RESUMEN
Syzygium cumini L. Skeels belongs to Myrtaceae family. This species has been recognized by its antidiabetic, anti-inflammatory, and antimicrobial activities. Despite ever-increasing scientific interest for this species there is no pharmacopeia method for characterization and standardization of S. cumini yet. So, toward this aim, the objective of this work was to develop an efficient analytical methodology able to determine polyphenols and tannins content from leaves hydroethanolic extract of S. cumini using Folin-Ciocalteu method by ultraviolet absorption spectrophotometry (UV-Vis). The analytical methodology was developed for the first time in the literature for leaves of this specie shown to be fast and low-cost with results expressed through tannic acid equivalent (TAE). Moreover, the methodology presented selectivity with maximum absorption at 706 nm wavelength, linearity with R2>0.99; limit of detection 0.275 µg TAE mL-1 and 0.102 µg TAE mL-1; limit of quantification 1.046 µg TAE mL-1 and 0.912 µg TAE mL-1 for total polyphenols and total tannins, respectively. Furthermore, the methodology was accurate with recover value greater than 98%, as well as exact, reproductive, and robust with coefficient of variation values less than 15% for both compounds. All the results are found within the fixed limits according to RDC 166/2017.
Asunto(s)
Syzygium , Antioxidantes , Extractos Vegetales , Hojas de la Planta , Polifenoles , TaninosRESUMEN
The present study consisted in optimizing the extractive method of polyphenols and total tannins of leaves of Syzygium cumini (L) Skeels assisted by microwaves to potentiate the antimicrobial activity of the dried extract of S. cumini against sensitive and resistant strains. A Box-Behnken design that consisted of 27 experimental runs coupled with a desirability function for multiple response optimization was employed to optimize the total polyphenols content and total tannins content. Antimicrobial sensitivity tests were evaluated by obtaining the minimum inhibitory concentration, minimum fungicidal concentration and minimum bactericidal concentration in 96-well petri dishes. The optimal extraction conditions were found to be 8 min of extraction, under 300 w of microwave power, using a 1:34 g/mL solid/solvent ratio and 38% of ethanol concentration as extraction solvent. The parameter with the greatest influence in the extraction was primarily the time, followed by the potency and proportion solid/solvent. This yielded a total polyphenol content of 87.37 ± 1.85 mg TAE g-1ext and a total tannin content of 79.68 ± 1.64 mg TAE g-1 ext. All tested microorganisms were sensitive to the extract, evidencing the effectiveness of the extraction method optimization.
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Polifenoles , Syzygium , Antioxidantes , Microondas , Extractos Vegetales/farmacología , Hojas de la Planta , Proyectos de Investigación , TaninosRESUMEN
Triplaris gardneriana is used by traditional medicine. The objective of this work was the leaves chemical study with isolate, identify and quantify the chemical constituent, validate the analytical method and evaluate the antibacterial activity. The ethyl acetate and chloroform fractions were subjected to column chromatography for isolation of the compounds quercetin and lupeol, respectively. For the identification, quantification of quercetin in the samples and validation of method were performed using HPLC-DAD. The antibacterial activity was evaluated by the microdilution method. The isolated phytochemicals are being reported for the first time in the species. The ethyl acetate fraction showed a higher content of quercetin with 9.967 ± 1.01 mg.g-1. The method was validated. The samples showed good antibacterial activity. In this study, quercetin was isolated and quantified in the species being a great alternative as a producer of this secondary metabolite, which can be safely applied in the quality control analysis.
