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1.
Braz. J. Pharm. Sci. (Online) ; 58: e20079, 2022. tab, graf
Article in English | LILACS | ID: biblio-1403747

ABSTRACT

Abstract Sustained release matrix tablets of 100 mg losartan potassium HCl were fabricated with two release retarding polymers namely HPMC K100 M and affinisol by direct compression method. Nine trial formulations were prepared by varying content of these polymers, each from 50 mg to 100 mg; keeping the total weight of the tablet 310 mg. The best formulation was selected based on in vitro drug release profile for 12 hours conducted in Type II dissolution apparatus at 50 rpm and water as dissolution medium. Pre-compression parameters such as bulk density, tap density, Carr's index and Hausner ratio were evaluated for the selected tablet. The tablets were subjected to thickness, weight variation test, drug content, hardness and friability. Drug release kinetics, surface morphology and accelerated stability study were investigated for that selected formulation. Formulation F4 with the composition of 75 mg HPMC K100M and 100 mg affinisol was selected as the best formulation that extended the drug release up to 12 hours. Pre-compression parameters and other tableting properties were within the Pharmacopoeia limit. Release kinetics analysis proved non-fickian zero-order drug release and that was further confirmed by surface morphology of the tablets before and after dissolution study visualized by SEM. The developed formulation was found to be stable for one month stored at 60 ○C.


Subject(s)
Tablets/analysis , In Vitro Techniques/methods , Pharmaceutical Preparations/analysis , Losartan/agonists , Drug Compounding/methods , Dissolution , Drug Liberation/drug effects , Methods
2.
China Journal of Chinese Materia Medica ; (24): 103-110, 2022.
Article in Chinese | WPRIM | ID: wpr-927916

ABSTRACT

The present study explored the effect of co-amorphous technology in improving the dissolution rate and stability of silybin based on the puerarin-silybin co-amorphous system prepared by the spray-drying method. Solid-state characterization was carried out by powder X-ray diffraction(PXRD), polarizing microscopy(PLM), Fourier transform infrared spectroscopy(FT-IR), differential scanning calorimetry(DSC), etc. Saturated powder dissolution, intrinsic dissolution rate, moisture absorption, and stability were further investigated. The results showed that puerarin and silybin formed a co-amorphous system at a single glass transition temperature which was higher than that of any crude drug. The intrinsic dissolution rate and supersaturated powder dissolution of silybin in the co-amorphous system were higher than those of the crude drug and amorphous system. The co-amorphous system kept stable for as long as three months under the condition of 40 ℃, 75% relative humidity, which was longer than that of the single amorphous silybin. Therefore, the co-amorphous technology could significantly improve the dissolution and stability of silybin.


Subject(s)
Calorimetry, Differential Scanning , Desiccation , Drug Compounding/methods , Drug Stability , Silymarin , Solubility , Spectroscopy, Fourier Transform Infrared , Technology , X-Ray Diffraction
3.
Rev. fac. cienc. méd. (Impr.) ; 17(2): 25-30, jul.-dic. 2020.
Article in Spanish | LILACS, BIMENA | ID: biblio-1292409

ABSTRACT

La preparación y administración de medicamentos, es parte importante en el proceso de recuperación de la salud, se destaca entre las funciones relevantes de los profesionales y auxiliares de enfermería, incluye etapas críticas que deben garantizar la correcta y segura administración de los mismos. Existe carencia de revisiones bibliográficas que aborden la problemática de los errores de enfermería, aunque, investigadores en todo el mundo, han estudiado el impacto que genera el error en la preparación de medicamentos, siendo este uno de los principales problemas en el campo de la enfermería. Objetivo: conocer la relación entre la calidad técnica en la preparación de medicamentos, identificando características y tipos, con la frecuencia en los errores de enfermería. Material y Métodos: se realizó revisión bibliográfica, identificando once artículos científicos en las bases de datos PubMed, Scopus y SciELO. Se incluyeron estudios originales y observacionales, excluyendo revisiones sistemáticas, estudios duplicados y sin acceso libre a la información. Conclusión: los factores predominantes en los errores de enfermería, se deben a la confusión al momento de elegir el fármaco, error en el cálculo de dosis, sobrecarga de trabajo y déficit de conocimiento...(AU)


Subject(s)
Humans , Preparation Scales , Nursing Assistants , Drug Compounding/methods , Inappropriate Prescribing
4.
Gac. méd. Méx ; 155(2): 191-195, mar.-abr. 2019. tab, graf
Article in Spanish | LILACS | ID: biblio-1286482

ABSTRACT

Resumen La enfermedad de Menkes es una patología neurodegenerativa y letal debida a mutaciones génicas de la enzima ATP-7A trasportadora de cobre; se manifiesta por síntomas neurológicos y alteraciones del tejido conectivo de severidad variable. El uso subcutáneo oportuno de histidinato de cobre (Cu-His) es determinante en la calidad de vida. Se reportan las primeras experiencias en México en la síntesis y uso seguro de Cu-His en tres casos en los que corroboramos hipocupremia e hipoceruloplasminemia. Bajo asesoramiento del Hospital for Sick Children, Toronto, Canadá, elaboramos una solución de 500 µg/mL. En los tres casos aplicamos 250 µg de Cu-His, sin efectos indeseables relevantes durante 30 días y observamos las siguientes determinaciones séricas de cobre (Cu en µg/L) y ceruloplasmina (Cp en mg/dL): caso 1, Cu días 0 y 30, 8 y 504 µg/L; Cp días 0 y 30, 4 y 10.75 mg/dL; caso 2, Cu días 0 y 30, < 50 y 502, µg/L; Cp días 0 y 30, 2 y 15 mg/dL; caso 3, Cu días 0 y 30, 3 y 84.2 µg/L; Cp días 0 y 30, 4 y 10.7 mg/dL. En México es posible la síntesis segura de Cu-His y tratar la enfermedad de Menkes, la cual debe ser intencionalmente buscada.


