No description available.

No description available.

No / A sensitive and rapid oil-in-water (O/W) microemulsion high performance liquid chromatography (MELC) method has been developed. The water-in-oil (w/o) microemulsion was used as a mobile phase in the determination of salbutamol in aqueous solutions. In addition, the influence of operating parameters on the separation performance was examined. The samples were injected into C18, (250mmx4.6mm) analytical columns maintained at 25(o)C with a flow rate 1 ml/min. The mobile phase was 95.5% v/v aqueous orthophosphate buffer 20 mM (adjusted to pH 3 with orthophosphoric acid), 0.5% ethyl acetate, 1.5% Brij35, and 2.5% 1-butanol, all w/w. The salbutamol and internal standard peaks were detected by fluorescence detection at the excitation and emission wavelengths of 267 and 313 nm respectively. The method had an accuracy of > 97.78% and the calibration curve was linear (r2 = 0.99) over salbutamol concentrations ranging from 25 to 500 ng/mL. The intra-day and inter-day precisions (CV %) were <1.6 and <1.8, respectively. The limit of detection (LOD) and limit of quantitation (LOQ) were 9.61ng/ml and 29.13ng/ml, respectively. The method reported is simple, precise and accurate, and has the capacity to be used for determination of salbutamol in the pharmaceutical preparation.

Background: The effectiveness of inhaled salbutamol in routine care depends particularly on prescribed dosage and applied inhalation technique. To achieve maximum effectiveness and to prevent drug-related problems, prescription and administration need to work in concert. Methods: We performed a controlled intervention pilot study with 4 consecutive groups in a general paediatric unit and assessed problems in salbutamol prescribing and administration. Control group [i]: Routine care without additional support. First intervention group [ii]: We carried out a teaching session for nurses aimed at preventing problems in inhalation technique. Independently from this, a pharmacist counselled physicians on problems in salbutamol prescribing. Second intervention group [iii]: Additionally to the first intervention, physicians received standardised feedback on the inhalation technique. Follow-up group [iv]: Subsequently, without any delay after the second intervention group had been completed, sustainability of the measures was assessed. We performed the chi-square test to calculate the level of significance with p ≤ 0.05 to indicate a statistically significant difference for the primary outcome. As we performed multiple testing, an adjusted p ≤ 0.01 according to Bonferroni correction was considered as significant. Results: We included a total of 225 patients. By counselling the physicians, we reduced the number of patients with problems from 55% to 43% (control [i] vs. first intervention [ii], n.s.). With additional feedback to physicians, this number was further reduced to 25% ([i] vs. [iii], p < 0.001). In the follow-up [iv], the number rose again to 48% (p < 0.01 compared to feedback group). Conclusions: Teaching nurses, counselling physicians, and providing feedback on the quality of inhalation technique effectively reduced problems in salbutamol treatment. However, for success to be sustained, continuous support needs to be provided. Trial registration: German Clinical Trials register: DRKS00006792.