Asunto(s)
Antibacterianos/farmacología , Polygonaceae/química , Quercetina , Antibacterianos/aislamiento & purificación , Cromatografía Líquida de Alta Presión , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Extractos Vegetales , Hojas de la Planta/química , Quercetina/aislamiento & purificación , Quercetina/farmacologíaRESUMEN
BACKGROUND: The health area in its most diverse fields has progressively incorporated nanotechnology into its products, such as in dermatology. In this sector, nanoparticles are one of the strategies that allow improvements, both in terms of value-added, as well as the efficacy, safety and stability of products for cosmetic or therapeutic purposes. OBJECTIVE: To understand the scenario of development and innovation of dermatological products with nanoparticles, through a patent prospection, evaluating the annual evolution, the main technology investors countries, the profile of the depositors, besides the uses and purposes of the products. METHODS: The Espacenet® database was used for consultation, using the search term "nanoparticle and skin". A total of 285 patents were found, of which 208 were available and 89 were based on the scope. RESULTS: There was a progressive evolution in the number of patents after the year 2000, with South Korea, the United States, China and Japan as the main depositor countries. Private companies and Education and Research Institutions were the entities with the largest amount of deposits. The cosmetic purpose was the predominant use compared to the therapeutic one. The most prominent nanoparticles were polymeric, metallic and lipid, while the therapeutic area presented a larger number of the functionalized ones. CONCLUSION: The market for dermatological products has been innovating and growing over the years through the use of nanoparticles, evidencing a prominent development of nanotechnology-based cosmetics. Countries investing in nanotechnology and major developers of innovative products are highlighted in this scenario.
Asunto(s)
Dermatología , Invenciones , Nanopartículas/química , Patentes como Asunto , Cosméticos , HumanosRESUMEN
Alternanthera brasiliana is popularly known as 'penicillin' and used as an anti-inflammatory and for wound healing. The objective of this work was the phytochemical study of the species by analytical techniques such as LC-MS/MS and GC-MS. Twenty-seven compounds were identified, five by LC-MS and 22 by GC-MS analysis. All compounds identified by LC-MS are flavonoids. However, several classes were found in GC-MS analysis, such as hydrocarbons, diterpenes, monoterpenes, vitamin and carotenoid derivatives, phytosterols and triterpenes. In the analysis, it is suggested the presence of 27 substances, of which 23 are unpublished for the species, that reaffirms the importance of this study and the contribution to chemical knowledge.
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Amaranthaceae/química , Fitoquímicos/análisis , Antiinflamatorios , Carotenoides/análisis , Cromatografía Liquida/métodos , Flavonoides/análisis , Cromatografía de Gases y Espectrometría de Masas/métodos , Fitoquímicos/aislamiento & purificación , Fitosteroles/análisis , Extractos Vegetales/química , Espectrometría de Masas en Tándem/métodos , Terpenos/análisis , Cicatrización de HeridasRESUMEN
Cirsiliol is a flavone found in many Lamiaceae species with high cytotoxic activity against tumor cell lines. Although cirsiliol is being used in cancer therapy, its pharmacological potential is limited by its low solubility and bioavailability. In this paper, a cirsiliol-ß-cyclodextrin inclusion complex was developed in order to increase its solubility and bioavailability. The formation of inclusion complex was proved by scanning electron microscopy, Fourier-transform infrared spectroscopy (FTIR) and nuclear magnetic resonance (NMR) and solubility increment was verified through the ultraviolet-visible (UV-Vis) method. The cytotoxic effect against tumor cells (PC3, HCT-116 and HL-60 human cell lines, and S-180 murine cell line) and the antitumor activity in mice bearing sarcoma S-180 were also investigated. The inclusion complex was obtained with 71.45% of total recovery and solubility 2.1 times higher compared to the compound in its free form. This increment in solubility was responsible by a tumor growth inhibition potentiation (1.5 times greater compared to compound in its free form). In addition, this study showed that cirsiliol and its inclusion complex in ß-cyclodextrin have strong antitumor potential at low doses without promoting side effects commonly observed for conventional drugs as doxorubicin.