Abstract Menkes disease is a neurodegenerative and lethal pathology caused by gene mutations of the copper-transporting ATP-7A enzyme; it manifests itself by neurological symptoms and connective tissue changes of varying severity. Timely subcutaneous use of copper histidinate (Cu-His) is determinant for quality of life. We report the first experiences in Mexico on Cu-His synthesis and its safe use in 3 cases where hypocupremia and hypoceruloplasminemia were corroborated. With advice of the Hospital for Sick Children of Toronto Canada, we prepared a 500 µg/mL solution. In all three cases were 250 µg of Cu-His applied without relevant undesirable effects for 30 days. Serum copper (Cu, expressed in µg/L) and ceruloplasmin (Cp, in mg/dL) were determined: case 1, Cu days 0 and 30, 8 and 504 µg/L; Cp days 0 and 30, 4 and 10.75 mg/dL; case 2, Cu days 0 and 30, <50 and 502 µg/L; Cp days 0 and 30, 2 and 15 mg/dL; case 3, Cu days 0 and 30, 3 and 84.2 µg/L; Cp days 0 and 30, 4 and 10.7 mg/dL. In Mexico, it is possible to safely synthesize Cu-His and treat MD, which must be intentionally sought.


Subject(s)
Humans , Infant , Child, Preschool , Organometallic Compounds/administration & dosage , Quality of Life , Drug Compounding/methods , Histidine/analogs & derivatives , Menkes Kinky Hair Syndrome/drug therapy , Organometallic Compounds/adverse effects , Copper/blood , Pharmaceutical Solutions , Histidine/administration & dosage , Histidine/adverse effects , Mexico
5.
Journal of Zhejiang University. Science. B ; (12): 901-909, 2019.
Article in English | WPRIM | ID: wpr-1010497

ABSTRACT

β-Carotene is one of the most abundant natural pigments in foods; however, usage of β-carotene is limited because of its instability. Microencapsulation techniques are usually applied to protect microencapsulated β-carotene from oxidization. In this study, β-carotene was microencapsulated using different drying processes: spray-drying, spray freeze-drying, coating, and spray granulation. The properties of morphology, particle size, water content, thermal characteristic, and chemical stability have been explored and compared. Scanning electron microscopy measurements showed that the coated powder had a dense surface surrounded by starch and suggested that the coating process gave a microencapsulated powder with the smallest bulk density and the best compressibility among the prepared powders. The chemical stabilities of microcapsules were evaluated during six months of storage at different temperatures. The coated powder had the highest mass fraction of β-carotene, which indicated that the coating process was superior to the three other drying processes.


Subject(s)
Drug Compounding/methods , Drug Stability , Freeze Drying , Microscopy, Electron, Scanning , Technology, Pharmaceutical , beta Carotene/chemistry
6.
Acta cir. bras ; 33(12): 1052-1060, Dec. 2018. graf
Article in English | LILACS | ID: biblio-973489

ABSTRACT

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.


Subject(s)
Animals , Male , Apoptosis/drug effects , Zoledronic Acid/pharmacology , Kupffer Cells/drug effects , Liver/cytology , Immunohistochemistry , Random Allocation , Cell Count , Reproducibility of Results , Treatment Outcome , Rats, Sprague-Dawley , Drug Compounding/methods , Flow Cytometry , Zoledronic Acid/administration & dosage , Zoledronic Acid/chemical synthesis , Liposomes/chemical synthesis
7.
Online braz. j. nurs. (Online) ; 17(2)jun. 2018. ilus
Article in English, Spanish, Portuguese | BDENF, LILACS | ID: biblio-1117868

ABSTRACT

O time de medicação constitui-se como um grupo de trabalho formado por enfermeiros que se dedicam às etapas do sistema de medicação, com uma certa uniformidade na realização das atividades, entretanto, não foi construída qualquer padronização do seu processo de trabalho. OBJETIVO: descrever o preparo de medicamentos enterais e soluções parenterais pelo time de medicação na unidade neonatal. MÉTODO: estudo qualitativo, descritivo, com o método pesquisa-ação. Os sujeitos foram os enfermeiros do time de medicação da unidade neonatal. A coleta de dados foi constituída por: pesquisa de documentos; observação do preparo da medicação; coleta de problemas na reunião do time de medicação. RESULTADOS: atualização do tema e das atribuições da equipe de enfermagem da unidade neonatal; construção de fluxogramas relacionados ao preparo de medicamentos. CONCLUSÃO: o estudo possibilitou implementar intervenções no preparo de medicamentos realizadas pelos sujeitos do estudo, padronizando as etapas e definindo as relações de trabalho da equipe de enfermagem


The medication team is a work group formed by nurses who dedicate themselves to the stages of the medication system, with certain uniformity in the accomplishment of the activities; however, no standardization of their work process was developed. AIM: describe the preparation of enteral medications and parenteral solutions by the medication team in the neonatal unit. METHOD: this is a qualitative, descriptive study that uses the action research method. The subjects were the nurses of the medication team of the neonatal unit. Data collection consisted of: document search; observation of medication preparation; and collection of problems at the medication team meeting. RESULTS: updating of the theme and attributions of the nursing team of the neonatal unit; construction of flowcharts related to the preparation of medicines. CONCLUSION: the study allowed implementing interventions in the preparation of medicines carried out by the study subjects, standardizing the steps and defining the work relationships of the nursing team


El equipo de medicación es un grupo de trabajo formado por enfermeros que se dedican a las etapas del sistema de medicación, realizándolas con una cierta uniformidad, pero sin haber sido construida cualquier estandarización de su proceso de trabajo. OBJETIVO: describir la preparación de medicamentos enterales y soluciones parenterales por el equipo de medicación en la unidad neonatal. MÉTODO: estudio cualitativo, descriptivo, con el método investigación-acción. Los sujetos fueron los enfermeros del equipo de medicación de la unidad neonatal. La recolección de los datos fue constituida por: investigación de documentos; observación de la preparación de la medicación; recopilación de problemas en la reunión del equipo de medicación. RESULTADOS: actualización del tema y de las atribuciones del equipo de enfermería de la unidad neonatal; construcción de organigramas relacionados a la preparación de medicamentos. CONCLUSIÓN: el estudio posibilitó implementar intervenciones en la preparación de medicamentos realizadas por los sujetos del estudio, estandarización de las etapas para definir las relaciones de trabajo del equipo de enfermería.