Made available in DSpace on 2016-01-26T18:55:29Z (GMT). No. of bitstreams: 1 Dissertacao.pdf: 262952 bytes, checksum: fed2a60f7a0605b64f30fb2d2656c986 (MD5) Previous issue date: 2009-06-26 / Salbutamol and fenoterol are agonists &#946;2 adrenergic of short duration, with important paper in the treatment of the breathing diseases due to excellent effect bronchodilator. The study had as objective evaluates through physical exam, laboratorial and electrocardiography the effects of the fenoterol and salbutamol for road inalatory in dogs. Twelve dogs were distributed in 2 groups being: group FE (fenoterol) it received fenoterol through inalatory, in the dose of 2droups/5Kg of alive weight diluted in solution of chloride of sodium 0,9% and administered by road inalatory through the inhalation apparel; group SA (salbutamol) treaty with salbutamol, through aerosol dosador, in the dose of 100 micrograms. They were appraised four different moments, being considered MC (moment controls) before the administration of the drug, M30, M2 and M6, where the evaluations were accomplished respectively with 30 minutes, 2 hours and 6 hours after administration of the drugs. They were checked temperature (T), heart frequency (FC), breathing frequency (f), systolic blood pressure (PAS), appraised the gasometry and electrocardiogram. The fenoterol and salbutamol caused discreet heart stimulation, being significant for the animals of the group SA two hours after the administration of the drug compared a moment controls. Tremors were observed with larger predominance in the animals of the group SA. Decrease of the systolic blood pressure and increase of the breathing frequency were observed in the two groups, and there were not significant alteration of the temperature, gasometry and electrocardiogram for both groups. Was ended that the fenoterol provokes smaller side effects of heart stimulation and tremors compared to the salbutamol being this way a safer drug. / Salbutamol e fenoterol são agonistas &#946;2 adrenérgicos de curta duração, com papel importante no tratamento das doenças respiratórias devido ao seu excelente efeito broncodilatador. O presente estudo teve como objetivo avaliar por meio de exame físico, laboratorial e eletrocardiográfico os efeitos destes fármacos administrados por via inalatória em cães. Doze cães foram distribuídos em dois grupos com seis em cada sendo: grupo FE (fenoterol) recebeu fenoterol via inalatória, na dose de 2 gotas/5Kg de peso vivo, diluídas em solução de cloreto de sódio 0,9% e administrados por meio do aparelho de inalação; grupo SA (salbutamol) tratado com salbutamol, por meio de dosador de aerossol, na dose de 100mg. Foram avaliados quatro diferentes momentos, sendo considerado MC (momento controle) antes da administração dos fármacos, M30, M2 e M6, onde as avaliações foram realizadas com 30 minutos, 2 horas e 6 horas após administração dos fármacos respectivamente. Foram aferidas temperatura retal(TR), freqüência cardíaca (FC), freqüência respiratória (FR), pressão arterial sistólica (PAS), avaliados a hemogasometria e eletrocardiograma. O fenoterol e salbutamol causaram discreta estimulação cardíaca, sendo estatisticamente significativo para os animais do grupo SA 2 horas após a sua administração comparado ao momento controle. Tremores foram observados com maior predominância nos animais do grupo SA. Diminuição da pressão arterial sistólica e aumento da freqüência respiratória foram observados nos dois grupos, e não houve alteração significativa da temperatura retal, dos valores da hemogasometria e eletrocardiograma em ambos os grupos. Conclui-se que o fenoterol provoca menor efeitos colaterais de estimulação cardíaca e tremores comparados ao salbutamol sendo desta forma um fármaco mais seguro.

Made available in DSpace on 2016-07-18T17:53:06Z (GMT). No. of bitstreams: 1 Dissertacao.pdf: 262952 bytes, checksum: fed2a60f7a0605b64f30fb2d2656c986 (MD5) Previous issue date: 2009-06-26 / Salbutamol and fenoterol are agonists &#946;2 adrenergic of short duration, with important paper in the treatment of the breathing diseases due to excellent effect bronchodilator. The study had as objective evaluates through physical exam, laboratorial and electrocardiography the effects of the fenoterol and salbutamol for road inalatory in dogs. Twelve dogs were distributed in 2 groups being: group FE (fenoterol) it received fenoterol through inalatory, in the dose of 2droups/5Kg of alive weight diluted in solution of chloride of sodium 0,9% and administered by road inalatory through the inhalation apparel; group SA (salbutamol) treaty with salbutamol, through aerosol dosador, in the dose of 100 micrograms. They were appraised four different moments, being considered MC (moment controls) before the administration of the drug, M30, M2 and M6, where the evaluations were accomplished respectively with 30 minutes, 2 hours and 6 hours after administration of the drugs. They were checked temperature (T), heart frequency (FC), breathing frequency (f), systolic blood pressure (PAS), appraised the gasometry and electrocardiogram. The fenoterol and salbutamol caused discreet heart stimulation, being significant for the animals of the group SA two hours after the administration of the drug compared a moment controls. Tremors were observed with larger predominance in the animals of the group SA. Decrease of the systolic blood pressure and increase of the breathing frequency were observed in the two groups, and there were not significant alteration of the temperature, gasometry and electrocardiogram for both groups. Was ended that the fenoterol provokes smaller side effects of heart stimulation and tremors compared to the salbutamol being this way a safer drug. / Salbutamol e fenoterol são agonistas &#946;2 adrenérgicos de curta duração, com papel importante no tratamento das doenças respiratórias devido ao seu excelente efeito broncodilatador. O presente estudo teve como objetivo avaliar por meio de exame físico, laboratorial e eletrocardiográfico os efeitos destes fármacos administrados por via inalatória em cães. Doze cães foram distribuídos em dois grupos com seis em cada sendo: grupo FE (fenoterol) recebeu fenoterol via inalatória, na dose de 2 gotas/5Kg de peso vivo, diluídas em solução de cloreto de sódio 0,9% e administrados por meio do aparelho de inalação; grupo SA (salbutamol) tratado com salbutamol, por meio de dosador de aerossol, na dose de 100mg. Foram avaliados quatro diferentes momentos, sendo considerado MC (momento controle) antes da administração dos fármacos, M30, M2 e M6, onde as avaliações foram realizadas com 30 minutos, 2 horas e 6 horas após administração dos fármacos respectivamente. Foram aferidas temperatura retal(TR), freqüência cardíaca (FC), freqüência respiratória (FR), pressão arterial sistólica (PAS), avaliados a hemogasometria e eletrocardiograma. O fenoterol e salbutamol causaram discreta estimulação cardíaca, sendo estatisticamente significativo para os animais do grupo SA 2 horas após a sua administração comparado ao momento controle. Tremores foram observados com maior predominância nos animais do grupo SA. Diminuição da pressão arterial sistólica e aumento da freqüência respiratória foram observados nos dois grupos, e não houve alteração significativa da temperatura retal, dos valores da hemogasometria e eletrocardiograma em ambos os grupos. Conclui-se que o fenoterol provoca menor efeitos colaterais de estimulação cardíaca e tremores comparados ao salbutamol sendo desta forma um fármaco mais seguro.

