemir, Elif Derya; Degim, Ismail Tuncer.
Título: Development of controlled release dexketoprofen tablets and prediction of drug release using Artificial Neural Network (ANN) modelling
Fonte: Braz. J. Pharm. Sci. (Online);56:e18540, 2020. tab, graf.
Idioma: en.
Resumo: Dexketoprofen trometamol (DT) is an active S (+) enantiomer of ketoprofen, and a non-steroidal anti-inflammatory agent. DT has a short biological half-life and the dosing interval is quite short when there is a need to maintain the desirable effect for longer time periods. Consequently, a controlled release DT tablet was designed for oral administration aiming to minimize the number of doses and the possible side effects. Calculations of the parameters for controlled release DT tablets were shown clearly. Controlled release matrix-type tablet formulations were prepared using hydroxypropyl methylcellulose (HPMC) (low and high viscosity), Eudragit RS and Carbopol, and the effects of different polymers on DT release from the tablet formulations were investigated. The dissolution rate profiles were compared and analyzed kinetically. An Artificial Neural Network (ANN) model was developed to predict drug release and a successful model was obtained. Subsequently, an optimum formulation was selected and evaluated in terms of its analgesic and anti-inflammatory activity. Although the developed controlled release tablets did not have an initial dose, they were found to be as effective as commercially available tablets on the market. Dissolution and in vivo studies have shown that the prepared tablets were able to release DT for longer time periods, making the tablets more effective, convenient and more tolerable.
Descritores: Comprimidos/análise
Trometamina/efeitos adversos
Administração Oral
-Anti-Inflamatórios não Esteroides/efeitos adversos
Cetoprofeno/agonistas
Dosagem/efeitos adversos
Liberação Controlada de Fármacos/efeitos dos fármacos
Analgésicos/farmacocinética
Responsável: BR40.1 - DBD - Divisão de Biblioteca e Documentacão do Conjunto das Químicas


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Id: biblio-1249174
Autor: Karimi, Maryam; Karimian, Khashayar; Heli, Hossein.
Título: A nanoemulsion-based delivery system for imatinib and in vitro anticancer efficacy
Fonte: Braz. J. Pharm. Sci. (Online);56:e18973, 2020. graf.
Idioma: en.
Projeto: Research Council of Shiraz University of Medical Sciences.
Resumo: A self-nanoemulsifying drug delivery system (SNEDDS) composed of ethyl oleate, Tween 80 and polyethylene glycol 600 was prepared as a new route to improve the efficacy of imatinib. The drug-loaded SNEDDS formed nanodroplets of ethyl oleate stabilized by Tween 80 and polyethylene glycol 600 with a diameter of 81.0±9.5 nm. The nanoemulsion-based delivery system was stable for at least two months, with entrapment efficiency and loading capacity of 16.4±0.1 and 48.3±0.2%, respectively. Imatinib-loaded SNEDDS was evaluated for the drug release profiles, and its effectiveness against MCF-7 cell line was investigated. IC50 values for the imatinib-loaded SNEDDS and an imatinib aqueous solution were 3.1 and 6.5 µg mL-1, respectively.
Descritores: Técnicas In Vitro/métodos
Eficácia/classificação
Mesilato de Imatinib/efeitos adversos
-Polietilenoglicóis/análise
Concentração Inibidora 50
Células MCF-7/classificação
Liberação Controlada de Fármacos/efeitos dos fármacos
Responsável: BR40.1 - DBD - Divisão de Biblioteca e Documentacão do Conjunto das Químicas