Subject(s)
Humans , Intensive Care Units, Neonatal , Drug Compounding/methods , Parenteral Nutrition Solutions , Medication Systems , Nursing, Team , Pharmaceutical Preparations , Patient Safety
8.
Braz. j. biol ; 78(2): 311-317, May-Aug. 2018. tab, graf
Article in English | LILACS | ID: biblio-888857

ABSTRACT

Abstract The aims of this research were first, to evaluate the antibacterial potential of commercial thyme essential oil against V. alginolyticus and V. parahaemolyticys and second, using the spray drying technique to produce microcapsules. chemical compounds of thyme oil and microcapsules were identified and quantified being thymol the chemical component present at the highest concentration. Oil-in-water (O/W) emulsions were prepared and the microcapsules were obtained with a spray dryer using maltodextrin as wall material (ratio 1:4). Thyme oil and the microcapsules exhibited antimicrobial activity against V. parahaemolyticus and V. alginolyticus. The spray drying process did not affect the antimicrobial activity of thyme essentialoil.


Resumo Os objetivos desta pesquisa foram avaliar o potencial antibacteriano do óleoessencial de tomilho sobre V. alginolyticus e V. parahaemolyticys e produzir microcápsulas através do processo de secagem por aspersão (spray dryer). Os compostos químicos do óleo essencial de tomilho e das microcápsulas foram identificados e quantificadaos. Foi preparada uma emulsão de óleo em água (O/A) e em seguida foram produzidas microcápsulas em um spray dryer utilizando-se óleo essencial de tomilho e maltodextrina como material de parede na proporção de 1:4 respectivamente. Entre os vários compostos identificados, o timol apresentou maior concentração. O óleo essencial de tomilho e as microcápsulas exibiram atividade antibacteriana sobre V. parahaemolyticus e V. alginolyticus. O processo de secagem por aspersão não afetou a atividade antibacteriana do óleo essencial de tomilho.


Subject(s)
Vibrio alginolyticus/drug effects , Thymus Plant/chemistry , Drug Compounding/methods , Anti-Bacterial Agents/isolation & purification , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry
9.
Braz. J. Pharm. Sci. (Online) ; 54(2): e17499, 2018. graf
Article in English | LILACS | ID: biblio-1039034

ABSTRACT

ABSTRACT For the release of pharmaceutical products into the drug market; most of the pharmaceutical companies depend on acceptance criteria - that are set internally, regulatory and/or pharmacopeially. However, statistical process control monitoring is underestimated in most quality control in cases; although it is important not only for process stability and efficiency assessment but also for compliance with all appropriate pharmaceutical practices such as good manufacturing practice and good laboratory practice, known collectively as GXP. The current work aims to investigate two tablet inspection characteristics monitored during in-process control viz. tablet average weight and hardness. Both properties were assessed during the compression phase of the tablet and before the coating stage. Data gathering was performed by the Quality Assurance Team and processed by Commercial Statistical Software packages. Screening of collected results of 31 batches of an antibacterial tablet - based on Fluoroquinolone -showed that all the tested lots met the release specifications, although the process mean has been unstable which could be strongly evident in the variable control chart. Accordingly, the two inspected processes were not in the state of control and require strong actions to correct for the non-compliance to GXP. What is not controlled cannot be predicted in the future and thus the capability analysis would be of no value except to show the process capability retrospectively only. Setting the rules for the application of Statistical Process Control (SPC) should be mandated by Regulatory Agencies.


Subject(s)
Tablets, Enteric-Coated/analysis , Tablets, Enteric-Coated/standards , Pharmaceutical Preparations/standards , Data Interpretation, Statistical , Fluoroquinolones/standards , Drug Compounding/methods , Drug Industry/classification
10.
Rev. bras. enferm ; 71(supl.3): 1388-1394, 2018. tab
Article in English | LILACS, BDENF | ID: biblio-958729

ABSTRACT

ABSTRACT Objective: to evaluate the preparation and administration of oral medications to institutionalized children by nursing professionals. Method: quantitative study, developed from August to September 2016, in a shelter in Fortaleza, Ceará. 323 observations of preparation and administration of oral drugs were carried out. Interview and non-participant direct observation of the process of drug administration were performed, whose data were analyzed through descriptive statistics. Results: Of the 29 actions of preparation and administration of the drugs, ten were considered satisfactory. Sanitizing of hands before touching the pills occurred in only 5.2% of the observations and cleansing of the bottle for liquid drugs was performed in 23.8%. The actions "check the right child"; "checking medication with the prescription", and "check the right dose" obtained percentages below 15%. Conclusion: measures recommended by the literature for the administration of medication were not, in their clear majority, followed, making specific training and protocols necessary.


RESUMEN Objetivo: evaluar el preparo y la administración de medicinas orales por profesionales de enfermería a niños institucionalizados. Método: estudio cuantitativo desarrollado en agosto y septiembre de 2016, en un refugio de niños de Fortaleza, Ceará. Fueron realizadas 323 observaciones del preparo y de la administración de medicinas. Se realizaron encuesta y observación directa en el participante del proceso de administración de las medicinas, cuyos datos fueron evaluados por la estadística descriptiva. Resultados: de entre las 29 acciones del preparo y de la administración de las medicinas, diez fueron consideradas satisfactorias. La higienización de las manos antes de manosear las pastillas ocurrió en el 5,2% de las observaciones y la limpieza de los frascos de medicinas se dio en el 23,8%. Las acciones "verificar el niño bien"; "verificar la medicina con la prescripción" y "certificar la dosis correcta" obtuvieron porcentuales inferiores al 15%. Conclusión: medidas recomendadas por la literatura para administración de medicinas no fueron, en su gran parte, adoptadas, convirtiéndose necesarias las capacitaciones y los protocolos específicos.