RESUMEN
Drug candidate LPSF/FZ4 with promising schistosomicidal properties in vitro was previously synthesized. However, LPSF/FZ4 has limited aqueous solubility (<1⯵g/mL), leading to ineffective dissolution and, therefore, no meaningful in vivo comparative studies could be pursued. This study was aimed to develop a proper amorphous solid dispersion (SD) to enhance the solubility and dissolution rate of LPSF/FZ4 such that its biological activity could be investigated. To better understand its physiological behavior, the pKa of LPSF/FZ4, a monoprotic weak acid with NH group at the imidazolidine ring, was first determined to be 8.13 using an automated SiriusT3. The development of SD systems for LPSF/FZ4 involved the evaluation of various water-soluble polymer carriers such as PVP K-29/32, PVP K-90, HPMC K4M, PVPVA 64 and SOLUPLUS®. The most promising SD systems were selected through in vitro dissolution studies under nonsink conditions, together with physicochemical characterization as well as accelerated stability study. It was shown that SD of 10% LPSF/FZ4 in SOLUPLUS® and PVP K-90 could significantly increase the area-under-the-curve value of the nonsink dissolution profile (AUC values of the SD in SOLUPLUS® and PVP K-90 were 1381.03 and 1342.34⯵L/mL·min, respectively, and that of the pure crystalline drug was 0.02⯵L/mL·min), a useful surrogate for the in vivo bioavailability. Cmax values for the SD in SOLUPLUS® (12.50⯵L/mL) and PVP K-90 (25.86⯵L/mL) were also higher than the one of the crystalline drug (0.02⯵L/mL). The SD system of LPSF/FZ4 in SOLUPLUS® showed a significant increase in schistosomicidal activity in an animal model as compared with the conventional treatment using crystalline drug, consistent with the AUC trend from the nonsink dissolution. Thus this SD system of LPSF/FZ4 could be useful as a potential formulation for treating schistosomiasis.
Asunto(s)
Compuestos de Bencilideno/química , Compuestos de Bencilideno/farmacología , Hidantoínas/química , Hidantoínas/farmacología , Polímeros/química , Esquistosomiasis/tratamiento farmacológico , Animales , Disponibilidad Biológica , Química Farmacéutica/métodos , Portadores de Fármacos/química , Composición de Medicamentos/métodos , Femenino , Hidantoínas/farmacocinética , Ratones , Solubilidad/efectos de los fármacosRESUMEN
Inflammation is a protective reaction of the microcirculation. However, sustained inflammation can lead to undesired effects. Thuja occidentalis Linn has many pharmacological properties but has no anti-inflammatory activity described. Thus, this study aims evaluating the anti-inflammatory activity of the aqueous extract (AE) and the polysaccharide fraction (PLS) of T. occidentalis L. in mice. The results of our evaluations in various experimental models indicated that AE and PLS (3, 10, and 30mg/kg, i.p.) reduced (pË0.05) paw edema induced by carrageenan, dextran sulfate (DEX), compound 48/80, serotonin (5-HT), bradykinin (BK), histamine (HIST), and prostaglandin E2 (PGE2). Furthermore, it inhibited neutrophils recruitment; decreased MPO activity, tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) levels, vascular permeability, nitrite concentration, and MDA concentration; and maintained the GSH levels in the peritoneal exudate. The AE and PLS reduced neutrophil infiltration and cyclooxygenase (COX)-2 and inducible nitric oxide synthase (iNOS) immunostaining in paw tissue. Treatment with the AE and PLS (300mg/kg) did not induce gastric toxicity. In conclusion, these results show that the AE and PLS reduced the inflammatory response by inhibiting vascular and cellular events, inhibiting pro-inflammatory cytokine production, and reducing oxidative stress. Furthermore, they did not induce gastric toxicity at high doses.
Asunto(s)
Antiinflamatorios/farmacología , Polisacáridos/farmacología , Thuja/química , Agua/química , Animales , Antiinflamatorios/uso terapéutico , Permeabilidad Capilar/efectos de los fármacos , Edema/tratamiento farmacológico , Edema/metabolismo , Glutatión/metabolismo , Interleucina-6/metabolismo , Masculino , Malondialdehído/metabolismo , Ratones , Óxido Nítrico/biosíntesis , Cavidad Peritoneal , Peritonitis/tratamiento farmacológico , Peroxidasa/metabolismo , Polisacáridos/uso terapéutico , Factor de Necrosis Tumoral alfa/metabolismoRESUMEN
Several factors can intervene in the molecular properties and consequently in the stability of drugs. The molecular complexes formation often occur due to favor the formation of hydrogen bonds, leading the system to configuration more energy stable. This work we aim to investigate through theoretical and experimental methods the relation between stability and properties of molecular complexes the molecular complex formed between the drugs, efavirenz (EFV), lamivudine (3TC) and zidovudine (AZT). With this study was possible determining the most stable complex formed between the compounds evaluated. In addition the energy and structural properties of the complex formed in relation to its individual components allowed us to evaluate the stability of the same.