Zugl.: Giessen, Univ., Diss., 2009

Le traitement de l’asthme concerne une large population et fait appel très majoritairement à une administration par voie pulmonaire. Cette voie présente certains inconvénients qui pourraient être palliés par le recours à la voie buccale comme envisagé dans cette étude, avec une amélioration attendue de la compliance et de la biodisponibilité. Aussi ce travail a eu pour objectif de développer et caractériser une formulation mucoadhésive thermogélifiante à base de salbutamol. Au regard des contraintes liées à la voie buccale et à la prise en charge du traitement de l’asthme aigu, les principales propriétés pharmacotechniques attendues pour optimiser la biodisponibilité de cette formulation ont été : (i) une gélification optimale autour de 30°C après pulvérisation pour faciliter notamment l’administration ; (ii) des propriétés mécaniques et mucoadhésives importantes pour assurer un maintien de la forme au site d’absorption ; (iii) une cinétique de libération compatible avec le traitement de la phase aigüe de la pathologie. Le choix des excipients a été défini afin d’avoir la plus grande innocuité de la formulation finale. Les travaux expérimentaux ont mis en évidence l’intérêt de certaines techniques innovantes pour la caractérisation de ce type de formulation comme notamment l’étude de libération à l’aide de l’appareil de dissolution à flux continu, la détermination de la cytotoxicité par microscopie holographique digitale et l’évaluation de la mucoadhésion in vitro et in vivo par imagerie. Les résultats ont aussi permis de proposer des modèles mathématiques pour l’interprétation des mécanismes de libération du salbutamol et quantifier l’importance des phénomènes de diffusion et d’érosion. Les conclusions de cette étude sont favorables à la poursuite du développement en vue d’une commercialisation. / The treatment of asthma concerns a large population and generally necessitates an administration by the pulmonary route. This route has some drawbacks which could be overcome by the buccal route, like considered in this study expecting an improvement of the compliance and the bioavailability. The aim of this work was to develop and characterize a thermogelling mucoadhesive formulation containing salbutamol sulfate. The main properties of the formulation were: (i) thermogelation around 30°C to facilitate the administration by spray; (ii) strong mechanical properties and high mucoadhesive strength to maintain the formulation in situ; (iii) drug release kinetics adapted to the treatment. The excipients were selected with regard to the final formulation safety. The experimental work emphasized the great interest of certain techniques in the characterization of this kind of formulation, for example the drug release study using flow through apparatus, the cytotoxicity study using digital holographic microscopy and also the mucoadhesion study by in vivo imaging. The use of mathematical models provided a relevant understanding of drug release mechanisms. The conclusion of this study is favorable to a further development of the project for a future marketing.