RESUMO Objetivo: avaliar o preparo e a administração de medicamentos orais por profissionais de enfermagem a crianças institucionalizadas. Método: estudo quantitativo desenvolvido em agosto e setembro de 2016, em um abrigo de Fortaleza, Ceará. Foram realizadas 323 observações do preparo e da administração de medicamentos. Realizaram-se entrevista e observação direta não participante do processo de administração dos medicamentos, cujos dados foram avaliados pela estatística descritiva. Resultados: dentre as 29 ações do preparo e da administração dos medicamentos, dez foram consideradas satisfatórias. A higienização das mãos antes de tocar em comprimidos ocorreu em 5,2% das observações e a limpeza dos frascos de medicamentos deu-se em 23,8%. As ações "conferir a criança certa"; "conferir o medicamento com a prescrição" e "verificar a dose certa" obtiveram percentuais inferiores a 15%. Conclusão: medidas recomendadas pela literatura para administração de medicamentos não foram, em maioria, adotadas, tornando-se necessários treinamentos e protocolos específicos.


Subject(s)
Humans , Male , Female , Infant , Child, Preschool , Child , Adult , Child, Institutionalized , Administration, Oral , Drug Compounding/standards , Brazil , Interviews as Topic/methods , Drug Compounding/methods , Medication Errors/nursing , Middle Aged
11.
Rev. cuba. plantas med ; 21(2): 196-202, abr.-jun. 2016. tab
Article in Portuguese | LILACS | ID: lil-788936

ABSTRACT

Introdução: Musa sp., Musaceae, conhecida como bananeira, abundante no Brasil sendo utilizada para fins alimentares. Objetivos: microencapsular extratos de frutos de Musa sp. visando o desenvolvimento de material-prima enriquecida de polifenóis para formulação de alimentos funcionais. Métodos: os frutos de Musa cv. Vitória foram fornecidos pelo Incaper (Instituto Capixaba de Pesquisa, Assistência Técnica e Extensão Rural). Empregou-se extrato hidroalcóolico acidificado de frutos de banana. Determinações de polifenóis totais, taninos e flavonoides foram realizadas por método colorimétrico de Folin-Ciocalteau e complexação com cloreto de alumínio. A avaliação do potencial antioxidante foi realizada por ensaio de redução do radical 2,2-diphenyl-1-picrylhydrazyl. Microencapsulação realizada com dois biopolímeros. Fez-se uma análise de conservação de fenólicos com os microencapsulados. Os resultados foram submetidos à análise de variância e as médias comparadas pelo teste de Tukey (p < 0,05) e pelo teste de Mann-Whitney (p < 0,05). Resultados: a quantificação de fenólicos totais foi de 251,98 ± 0,1 mg/g de amostra e de taninos foi de 179,89 ± 0,01 mg/g de amostra. O teor de flavonoides totais foi abaixo do limite de quantificação. A atividade antioxidante por redução do radical 2,2-diphenyl-1-picrylhydrazyl teve CI50 > 5 mg/mL. A quantificação inicial nas microcápsulas em goma arábica de polifenóis totais e apresentou-se maior quando comparada à maltodextrina. Após o armazenamento do material, 12 dias, a -5 ºC, a goma arábica preservou os polifenóis e taninos em comparação à maltodextrina. Conclusões: pode-se empregar o extrato Musa cv. para matéria-prima como fonte de fenólicos totais e taninos. Em comparação dos biopolímeros utilizados, demonstrou-se que a maltodextrina tem menor capacidade de conservação de fenólicos totais e taninos(AU)


Introducción: Musa sp., Musaceae, conocido como plátano, abundante en Brasil se utiliza para fines alimenticios. Objetivos: microencapsular extractos de frutas microencapsulado de Musa sp. para el desarrollo de la materia prima enriquecida con polifenoles para la formulación de los alimentos funcionales. Métodos: los frutos de Musa cv. Vitória fueron proporcionados por Incaper (Capixaba Instituto de Investigación, Asistencia Técnica y Extensión Rural), Espírito Santo, Brasil. Preparación del extracto hidroalcohólico acidificado de frutos de plátano verde. Determinación de polifenoles totales, taninos y flavonoides fueron realizadas por colorimétria de Folin-Ciocalteu y complejación con cloruro de aluminio. Se realizó la evaluación del potencial antioxidante mediante el ensayo de reducción radical 2,2-difenil-1-picrilhidracilo. La microencapsulación se realiza con dos biopolímeros. Hubo un análisis de la conservación fenólico con microencapsulado. Los resultados fueron sometidos a análisis de varianza y las medias se compararon mediante la prueba de Tukey (p <0,05) y pela prueba de Mann-Whitney (p <0,05). Resultados: la cuantificación de fenoles totales fue 251,98 ± 0,1 mg/g de muestra y taninos fue 179,89 ± 0,01 mg/g de muestra. El contenido total de flavonoides estaba por debajo del límite de cuantificación. La actividad antioxidante por reducción radical 2,2-difenil-1-picrilhidracilo tenía IC50> 5 mg/mL. La cuantificación de los polifenoles totales y taninos que comienzan con el material microencapsulado acacia presentado sea mayor que con maltodextrina. Después del almacenamiento del material a -5 °C se cuantificó fenoles totales y taninos. La cuantificación de la maltodextrina ha demostrado una mayor pérdida de metabolitos. Conclusiones: se puede emplear el extracto de Musa cv. para materia-prima como fuente de fenoles totales y taninos. En biopolímeros de comparación utilizado, se demostró que la maltodextrina tiene una menor capacidad para preservar fenoles totales y taninos(AU)