Asunto(s)
Fármacos Anti-VIH/química , Benzoxazinas/química , Lamivudine/química , Zidovudina/química , Alquinos , Ciclopropanos , Interacciones Farmacológicas , Estabilidad de Medicamentos , Enlace de Hidrógeno , Simulación del Acoplamiento Molecular , Simulación de Dinámica Molecular , TermodinámicaRESUMEN
This study aimed to evaluate the mechanism associated with cytotoxic activity displayed by the drug 5-fluorouracil incorporated in Cu-BTC MOF and its slow delivery from the Cu-BTC MOF. Structural characterization encompasses elemental analysis (CHNS), differential scanning calorimetry (DSC), thermogravimetric analysis (TG/DTG), Fournier transform infrared (FIT-IR) and X-ray diffraction (XRD) was performed to verify the process of association between the drug 5-FU and Cu-BTC MOF. Flow cytometry was done to indicate that apoptosis is the mechanism responsible for the cell death. The release profile of the drug 5-FU from Cu-BTC MOF for 48 hours was obeisant. Also, the anti-inflammatory activity was evaluated by the peritonitis testing and the production of nitric oxide and pro-inflammatory cytokines were measured. The chemical characterization of the material indicated the presence of drug associated with the coordination network in a proportion of 0.82 g 5-FU per 1.0 g of Cu-BTC MOF. The cytotoxic tests were carried out against four cell lines: NCI-H292, MCF-7, HT29 and HL60. The Cu-BTC MOF associated drug was extremely cytotoxic against the human breast cancer adenocarcinoma (MCF-7) cell line and against human acute promyelocytic leukemia cells (HL60), cancer cells were killed by apoptosis mechanisms. The drug demonstrated a slow release profile where 82% of the drug was released in 48 hours. The results indicated that the drug incorporated in Cu-BTC MOF decreased significantly the number of leukocytes in the peritoneal cavity of rodents as well as reduced levels of cytokines and nitric oxide production.
Asunto(s)
Antimetabolitos Antineoplásicos/farmacología , Apoptosis/efectos de los fármacos , Cobre/química , Portadores de Fármacos/química , Fluorouracilo/farmacología , Compuestos Organometálicos/química , Ácidos Tricarboxílicos/química , Animales , Antimetabolitos Antineoplásicos/administración & dosificación , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Preparaciones de Acción Retardada , Femenino , Fluorouracilo/administración & dosificación , Humanos , RatonesRESUMEN
OBJECTIVE AND DESIGN: The purpose of this study was to evaluate the anti-inflammatory and anti-arthritic activities of 3,4-dihydro-2,2-dimethyl-2H-naphthol[1,2-b]pyran-5,6-dione (ß-lapachone; ß-lap) and to elucidate its probable mode of action. METHODS: Carrageenan-induced paw edema, cell migration evaluation and production of pro-inflammatory cytokines tumor necrosis factor (TNF)-α, interleukin (IL)-6 and nitric oxide were used for this study. Freund's complete adjuvant (FCA)-induced arthritis was used as a model of chronic inflammation. ß-Lap was tested in doses of 40 and 60 mg/kg, orally. RESULTS: In the paw edema test, the dose of 60 mg/kg gave a higher percentage inhibition of edema (49.3 %) than control. ß-Lap inhibited neutrophil migration and reduced concentrations of TNF-α, IL-6 and NO in peritoneal exudates of animals with peritonitis. In the arthritis test, ß-lap inhibited edema and NO production in the serum of treated animals. CONCLUSION: Significant anti-inflammatory and anti-arthritic activities were observed in animals treated with ß-lap. The effects of ß-lap can be attributed in part to immunomodulation with reduction of pro-inflammatory cytokines and NO.