Procedimentos analíticos baseados em medidas de quimiluminescência caracterizam-se por apresentar alta sensibilidade, baixos limites de detecção, ampla faixa de resposta linear e instrumentação simples. Uma das principais dificuldades relacionadas a este tipo de medida é maximizar a quantidade de radiação detectada, já que a emissão ocorre em todas as direções, o que dificulta o posicionamento adequado da cela de medida em relação ao sistema de detecção. Uma alternativa consiste na utilização de guias de ondas, que são dispositivos que conduzem a radiação emitida, minimizando perdas durante o transporte, tal como ocorre nos cabos de fibras ópticas. O acoplamento de sistemas de análises em fluxo com detecção por quimiluminescência é bastante conveniente, já que a mistura entre amostras a reagentes precisa ser rápida e altamente reprodutível, além de ser realizada a uma distância muito pequena do sistema de detecção, devido ao curto tempo de vida dos intermediários no estado excitado. Neste trabalho, é apresentada a avaliação de uma cela constituída por um guia de ondas para medidas de quimiluminescência. Estas ferramentas foram aplicadas à determinação de hipoclorito em amostras de líquido de Dakin por quimiluminescência empregando a reação de oxidação do luminol por hipoclorito. Também foi desenvolvido um procedimento analítico para a determinação de salbutamol, explorando a inibição da quimiluminescência da reação de oxidação de luminol por hipoclorito, caracterizando-se como uma alternativa promissora para a quantificação do fármaco. Em ambas as aplicações, os resultados foram concordantes com os obtidos por procedimentos de referência a nível de confiança de 95% / Analytical procedures based on chemiluminescence are characterized by high sensitivity, low detection limits, wide linear response ranges and simple instrumentation. One of the main troubles is to increase the amount of detected radiation, because emission occurs in all directions, making difficulty the positioning of the measurement cell in relation to the detection system. An alternative consists in the use of liquid-core waveguides, devices that constrain the emitted radiation, minimizing losses during the transport, in a similar way to optical fibers. Coupling flow analysis to chemiluminescence is attractive, because sample and reagents mixing needs to be fast, highly reproducible and accomplished close to the detector, in view of the short lifetime of the intermediates in the excited state. In this work, a cell constituted by a liquid-core waveguide was evaluated for chemiluminescence measurements. These tools were applied to the determination of hypochlorite in Dakin solution samples by chemiluminescence exploiting the oxidation of luminol by hypochlorite. An analytical procedure for salbutamol determination, exploiting the inhibition of chemiluminescence of luminol oxidation by hypochlorite, was developed, characterizing as a promising alternative for the quantification of this pharmaceutical substance. In both applications, results were in agreement to those obtained by reference procedures at the 95% confidence level

Le traitement de l’asthme concerne une large population et fait appel très majoritairement à une administration par voie pulmonaire. Cette voie présente certains inconvénients qui pourraient être palliés par le recours à la voie buccale comme envisagé dans cette étude, avec une amélioration attendue de la compliance et de la biodisponibilité. Aussi ce travail a eu pour objectif de développer et caractériser une formulation mucoadhésive thermogélifiante à base de salbutamol. Au regard des contraintes liées à la voie buccale et à la prise en charge du traitement de l’asthme aigu, les principales propriétés pharmacotechniques attendues pour optimiser la biodisponibilité de cette formulation ont été : (i) une gélification optimale autour de 30°C après pulvérisation pour faciliter notamment l’administration ; (ii) des propriétés mécaniques et mucoadhésives importantes pour assurer un maintien de la forme au site d’absorption ; (iii) une cinétique de libération compatible avec le traitement de la phase aigüe de la pathologie. Le choix des excipients a été défini afin d’avoir la plus grande innocuité de la formulation finale. Les travaux expérimentaux ont mis en évidence l’intérêt de certaines techniques innovantes pour la caractérisation de ce type de formulation comme notamment l’étude de libération à l’aide de l’appareil de dissolution à flux continu, la détermination de la cytotoxicité par microscopie holographique digitale et l’évaluation de la mucoadhésion in vitro et in vivo par imagerie. Les résultats ont aussi permis de proposer des modèles mathématiques pour l’interprétation des mécanismes de libération du salbutamol et quantifier l’importance des phénomènes de diffusion et d’érosion. Les conclusions de cette étude sont favorables à la poursuite du développement en vue d’une commercialisation. / The treatment of asthma concerns a large population and generally necessitates an administration by the pulmonary route. This route has some drawbacks which could be overcome by the buccal route, like considered in this study expecting an improvement of the compliance and the bioavailability. The aim of this work was to develop and characterize a thermogelling mucoadhesive formulation containing salbutamol sulfate. The main properties of the formulation were: (i) thermogelation around 30°C to facilitate the administration by spray; (ii) strong mechanical properties and high mucoadhesive strength to maintain the formulation in situ; (iii) drug release kinetics adapted to the treatment. The excipients were selected with regard to the final formulation safety. The experimental work emphasized the great interest of certain techniques in the characterization of this kind of formulation, for example the drug release study using flow through apparatus, the cytotoxicity study using digital holographic microscopy and also the mucoadhesion study by in vivo imaging. The use of mathematical models provided a relevant understanding of drug release mechanisms. The conclusion of this study is favorable to a further development of the project for a future marketing.