Introduction: Musa sp., Musaceae, known as banana, abundant in Brazil being used for food purposes. Objectives: To microencapsulate fruit extracts of Musa cv. Vitória, for the development of raw material enriched with polyphenols for formulation of functional foods. Methods: The fruits of Musa cv. Vitória were provided by Incaper (Capixaba Institute of Research, Technical Assistance and Rural Extension). We applied acidified hydroalcoholic extract of banana fruit. Determinations of total polyphenols, tannins and flavonoids were performed by colorimetric method of Folin-Ciocalteu method and, complexation with aluminum chloride. Evaluation of antioxidant activity assay was performed by reduction of the radical 2.2-diphenyl-1-picrylhydrazyl. Microencapsulation performed with two biopolymers. There was a phenolic analysis with conservation microencapsulated. Data were analyzed by analysis of variance and means compared by Tukey test and by Mann-Whitney test (p < 0.05). Results: The quantification of total phenolics and tannins was 251.98 ± 0.1 mg / g sample and 179.89 ± 0.01 mg / g sample, respectively. The total flavonoid content was below the limit of quantification. The antioxidant activity by DPPH had IC50 > 5 mg / mL. The initial quantification in microcapsules in gum arabic total polyphenols and was higher compared to maltodextrin. After storage of the material 12 days, -5 °C, gum arabic preserved polyphenols and tannins compared to maltodextrin. Conclusion: Can use the Musa cv. extract for raw materials as a source of total phenolics and tannins. In comparison of biopolymers used, it was demonstrated that the maltodextrin has a lower retention capacity for total phenolics and tannins(AU)


Subject(s)
Humans , Musa/drug effects , Musa/chemistry , Drug Compounding/methods , Brazil
12.
Braz. j. pharm. sci ; 52(1): 27-34, Jan.-Mar. 2016. tab, graf
Article in English | LILACS | ID: lil-789087

ABSTRACT

ABSTRACT The present study describes the development of theophylline microcapsules by a non-solvent addition method and the effect of plasticizer addition on microencapsulation. The release was studied in distilled water and the data were analysed by various mathematical models for determining the mechanism of release. Prepared microcapsules were found to be spherical, free flowing and having more than 80% entrapped drug. The polymer - cellulose acetate phthalate and plasticizer - polyethylene glycol was considered to be affecting the properties of microcapsules including drug release (time for 50% drug release, T50). The formulation with the highest proportion of polymer and without plasticizer (F3) showed the slowest release with T50 = 4.3 h, while the formulation with lower proportion of polymer and 20% (w/w) plasticizer (F13 &14) showed the fastest release of drug with T50 values of 1.2 h and 1.3 h, respectively. The drug release from most of the formulations was found to be following Higuchi model. It is concluded from the results of the present study that cellulose acetate phthalate significantly affects the sustained release of the drug in water, whereas the addition of polyethylene glycol slightly enhances the drug release.


RESUMO O presente estudo descreve o desenvolvimento de microcápsulas de teofilina pelo método sem adição de solvente e o efeito da adição de plastificante na microencapsulação. A liberação foi estudada em água destilada e os dados foram analisados por vários modelos matemáticos para determinação do mecanismo de liberação. As microcápsulas preparadas mostraram-se esféricas, livres de corrente e com mais de 80% de fármaco encapsulado. O polímero - ftalato de acetato de celulose e o plastificante - polietileno glicol - afetaram as propriedades das microcápsulas, incluindo a liberação do fármaco (tempo para liberação de 50% do fármaco, T50). A formulação com a maior proporção de polímero e sem plastificante (F3) se mostrou como a de liberação mais lenta, com T50 = 4,3 h, enquanto as formulações com menor proporção de polímero e 20% de plastificante (m/m) (F13 &14) apresentaram a liberação mais rápida do fármaco, com T50 de 1,2 h e 1,3 h, respectivamente. A liberação do fármaco para a maioria das formulações seguiu o modelo de Higuchi. Concluiu-se, dos resultados do presente estudo, que o ftalato do acetato de celulose afeta significativamente a liberação controlada do fármaco em água, enquanto que a adição de polietileno glicol aumenta ligeiramente a liberação do fármaco.


Subject(s)
Theophylline/pharmacokinetics , Capsules/administration & dosage , Cetomacrogol/pharmacokinetics , Dibutyl Phthalate/pharmacokinetics , Pharmaceutical Preparations , Drug Compounding/methods , Drug Liberation
13.
Rev. Assoc. Med. Bras. (1992) ; 61(4): 368-374, July-Aug. 2015. tab
Article in English | LILACS | ID: lil-761721

ABSTRACT

SummaryIntroduction:chemotherapy is essential to treat most types of cancer. Often, there is chemotherapy waste in the preparation of drugs prescribed to the patient. Leftover doses result in toxic waste production.Objective:the aim of the study was to analyze chemotherapy waste reduction at a centralized drug preparation unit.Methods:the study was cross-sectional, observational and descriptive, conducted between 2010 and 2012. The data were obtained from chemotherapy prescriptions made by oncologists linked to a health insurance plan in Curitiba, capital of the state of Paraná, in southern Brazil. Dose and the cost of chemotherapy waste were calculated in each application, considering the dose prescribed by the doctor and the drug dosages available for sale. The variables were then calculated considering a hypothetical centralized drug preparation unit.Results:there were 176 patients with a cancer diagnosis, 106 of which underwent treatment with intravenous chemotherapy. There were 1,284 applications for intravenous anticancer medications. There was a total of 63,824mg in chemotherapy waste, the cost of which was BRL 448,397.00. The average cost of chemotherapy waste per patient was BRL 4,607.00. In the centralized model, there was 971.80mg of chemotherapy waste, costing BRL 13,991.64. The average cost of chemotherapy waste per patient was BRL 132.00.Conclusion:the use of centralized drug preparation units may be a strategy to reduce chemotherapy waste.