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Id: biblio-1150986
Autor: Andueza Galeno, Isabel Cecilia.
Título: Desarrollo de un nanosistema para la liberación de fármacos intravítreo / Development of intravitreal nanosistema for drugs release.
Fonte: Caracas; s.n; oct. 2012. ilus, tab, graf.
Idioma: es.
Tese: Apresentada a Universidad Central de Venezuela. Facultad de Farmacia para obtenção do grau de Doctor.
Resumo: La inyección intravítrea ha sido la vía de administración más eficaz para el tratamiento de enfermedades vitreorretinianas. Su práctica continua, no es agradable para los pacientes y a su vez podría causar complicaciones indeseadas. El presente trabajo tuvo como objetivo desarrollar un nanosistema de liberación polímero-terapéutico (conjugado)/nanopartícula, utilizando Dextrano y Quitosano como polímeros transportadores biodegradables, hidrosolubles y compatibles a nivel ocular así como Hemisuccinato de Metilprednisolona como fármaco modelo. Primeramente, el fármaco fue capaz de unirse covalentemente a dos Dextranos de pesos moleculares 10 y 70 kDa. En función del contenido del componente activo y perfil de liberación, se seleccionó el Hemisuccinato de Metilprednisolona-Dextrano 10 kDa para elaborar las nanopartículas de Quitosano por el método de gelificación iónica empleando tripolifosfato sódico como agente entrecruzante. Por último, las nanopartículas fueron cubiertas con lactosa aplicando el secado por atomización. Se evaluó morfología, distribución de tamaño de las partículas, carga superficial, contenido y eficacia de captura del fármaco. Las partículas esféricas presentaron superficies lisas y uniformes. El pH tuvo influencia en el tamaño de las partículas observándose una distribución bimodal a pHs ≈ pKa del Quitosano y unimodal con un rango entre 130 - 170 nm a pHs < pKa. La variación de los potenciales Zeta entre los compuestos involucrados en la reacción, indicaron la posible ocurrencia de la misma. Al comparar la liberación del conjugado con las Nanopartículas a pH fisiológico, se observó que la encapsulación retrasó la liberación del fármaco alrededor de un 50%. Las nanopartículas recubiertas formaron micropartículas de 1.780 ± 0,5 nm, lo que favoreció su dispersibilidad en agua. Este nuevo nanosistema, evidenció su posible potencial en el desarrollo de formulaciones de liberación intravítrea, que reduzca la frecuencia de administración, ofreciendo una excelente alternativa que proporcione un mayor grado de satisfacción y mejore la calidad de vida del paciente.
Descritores: Doenças Retinianas/tratamento farmacológico
Nanotecnologia/organização & administração
Liberação Controlada de Fármacos/efeitos dos fármacos
-Polímeros/farmacologia
Qualidade de Vida
Doenças Retinianas/complicações
Metilprednisolona/uso terapêutico
Cromatografia Líquida/métodos
Dextranos/uso terapêutico
Membrana Epirretiniana/tratamento farmacológico
Preparações de Ação Retardada/farmacologia
Quitosana/uso terapêutico
Composição de Medicamentos/métodos
Material Particulado/uso terapêutico
Nanopartículas/administração & dosagem
Injeções Intravítreas/efeitos adversos
Limites: Humanos
Tipo de Publ: Estudo de Validação
Responsável: VE497.1 - Biblioteca Dr. Oswaldo Enríquez Isava
VE497.1; D-CF, An3


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Id: biblio-1039046
Autor: Riaz, Muhammad Ijaz; Sarwar, Hafiz Shoaib; Rehman, Mubashir; Gohar, Umar Farooq; Raza, Syed Atif; Siddique, Muhammad Irfan; Shahnaz, Gul; Sohail, Muhammad Farhan.
Título: Study of erythrocytes as a novel drug carrier for the delivery of artemether
Fonte: Braz. J. Pharm. Sci. (Online);55:e17680, 2019. graf.
Idioma: en.
Resumo: Resealed erythrocytes have been explored in various dimensions of drug delivery, owing to their high biocompatibility and inability to initiate immune response. The present research was designed to evaluate the drug delivery potential of erythrocytes by loading a hydrophobic anti-malarial drug, Artemether. Three different loading techniques were applied to achieve maximum optimized drug loading. A HPLC method was validated for drug quantification in erythrocytes. The relatively high loading was achieved using hypotonic treatment was 31.39% as compared to other two methods. These, drug loaded erythrocytes were characterized for membrane integrity via ESR showing higher ESR values for drug loaded cells as compared to normal cells. Moreover, microscopic evaluation was done to observe morphological changes in erythrocytes after successful loading which showed swollen cells with slight rough surface as compared to smooth surface of normal cells. Drug release was studied for 8 h which showed more than 80% release within 3-7 h from erythrocytes treated with different hypotonic methods. Overall, the study revealed a potential application of erythrocytes in delivery of hydrophobic drugs using hypotonic treatment as compared to other methods.
Descritores: Eritrócitos/classificação
Liberação Controlada de Fármacos
/administração & dosagem
FRUCTOKINASESABBREVIATIONS AS TOPIC/administração & dosagem
-Preparações Farmacêuticas/administração & dosagem
Cromatografia Líquida de Alta Pressão/métodos
Responsável: BR40.1 - DBD - Divisão de Biblioteca e Documentacão do Conjunto das Químicas