Asunto(s)
Antiinflamatorios/farmacología , Artritis Experimental/tratamiento farmacológico , Naftoquinonas/farmacología , Animales , Artritis Experimental/inmunología , Edema/tratamiento farmacológico , Femenino , Interleucina-6/análisis , Masculino , Ratones , Naftoquinonas/uso terapéutico , Óxido Nítrico/análisis , Ratas , Ratas Wistar , Factor de Necrosis Tumoral alfa/análisisRESUMEN
Benznidazole (BNZ) is the drug of choice for Chagas disease treatment, which affects about 9.8 million people worldwide. It has low solubility and high toxicity. The present study aimed to develop and characterize inclusion complexes (IC) in binary systems (BS) with BNZ and randomly methylated-ß-cyclodextrin (RMßCD) and in ternary systems (TS) with BNZ, RMßCD and hydrophilic polymers. The results showed that the solid BS had a large increase in dissolution rate (Q>80%). For the solid IC obtained, the kneading method, in ratio of 1:0.17 (77.8% in 60 min), appeared to be the most suitable for the development of a solid oral pharmaceutical product, with possible industrial scale-up and low concentration of CD. The solid TS containing 0.1% of hydroxypropylmethylcellulose (HPMC) showed no significant advantages compared to the binary IC in solid state. The use of cyclodextrins proved to be a viable tool for effective, standardized and safe drug delivery.
Asunto(s)
Sistemas de Liberación de Medicamentos , Nitroimidazoles/química , Tripanocidas/química , beta-Ciclodextrinas/química , Interacciones Hidrofóbicas e Hidrofílicas , Derivados de la Hipromelosa/química , Metilación , Povidona/química , SolubilidadRESUMEN
The present study investigates the release mechanism of benznidazole (BNZ) in solid dispersions with polyethylene glycol 6000 (PEG 6000) and polyvinylpirrolydone K-30 (PVP K-30), with a view to observing the increase in solubility of BNZ in water in the presence of these two hydrophilic polymers. The interaction of BNZ with the polymers was evaluated using scanning electron microscopy, Fourier-transformation infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, and in vitro dissolution tests, and a theoretical study of molecular modeling was also carried out. The drug-polymer interaction was studied trough molecular modeling, using density functional theory with the B3LYP exchange correlation function. The corrected interaction energies were calculated to be -20.9 kJ/mol with PVP and -6.6 kJ/mol with PEG. The experimental and theoretical results indicate that a powerful interaction occurred between BNZ and the polymers, which was especially strong in the case of PVP, and that this interaction contributed to improvement of BNZ solubility.
Asunto(s)
Portadores de Fármacos/química , Composición de Medicamentos/métodos , Nitroimidazoles/administración & dosificación , Polietilenglicoles/química , Povidona/química , Tripanocidas/administración & dosificación , Rastreo Diferencial de Calorimetría , Estabilidad de Medicamentos , Interacciones Hidrofóbicas e Hidrofílicas , Microscopía Electrónica de Rastreo , Modelos Moleculares , Estructura Molecular , Nitroimidazoles/química , Solubilidad , Espectroscopía Infrarroja por Transformada de Fourier , Propiedades de Superficie , Tripanocidas/química , Difracción de Rayos XRESUMEN
Própolis é uma mistura complexa, formada por material resinoso e balsâmico. Sua composição química é complexa e variada, estando relacionada com a flora de cada região visitada pelas abelhas e com o período de coleta da resina. Inclui flavonóides, ácidos aromáticos, terpenóides e fenilpropanóides, ácidos graxos e vários outros compostos. A própolis tem sido objeto de intensos estudos farmacológicos e químicos nos últimos 30 anos. Em várias partes do mundo é indicada para melhorar a saúde e prevenir doenças. Atualmente, é disponível em várias formas farmacêuticas como cápsulas, extratos, enxaguatório bucal, na forma de pó, entre outras. Ainda são necessários estudos correlacionando a composição química com a atividade biológica, definindo cada tipo de própolis com a sua aplicação terapêutica. É uma tarefa imprescindível para um mercado cada vez maior e exigente em todo o mundo.
Propolis (bee glue) is a complex mixture, formed by resinous and balsamic material. Its chemical composition is variable and complex, being related with the flora of each region visited by the bees and with the period of resins collection. Flavonoids, aromatic acids, terpenoids and phenylpropanoids, fatty acids, and other compounds are found in propolis. In the last 30 years, propolis has become subject of intense pharmacological and chemical studies. In different parts of the world it is indicated to improve health and prevent illnesses. Currently, it is available in some pharmaceutical forms as capsules, extracts, mouthrinses, powder form, among others. Indeed, studies correlating the chemical composition with the biological activity are necessary, defining each type of propolis with its therapeutic application. It is an essential task for a market ever bigger and demanding in the whole word.