ResumoIntrodução:a quimioterapia é essencial no tratamento da maioria dos tipos de câncer. No processo de preparo da quimioterapia, com frequência, parte da medicação precisa ser descartada para se atingir a dose prescrita pelo médico. A dose excedente da medicação resulta na produção de resíduo tóxico.Objetivo:analisar a redução do resíduo de quimioterapia obtida por meio da centralização do preparo da medicação.Metodologia:foi realizado um estudo transversal observacional e descritivo entre 2010 e 2012, a partir da análise das prescrições de quimioterapia, pela auditoria médica de um plano de saúde, no estado do Paraná. Foi calculada a dose de quimioterapia desprezada e o seu custo, em cada aplicação, considerando a dose prescrita pelo médico e as apresentações comerciais das drogas. A mesma análise foi realizada em um modelo hipotético centralizado de preparo de quimioterapia.Resultados:foram identificados 176 pacientes, com diagnóstico de câncer, sendo que 106 pacientes realizaram um total de 1.284 aplicações endovenosas. Houve um total de 63.824 mg de resíduo de quimioterapia com custo de R$ 448.397,00. O custo médio de quimioterapia desprezada por paciente foi de R$ 4.607,00. No modelo centralizado de preparo houve 971,80 mg de resíduo com custo de R$ 13.991,64. Nesse modelo, o custo médio de quimioterapia desprezada por paciente seria de R$ 132,00.Conclusão:conclui-se que a centralização no preparo da medicação para o tratamento do câncer pode ser uma estratégia para reduzir os resíduos de quimioterapia.


Subject(s)
Aged , Female , Humans , Male , Middle Aged , Antineoplastic Agents/administration & dosage , Drug Compounding/methods , Neoplasms/drug therapy , Antineoplastic Agents/economics , Brazil , Cost Savings , Cross-Sectional Studies , Centralized Hospital Services/methods , Drug Costs , Drug Compounding/economics
14.
Braz. j. pharm. sci ; 51(2): 349-360, Apr.-June 2015. tab, ilus
Article in English | LILACS | ID: lil-755049

ABSTRACT

Three methods are proposed for the quantitative determination of raloxifene hydrochloride in pharmaceutical dosage form: ultraviolet method (UV) high performance liquid chromatography (HPLC) and micellar capillary electrophoresis (MEKC). These methods were developed and validated and showed good linearity, precision and accuracy. Also they demonstrated to be specific and robust. The HPLC and MEKC methods were tested in regards to be stability indicating methods and they showed to have this attribute. The UV method used methanol as solvent and optimal wavelength at 284 nm, obeying Lambert-Beer law in these conditions. The chromatographic conditions for the HPLC method included: NST column C18 (250 x 4.6 mm x 5 µm), mobile phase water:acetonitrile:triethylamine (67:33:0,3 v/v), pH 3.5, flow rate 1.0 mL min-1, injection volume 20.0 µl, UV detection 287 nm and analysis temperature 30 °C. The MEKC method was performed on a fused-silica capillary (40 cm effective length x 50 µm i.d.) using as background electrolyte 35.0 mmol L-1 borate buffer and 50.0 mmol L-1 anionic detergent sodium dodecyl sulfate (SDS) at pH 8.8. The capillary temperature was 32°C, applied voltage 25 kV, UV detection at 280 nm and injection was perfomed at 45 mBar for 4 s, hydrodimanic mode. In this MEKC method, potassium diclofenac (200.0 µg mL-1) was used as internal standard. All these methods were statistically analyzed and demonstrated to be equivalent for quantitative analysis of RLX in tablets and were successfully applied for the determination of the drug...


Três métodos são propostos para a quantificação de cloridrato de raloxifeno em sua forma farmacêutica de comprimidos: espectrofotometria no ultravioleta (UV), cromatografia líquida de alta eficiência (HPLC) e eletroforese capilar micelar (MEKC). Estes métodos desenvolvidos e validados demonstraram linearidade, precisão e exatidão. Também foram específicos e robustos. Os métodos HPLC e MEKC foram desenvolvidos para indicar a estabilidade do fármaco e demonstraram ter este atributo. O método UV usou metanol como solvente e comprimento de onda de 284nm, obedecendo a Lei de Lambert-Beer nestas condições. Os parâmetros cromatográficos para o método HPLC foram: coluna NST C18 (250 x 4,6 mm x 5 µm), fase móvel composta de água:acetonitrila:trietilamina (67:33:0,3 v/v), pH 3,5, vazão da fase móvel de 1,0 mL min-1, volume de injeção de 20 µl, detecção no comprimento de onda de 287 nm e temperatura de análise de 30°C. O método MEKC foi realizado utilizando capilar de sílica fundida (40 cm de comprimento efetivo x 50 µm de diâmetro interno) usando como fase móvel solução tampão borato 35.0 mmol L-1 e solução de dodecil sulfato de sódio (SDS) 50.0 mmol L-1 pH 8,8. A temperatura de análise foi de 32 °C, com voltagem aplicada de 25 kV, detecção no comprimento de onda de 280 nm e injeção da amostra realizada a 45 mBar por 4 s em modo hidrodinâmico. Para este método MEKC, foi utilizado diclofenaco de potássio (200.0 µg mL-1) como padrão interno. Todos os métodos foram analisados estatisticamente e demostraram ser equivalentes para a análise quantitativa de raloxifeno em comprimidos e foram aplicados com sucesso na determinação do fármaco...


Subject(s)
Humans , Raloxifene Hydrochloride/analysis , Raloxifene Hydrochloride/pharmacology , Drug Compounding/methods , Drug Stability , Chromatography, High Pressure Liquid/methods , Electrophoresis, Capillary/methods , Spectrum Analysis/methods
15.
Braz. j. pharm. sci ; 51(2): 265-272, Apr.-June 2015. ilus
Article in English | LILACS | ID: lil-755054

ABSTRACT

USP Apparatus 3 (reciprocating cylinder) is a very versatile device for the in vitro assessment of release characteristics of solid oral dosage forms, because it enables the product to be subjected to different dissolution media and agitation speeds in a single run. In this paper, a brief history and a description of this system are presented, along with its applications in the development of immediate and modified release products and in the simulation of fasted and fed states using biorelevant media. Furthermore, a comparison is made with the basket and paddle apparatus, especially highlighting the superior hydrodynamics of USP apparatus 3, since the results are not sensitive to factors such as the presence of sample collection probes or air bubbles in the dissolution medium...