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Id: biblio-998224
Autor: Martín Casanova-Godoy, Luis Antonio; Castillo-Saavedra, Ericson Félix; Reynoso-Leyva, Elva Milagros; Ayala-Jara, Carmen Isolina.
Título: Estudio comparativo de perfiles de disolución de tabletas de prednisona 20 mg comercializados en Perú / Comparative study of dissolution profiles of prednisone 20 mg tablets marketed in Peru
Fonte: Mem. Inst. Invest. Cienc. Salud (Impr.);16(3):13-21, dic. 2018. tab, ilus.
Idioma: es.
Resumo: El estudio tuvo como finalidad comparar los perfiles de disolución de tabletas de prednisona 20 mg comercializados en Perú. Se realizó un estudio cuantitativo comparativo con diseño no experimental, que incluyó doce tabletas para cada formulación a evaluar (referente y multifuente), bajo condiciones similares de trabajo, en tres medios de disolución: buffer ácido clorhídrico pH 1,2; buffer acetato pH 4,5 y buffer fosfato pH 6,8. Los porcentajes temporales disueltos de prednisona fueron evaluados mediante el orden cinético cero, uno, Higuchi, raíz cúbica y Weibull para el modelo dependiente; mientras que el factor de similitud (f2), tiempo medio de disolución y eficiencia de disolución fueron utilizados para el modelo independiente. En el modelo dependiente, la liberación de prednisona; se ajustó a la cinética de función de Weibull; evaluada mediante el criterio de información de Akaike. En el modelo independiente, los valores de f2 en todos los medios de disolución cumplieron con el rango 50 - 100 establecida por la Food and Drug Adminstration, para indicar similitud in vitro entre los perfiles de disolución. Asimismo, se evidenció que no existe diferencia estadísticamente significativa entre las formulaciones, respecto al tiempo medio de disolución y la eficiencia de disolución. Las tabletas de prednisona 20 mg referente y multifuente comercializados en Perú son similares, con base en pruebas de perfiles de disolución in vitro(AU)

The purpose of the study was to compare the dissolution profiles of prednisone 20 mg tablets marketed in Peru. A comparative quantitative study with a non-experimental design was carried out, which included twelve tablets for each formulation to be evaluated (referent and multi-source), under similar work conditions in three dissolution media: hydrochloric acid buffer pH 1.2, acetate buffer pH 4.5 and phosphate buffer pH 6.8. The dissolved temporal percentages of prednisone were evaluated by zero kinetic order and first kinetic order, Higuchi, cubic root and Weibull models for the dependent model; while the similarity factor (f2), mean dissolution time and dissolution efficiency were used for the independent model. In the dependent model, the release of prednisone was adjusted to the Weibull function kinetics, evaluated using the Akaike information criterion. In the independent model, the values of f2 in all the dissolution media fulfilled the range 50 - 100 established by the Food and Drug Administration, to indicate in vitro similarity between the dissolution profiles. Likewise, it was evidenced that there is no statistically significant difference between the formulations with respect to the mean dissolution time and the dissolution efficiency. The reference and multi-source prednisone 20 mg tablets marketed in Peru are similar based on in vitro dissolution profiles tests(AU)
Descritores: Prednisona/farmacocinética
Liberação Controlada de Fármacos
Glucocorticoides/farmacocinética
-Peru
Comprimidos
Técnicas In Vitro
Dissolução
Tipo de Publ: Estudo Comparativo
Responsável: PY3.1 - Biblioteca


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Id: biblio-951934
Autor: Montaña, Jorge Andrés; Perez, León Darío; Baena, Yolima.
Título: A pH-responsive drug delivery matrix from an interpolyelectrolyte complex: preparation and pharmacotechnical properties
Fonte: Braz. J. Pharm. Sci. (Online);54(2):e17183, 2018. tab, graf, ilus.
Idioma: en.
Projeto: COLCIENCIAS.
Resumo: ABSTRACT Interpolyelectrolyte complexes, which constitute a type of polymeric material obtained through the self-assembly of oppositely charged polymers, exhibit interesting properties for use in the design of smart matrices for drug delivery. In the present study, a stoichiometric interpolyelectrolyte complex (SIPEC) composed of Eudragit E® and Eudragit® L100 was obtained at pH 6.0 and characterized and evaluated as a hydrophilic matrix for dexibuprofen. The formation of a SIPEC was monitored by ζ-potential measurements and characterized using infrared spectroscopy, thermal analysis, and scanning electron microscopy. The results indicated that a SIPEC obtained under these conditions can be used as a matrix for controlling the release of dexibuprofen and exhibit a pH-triggered release
Descritores: Liberação Controlada de Fármacos
Concentração de Íons de Hidrogênio
-Tecnologia Farmacêutica/instrumentação
Anti-Inflamatórios/análise
Responsável: BR1.1 - BIREME