RESUMEN
Furosemide (40mg) was administered to 20 street dogs, 10 males and 10 females, in two different pharmaceutical forms: (1) compressed furosemide 40mg formulated at the Federal University of Pernambuco (UFPE-tablet), and (2) a commercial formulation with equal bioequivalence produced by the Laboratory for Pharmaceutical Technology of Pernambuco State (LAFEPE), the LAFEPE-furosemide. The study aimed to evaluate the kinetics of dissolution of the UFPE-tablet in order to analyze the behavior of bioavailability of the best formulation for veterinary use. The plasmatic concentrations of furosemide for the determination of parameters of pharmacological kinetics were analyzed by high-performance liquid chromatographic method (HPLC). The in vitro study accomplished through physiochemical analyses demonstrated that the formulas of the furosemide tablets attained the pharmaceutical requirements in agreement with USP 23 and the Brazilian Pharmacopoeia. The evaluation accomplished in dogs with UFPE-tablets given in only dose demonstrated uniformity in blood levels indicating stability in maintenance of the pharmaceutical formulation and efficiency in absorption of the active compound. These values are not significantly different in relation to the 5 percent confidence limit. Regarding maximum concentration (Tmax) time and global bioavaibility assessed by AUC means, there were no considerable differences as well. UFPE-furosemide displayed 743.492µg/mL.h as AUC average value whereas LAFEPE-furosemide had an average of 537.284µg/mL.h.
Furosemida (40mg) foi administrada a 20 cães de rua (cães SRD), 10 machos e 10 fêmeas, em duas formas farmacêuicas distintas: (1) furosemida comprimido 40mg formulada na Universidade Federal de Pernambuco (UFPE-comprimido) e (2) uma formulação comercial bioequivalente produzida pelo Laboratório de Tecnologia Farmacêutica do Estado de Pernambuco (LAFEPE-furosemida). O estudo objetivou avaliar a cinética de dissolução do UFPE-comprimido para analisar o comportamento da liodisponibilidade dos comprimidos buscando a melhor formulação para uso veterinário. As concentrações plasmáticas de furosemida para determinação de parâmetros farmacocinéticos, foram analisadas por cromatografia líquida de alto desempenho (HPLC). O estudo in vitro realizado através de análises físico-químicas demonstrou que as fórmulas dos comprimidos de furosemida preencheram os requisitos farmacêuticos de acordo com USP 23 e a Farmacopéia Brasileira. Avaliações realizadas em cães da formulação UFPE-comprimidos administrados em dose única, demonstrou uma uniformidade nos níveis sangüíneos indicando estabilidade na manutenção da forma farmacêutica e eficiência na absorção do princípio ativo. Estes valores não são significativamente diferentes em relação ao limite de confiança de 5 por cento. Em relação a concentração de máximo (Tmax) e ao tempo de biodisponibilidade global avaliados por meios de AUC, não houve nenhuma diferença considerável. O comprimido UFPE-furosemide exibiu AUC de 743.492µg/mL.h e o LAFEPE-furosemide teve uma média de 537.284µg/mL.h.
Asunto(s)
Animales , Absorción , Perros , Furosemida/administración & dosificación , Furosemida/efectos adversos , FarmacocinéticaRESUMEN
O extrato de tubérculos de Operculina macrocarpa (Jalapa do Brasil) é um produto fitoterápico, com eficácia no tratamento de constipação, como laxante. A resina quantificada é extraída com solução hidroalcóolica apresentando constituintes orgânicos e inorgânicos, podendo ser dividida em duas frações principais: uma solúvel em éter, chamada de jalapina e outra, mais polar, ainda pouco estudada, denominada convolvulina. O interesse principal deste trabalho foi propor uma otimização da metodologia gravimétrica para doseamento da resina descrita na Farmacopéia Brasileira primeira edição e sua validação com o objetivo de diminuir os custos e o tempo de partição das fases. Os resultados obtidos na validação foram tratados estatisticamente por análise de variância one-way (ANOVA) e teste t de Student. O método demonstrou atender aos requisitos de boas práticas em laboratórios exigidos pela legislação brasileira em vigor, RE n° 899 de 29 de maio de 2003 da Agência Nacional de Vigilância Sanitária, sendo, portanto, sensível, exato e preciso para o doseamento do extrato de Operculina macrocarpa, conhecida popularmente como Jalapa-do-Brasil.