USP aparato 3 (cilindros recíprocos) é um equipamento bastante versátil para a avaliação das características de liberação in vitro de formas farmacêuticas sólidas orais, pois permite que o produto seja submetido a diferentes meios de dissolução e condições de agitação, em um único ensaio. Neste trabalho, são apresentados um breve histórico e a descrição desse sistema, suas aplicações no desenvolvimento de produtos de liberação imediata e modificada, assim como sua utilização na simulação dos estados não alimentado e alimentado com o emprego de meios biorrelevantes. Além disso, uma comparação é estabelecida com o cesto e a pá, com destaque para a hidrodinâmica superior do USP aparato 3, que faz com que os resultados não sejam influenciados por fatores como o uso de sondas de coleta de amostras ou presença de bolhas de ar no meio de dissolução...


Subject(s)
Humans , Equipment and Supplies , Pharmacy/instrumentation , Laboratories , Drug Compounding/methods , Technology, Pharmaceutical/instrumentation
16.
Braz. j. pharm. sci ; 51(2): 461-466, Apr.-June 2015. tab, ilus
Article in English | LILACS | ID: lil-755065

ABSTRACT

Saxagliptin is a potent and selective inhibitor of the enzyme dipeptidyl peptidase 4. It is effective in the treatment of type 2 diabetes mellitus because it stimulates the pancreas to produce insulin. In the present study, a liquid chromatography method was developed and validated to quantify the drug in tablets. This method was based on the isocratic elution of saxagliptin, using a mobile phase consisting of 0.1% phosphoric acid at pH 3.0 - methanol (70: 30, v/v) at a flow rate of 1 mL.min-1 with UV detection at 225 nm. The chromatographic separation was achieved in 8 minutes on a Waters XBridge C18 column (250 mm x 4.6 mm, 5µm) maintained at ambient temperature. The proposed method proved to be specific and robust for the quality control of saxagliptin in pharmaceutical dosage forms, showing good linearity in the range of 15.0 - 100.0 µg.mL-1 (r>0.999), precision (RSD<1.49%) and accuracy values between 99.42 and 101.59%. The method was found to be stability indicating and was successfully applied for the analysis of saxagliptin in tablets in a routine quality control laboratory...


A saxagliptina é uma inibidora potente e seletiva da enzima dipeptidil peptidase 4. É efetiva no tratamento do Diabete mellitus tipo 2, pois estimula a produção de insulina pelo pâncreas. No presente estudo, desenvolveu-se e validou-se método por cromatografia líquida de alta eficiência para quantificar o fármaco em comprimidos. O método foi baseado em eluição isocrática, utilizando fase móvel constituída por ácido fosfórico 0,1% pH 3,0-metanol (70 : 30, v/v), fluxo de 1,0 mL.min-1, com detecção UV em 225 nm. A separação cromatográfica foi alcançada em 8 minutos em coluna Waters XBridge C18 (250 mm x 4,6 mm, 5 µm) mantida à temperatura ambiente. O método proposto mostrou-se específico e robusto para o controle de qualidade de saxagliptina em comprimidos, sendo linear na faixa de concentração de 15,0-100,0 µg.mL-1 (r>0,999), preciso (RSD<1,49%) e exato, com resultados entre 99,42 e 101,59%. O método mostrou-se indicativo de estabilidade e foi aplicado com sucesso no controle de qualidade de saxagliptina em comprimidos...


Subject(s)
Humans , Drug Compounding/methods , Chromatography, Liquid/methods , Diabetes Mellitus/drug therapy , Enzyme Inhibitors/pharmacology , Clinical Chemistry Tests/methods
17.
Braz. j. pharm. sci ; 50(4): 741-748, Oct-Dec/2014. tab, graf
Article in English | LILACS | ID: lil-741335

ABSTRACT

Calcium alginate beads containing pomegranate peels' polyphenol extract were encapsulated by ionic gelation method. The effects of various formulation factors (sodium alginate concentration, calcium chloride concentration, calcium chloride exposure time, gelling bath time maintaining, and extract concentration) on the efficiency of extract loading were investigated. The formulation containing an extract of 1 g pomegranate peels in 100 mL distilled water encapsulated with 3 % of sodium alginate cured in 0.05 M calcium chloride for 20 minutes and kept in a gelling bath for 15 minutes was chosen as the best formula regarding the loading efficiency. These optimized conditions allowed the encapsulation of 43.90% of total extracted polyphenols and 46.34 % of total extracted proanthocyanidins. Microencapsulation of pomegranate peels' extract in calcium alginate beads is a promising technique for pharmaceutical and food supplementation with natural antioxidants.


Pérolas de alginato de cálcio, contendo polifenóis de extrato de casca de romã, foram encapsuladas pelo método de gelificação iônica. Os efeitos de vários fatores de formulação (concentração de alginato de sódio, concentração de cloreto de cálcio, cloreto de cálcio, o tempo de exposição, o tempo de manutenção do banho de gelificação e a concentração do extrato) sobre a eficiência de carga do extrato foram investigados. A formulação que contém 1 g extrato de casca de romã em 100 mL de água destilada, encapsulado com 3% de alginato de sódio curada em 0,05 M de cloreto de cálcio durante 20 minutos e mantido em banho de gelificação por 15 min foi escolhida como a melhor em relação à eficiência de carga. Estas condições otimizadas permitem o encapsulamento de 43,90% do total de polifenóis extraídos e de 46,34% do total de proantocianidinas extraídas. A microencapsulação de extrato de cascas de romã em esferas de alginato de cálcio é uma técnica promissora para a suplementação farmacêutica e de alimentos com antioxidantes naturais.