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Id: biblio-1001579
Autor: Shaheen, Nabeela; Zaman, Shahiq uz.
Título: Development of fast dissolving tablets of flurbiprofen by sublimation method and its in vitro evaluation
Fonte: Braz. J. Pharm. Sci. (Online);54(4):e17061, 2018. tab, graf.
Idioma: en.
Resumo: Flurbiprofen belongs to Biopharmaceutical Classification System (BCS) class II drugs which are poorly soluble in water. The objective of present research work was to prepare fast dissolving tablets of Flurbiprofen using varying concentrations of three different sublimating agents to improve the dissolution rate. Seven formulations were prepared containing different concentrations of camphor, ammonium bicarbonate and thymol as sublimating agent along with primogel as a superdisintegrant. Tablets were manufactured by direct compression method. The prepared tablets were evaluated for pre-compression and post-compression parameters result, For all formulations result was within official limits. FTIR studies revealed that there were no interactions between the drug and the excipients used. From in vitro drug release studies it was concluded that the formulations F6 and F7 containing 10% and 15% of thymol showed fast drug release of 100.00% and 100.84% respectively in 30 minutes. Formulations containing camphor (F2 & F3) and ammonium bicarbonate (F4 & F5) as sublimating agents showed a drug release of less than 80%, while the control formulation F1 having no sublimating agent showed 49.14% of drug release in 30 minutes. Thus thymol can successfully be used to formulate fast dissolving tablets of flurbiprofen by sublimation method with much better dissolution profile
Descritores: Comprimidos/farmacologia
Técnicas In Vitro
Flurbiprofeno/análise
Dissolução/análise
-Liberação Controlada de Fármacos
Responsável: BR40.1 - DBD - Divisão de Biblioteca e Documentacão do Conjunto das Químicas


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Id: biblio-1001570
Autor: Shabbir, Maryam; Sajid, Ali; Hamid, Irfan; Sharif, Ali; Akhtar, Muhammad Furqan; Raza, Moosa; Ahmed, Shoaib; Peerzada, Sohaib; Amin, Muhammad Umair.
Título: Influence of different formulation variables on the performance of transdermal drug delivery system containing tizanidine hydrochloride: in vitro and ex vivo evaluations
Fonte: Braz. J. Pharm. Sci. (Online);54(4):e00130, 2018. tab, graf.
Idioma: en.
Resumo: The present study was aimed at preparation of transdermal patches of tizanidine HCl, evaluation of the effect of polymers on in vitro release pattern of the drug, and the effect of permeation enhancers on the penetration of the drug through the rabbit skin. Various proportions of hydrophilic (HPMC) and hydrophobic (Eudragit L-100) polymers were used with PEG 400 as film-forming agent, and Span 20 or DMSO as permeation enhancer. The formulations were assessed for physicochemical characteristics and in vitro drug release studies using USP paddle over disc method in phosphate buffered saline (pH 7.4) at 32.0±1°C. On the basis of in vitro studies and physicochemical evaluations, S03-A and S04-A were selected at Eudragit : HPMC ratios of 8 : 2 and 7 : 3, respectively, for further ex vivo analysis. The effects of different concentrations of Span 20 and DMSO were evaluated on excised rabbit skin using Franz diffusion cell. Cumulative drug permeation, flux, permeability coefficient, target flux, and enhancement ratio were calculated and compared with the control formulations. Kinetic models and Tukey's multiple comparison test were applied to evaluate the drug release patterns. Formulation SB03-PE containing Eudragit L-100:HPMC (7:3) with Span 20 (15% w/w) produced the highest enhancement in drug permeation, and followed zero order kinetic model with super case-II drug release mechanism.
Descritores: Adesivo Transdérmico/classificação
Adesivo Transdérmico/provisão & distribuição
-Técnicas In Vitro
Preparações Farmacêuticas/análise
Interações Hidrofóbicas e Hidrofílicas
Liberação Controlada de Fármacos/efeitos dos fármacos
Limites: Animais
Coelhos
Responsável: BR40.1 - DBD - Divisão de Biblioteca e Documentacão do Conjunto das Químicas



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