The tubercle extract of Operculina macrocarpa (Jalap of Brazil) is a phytomedicine, with effectiveness in the treatment of constipation, as laxative. The quantified resin is extracted with hydro-alcoholic solution, presenting organic and inorganic constituents, separable in two main fractions: one soluble in ether, called jalapina and other, more polar, still little studied, called convolvulina. The main objective of this work was to consider the optimization of the gravimetrical methodology for assay of the resin described in the Brazilian Pharmacopeia, First Edition and its validation, with the objective to diminish the costs and the partition time of the phases. The results achieved in the validation had been statistically treated by one-way Variance Analysis (ANOVA) and t test of Student. The method demonstrated to attend to the Good Manufacture Practice requirements for laboratories, demanded by actual brazilian law, RE n° 899 of May 29th of 2003 from the National Agency of Sanitary Vigilance, being therefore, sensible, accurate and precise for the assay of the Operculina macrocarpa extract, known popularly as Jalap of Brazil.
RESUMEN
This study aimed to analyze the final fermentation culture of Bacillus sphaericus 2362, standardize it and develop an active tablet formulation for use in urban mosquito breeding sites. It was performed in three phases: analysis and standardization of a B. sphaericus fermented culture; physical, chemical, and biological analysis of the active powder (solubility, residual humidity, particle size, resting angle, flowing off time, compacted density, and biological activity against Culex quinquefasciatus larvae); and the development of fast-disintegrating tablets. Five formulations with differing compositions were developed and a UV protector was added to the selected formulation. The formulation products with or without UV protector, as well as the active powder caused 100% larval mortality from 1 day to 2 months after a single treatment under simulated field conditions. These results show that the UV protector does not affect the initial larvicide activity of B. sphaericus, nor its persistence over a period of two months.
Asunto(s)
Bacillus , Culex , Control Biológico de Vectores/métodos , Animales , Larva , Dosificación Letal Mediana , Comprimidos , Factores de TiempoRESUMEN
This study aimed to analyze the final fermentation culture of Bacillus sphaericus 2362, standardize it and develop an active tablet formulation for use in urban mosquito breeding sites. It was performed in three phases: analysis and standardization of a B. sphaericus fermented culture; physical, chemical, and biological analysis of the active powder (solubility, residual humidity, particle size, resting angle, flowing off time, compacted density, and biological activity against Culex quinquefasciatus larvae); and the development of fast-disintegrating tablets. Five formulations with differing compositions were developed and a UV protector was added to the selected formulation. The formulation products with or without UV protector, as well as the active powder caused 100 percent larval mortality from 1 day to 2 months after a single treatment under simulated field conditions. These results show that the UV protector does not affect the initial larvicide activity of B. sphaericus, nor its persistence over a period of two months.
Asunto(s)
Animales , Bacillus , Culex , Control Biológico de Vectores/métodos , Larva , Comprimidos , Factores de TiempoRESUMEN
O Lapachol é uma naftoquinona isolada de várias espécies de plantas da família Bignoniáceas, encontrado facilmente nas regiões norte e nordeste do Brasil. Conhecido por suas propriedades anticancerígenas, possui ainda antiinflamatória, analgésica, antibiótica, antimalária antitripanossoma, e antiulcerogênica. O LAFEPE® em parceria com o Departamento de Antibióticos da Universidade Federal de Pernambuco - UFPE disponibiliza o Lapachol na forma de cápsulas de 250 mg e pretende, com este trabalho, apresentar uma revisão bibliográfica sobre a segurança e eficácia do Lapachol na terapêutica de modo a proporcionar uma maior difusão de conhecimentos na sua prescrição e torná-lo medicamento de referência dentro da política de genéricos do país.