Subject(s)
/analysis , Polyphenols , Drug Compounding/methods , Antioxidants/analysis
18.
Braz. j. microbiol ; 44(3): 777-783, July-Sept. 2013. ilus, graf, tab
Article in English | LILACS | ID: lil-699810

ABSTRACT

In the present study, the cells of Bifidobacterium animalis subsp. lactis (BI-01) and Lactobacillus acidophilus (LAC-04) were encapsulated in cocoa butter using spray-chilling technology. Survival assays were conducted to evaluate the resistance of the probiotics to the spray-chilling process, their resistance to the simulated gastric and intestinal fluids (SGF and SIF), and their stability during 90 days of storage. The viability of the cells was not affected by microencapsulation. The free and encapsulated cells of B. animalis subsp. lactis were resistant to both SGF and SIF. The micro-encapsulated cells of L. acidophilus were more resistant to SGF and SIF than the free cells; the viability of the encapsulated cells was enhanced by 67%, while the free cells reached the detection limit of the method (10³ CFU/g). The encapsulated probiotics were unstable when they were stored at 20 °C. The population of encapsulated L. acidophilus decreased drastically when they were stored at 7 °C; only 20% of cells were viable after 90 days of storage. The percentage of viable cells of the encapsulated B. animalis subsp.lactis, however, was 72% after the same period of storage. Promising results were obtained when the microparticles were stored at -18 °C; the freeze granted 90 days of shelf life to the encapsulated cells. These results suggest that the spray-chilling process using cocoa butter as carrier protects L. acidophilus from gastrointestinal fluids. However, the viability of the cells during storage must be improved.


Subject(s)
Bifidobacterium/physiology , Biotechnology/methods , Drug Compounding/methods , Lactobacillus acidophilus/physiology , Microbial Viability/drug effects , Microbial Viability/radiation effects , Probiotics/pharmacology , Aerosols , Drug Stability , Dietary Fats/metabolism , Temperature , Technology, Pharmaceutical/methods
19.
Rev. Esc. Enferm. USP ; 47(1): 53-60, fev. 2013. ilus, graf, tab
Article in Portuguese | LILACS, BDENF | ID: lil-668192

ABSTRACT

Esta pesquisa teve como objetivo identificar a forma farmacêutica dos medicamentos preparados para serem administrados por cateteres e o perfil dos erros cometidos durante o preparo. Trata-se de estudo epidemiológico transversal, de natureza observacional, conduzido em uma unidade de terapia intensiva com amostra de 350 doses de medicamentos preparados por 56 técnicos de enfermagem. A coleta de dados ocorreu no mês de março de 2010. Os resultados mostram que 92% dos medicamentos eram sólidos. Os erros foram agrupados nas categorias diluição e mistura para formas líquidas, acrescidos de trituração para sólidos. As taxas de erro foram superiores a 40% em todas as categorias. Concluiu-se que: a trituração indevida pode ter comprometido o resultado terapêutico em comprimidos revestidos e de liberação controlada; não diluir xaropes pode ter contribuído para a obstrução de cateteres; misturar medicações ao triturá-las pode aumentar o risco de interações farmacêuticas.


The goals of the research were to assess the pharmaceutical form of medicinal preparations administered through catheters and identify the profile of errors that occur during their preparation. This is a cross-sectional study of an observational nature, conducted in an intensive care unit with a sample of 350 doses of medication prepared by 56 nursing technicians. Data collection occurred in March 2010. The results showed that 92% of the drugs were in the solid form. The errors were divided into two categories for liquid forms: dilution and mixing, and grinding was added as an error possibility for a solid form. The error rates were greater than 40% in all categories. The conclusions are that grinding can compromise the therapeutic effect of coated controlled-release tablets, not diluting syrups may contribute to the obstruction of catheters, and mixing medication during grinding may increase the risk of drug interactions.


Se apuntó a identificar la forma farmacéutica de los medicamentos preparados para ser administrados vía catéter y el perfil de errores cometidos durante la preparación. Estudio epidemiológico transversal, de tipo observacional, desarrollado en unidad de terapia intensiva sobre muestra de 350 dosis de medicamentos preparados por 56 técnicos de enfermería. Datos recolectados en marzo de 2010. Los resultados expresan que 92% de los medicamentos eran sólidos. Los errores se agruparon en las categorías: dilución y mezcla para formas líquidas, agregados de trituración para sólidos. Las tasas de errores superaron el 40% en todas las categorías. Se concluye en que: la trituración inapropiada pudo comprometer el resultado terapéutico con comprimidos revestidos y de liberación controlada; no diluir jarabes pudo haber ayudado a obstruir catéteres, y mezclar medicamentos al triturarlos puede aumentar el riesgo de interacciones medicamentosas.


Subject(s)
Humans , Catheters , Drug Compounding/methods , Intensive Care Units , Medication Errors/nursing , Cross-Sectional Studies , Medication Errors/statistics & numerical data
20.
Article in Spanish | LILACS, BINACIS | ID: biblio-1170950

ABSTRACT

BACKGROUND: In the hospital setting is frequent to manipulate solid dosage forms (SDF, tablets 16 and capsules), which can affect their physicochemical and biopharmaceutical properties, the pharmacoloeffect and sometimes to cause the appearance of undesirable side effects. OBJECTIVES: To identify the medicines whose SDF is altered in a Hospital of Cordoba (Argentina), to determine how these modifications are made and to establish whether they were properly performed or not. METHODS: We retrospectively analyzed the prescriptions made between the 5th and the 11th of March of 2012 and identified impaired requesting SDF modifications. Open interviews were held with nurses and service visits to each hospital to determine how they manipulated the SDF. RESULTS: We analyzed 700 prescriptions for 113 patients, of which 61 (54


) had manipulations of the received SDF (49 for medical prescription, 7 because they had nasogastric tubes, 3 due to patient choice and 2 by nursing decision). Twenty three medicines were manipulated, but only 12 were correctly manipulated. The major changes were partition of tablets and grinding of tablets or microgranules and dispersible in water. CONCLUSION: The SDF of several medicines is altered in the analyzed hospital, many times without medical indication and scientific justification. It would be appropriate to conduct training courses and establish closer collaborations between pharmacy and nursing units in the investigated hospital.


Subject(s)
Tablets/chemistry , Capsules/chemistry , Drug Prescriptions/statistics & numerical data , Administration, Oral , Argentina , Drug Compounding/methods , Tablets/administration & dosage , Capsules/administration & dosage , Retrospective Studies , Humans , Practice Patterns, Physicians' , Practice Patterns, Nurses' , Drug Prescriptions/standards , Dose-Response Relationship, Drug , Drug Administration Routes
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