ABSTRACT
Justicia pectoralis Jacq., Acanthaceae, is a herb known popularly in Cuba as Tilo and used traditionally as sedative. The development in a solid pharmaceutical (Tablets 100 mg) using dry extract of Justicia pectolaris aqueous extract is of interest for the development of phytomedicines, which uses this active raw material. The aim of the present study was to carry out chemical and biological stability studies to the formulation. A method of coumarin determination by High Performance Liquid Chromatography (HPLC) was used and validated. The stability studies during different periods of time (24 months) showed a stability of the product stored at 32 ± 2 °C, and protected of the light.
Justicia pectoralis Jacq., Acanthaceae é uma erva conhecida popularmente em Cuba como Tilo e utilizada tradicionalmente como sedativo. O desenvolvimento de formas farmacêuticas sólidas (comprimido 100 mg) usando extrato aquoso seco de J. pectoralis é de interesse no desenvolvimento de fitoterápicos que empreguem esse princípio ativo. O objetivo do presente estudo foi realizar estudos de estabilidade químicos e biológicos da formulação. Um método de determinação de cumarinas por Cromatografia Líquida de Alta Eficiência (CLAE) foi usado e devidamente validado. Os estudos de estabilidade durante diferentes períodos de tempo (24 meses) mostraram a estabilidade do produto preservado a 32 ± 2 °C e protegido da luz.
Subject(s)
Tablets/pharmacokinetics , Acanthaceae/classification , Pharmacognosy/methods , Coumarins/analysis , Phytotherapeutic DrugsABSTRACT
INTRODUCTION: Justicia pectoralis Jacq. (Acanthaceae) is medicinal plant species commonly used in Cuba for the treatment of nervous disorders because of its sedative effect. Coumarin is one of its main active phytochemicals present in the extracts obtained from this plant and used as analytic marker in quality control. On the other hand, this compound contributes to the sedative effect attributed to this plant. OBJECTIVE: to evaluate the influence of harvest time on the coumarin and umbelliferone (7-hydroxycoumarin) in Justicia pectoralis extracts. METHODS: the experiment lasted two years. The harvest was performed at 4, 6 and 8 months after planting. Aqueous and hydroalcohol extracts were produced and the coumarin and umbelliferone contents were determined by high resolution liquid chromatography. RESULTS: the achieved results showed the presence of coumarin and umbelliferone in both extracts. Both methods can be used for the extraction of these components from the plant, although in the case of umbelliferone, the best extraction results were achieved by using aqueous extract. In both cases, the recovery percentages were more than 98 percent. This study confirmed that the harvest time significantly influences on the coumarin and umbelliferone contents. CONCLUSIONS: the best results are observed in the first two harvests (4 and 6 months at summer time), which indicates that the industry should process the vegetal material in these two periods of the year(AU)
INTRODUCCIÓN: Justicia pectoralis Jacq. (Acanthaceae) es una planta medicinal comúnmente usada en Cuba para el tratamiento de enfermedades nerviosas por su efecto sedante. La cumarina es uno de los fitocomponentes mayoritarios en los extractos obtenidos con esta planta y empleado como marcador analítico en los controles de calidad. Por otro lado, este componente contribuye con el efecto sedante atribuido a esta planta. OBJETIVO: evaluar la influencia del tiempo de cosecha sobre el contenido de cumarina y umbelliferona (7 hidroxicumarina) en extractos de Justicia pectoralis. MÉTODOS: se desarrolló el experimento durante 2 años. Se realizaron las cosechas a los 4, 6 y 8 meses de plantada. Se elaboraron extractos acuosos e hidroalcohólicos y se determinó el contenido de cumarina y umbelliferone por cromatografía líquida de alta resolución. RESULTADOS: se mostró la presencia de cumarina y umbelliferona en ambos extractos. Además, en el caso de la umbelliferona, los mejores resultados se alcanzaron al aplicar extracción acuosa. En ambos casos, los por cientos de recobrados fueron superiores al 98 por ciento. Se confirmó que el tiempo de cosecha influyó significativamente sobre el contenido de cumarina y umbelliferona. CONCLUSIONES: los mejores resultados se obtienen en la primeras dos cosechas (4 y 6 meses que coincide con el verano), lo que sugiere que el material de la planta debe procesarse por la industria en esos periodos del año(AU)
Subject(s)
Umbelliferones/pharmacology , Coumarins/pharmacology , Cuba , TiliaABSTRACT
Introducción: Justicia pectoralis Jacq. (Acanthaceae) es una especie medicinal nativa de la América tropical. En Cuba es usada en la medicina tradicional en el tratamiento de afecciones nerviosas. La industria farmacéutica cubana trabaja en el desarrollo de procesos tecnológicos para la obtención de materias primas de calidad farmacéutica a partir de productos naturales. Objetivo: desarrollar un proceso tecnológico para la obtención de extractos secos a partir de extractos acuosos de Justicia pectoralis. Métodos: se desarrolló un proceso para la obtención de extracto seco por spray drying a partir de extracto acuoso de Justicia pectoralis. La influencia que sobre el contenido de cumarina tenían la relación sólido-líquido y el tiempo de extracción fue estudiada aplicando un diseño superficie respuesta. Se estudió el proceso de secado y la posterior evaluación farmacológica del polvo seco. Resultados: estos mostraron que la relación sólido-líquido tenía una fuerte influencia estadísticamente significativa sobre la extracción de la cumarina en las condiciones de trabajo experimentadas. El tiempo de extracción y la interacción entre ambos factores no fueron significativos para el modelo de regresión estudiado. Por otro lado, la evaluación de la influencia de aditivos inertes en el proceso de secado mostró que los mejores rendimientos se alcanzaban cuando se empleaba almidón soluble 30 por ciento, y no se afectaba la actividad sedante del producto. Conclusiones: una relación sólido-líquido de 1:20 y un tiempo de extracción de 15 min resultaron las condiciones óptimas para la extracción de cumarina
Introduction: Justicia pectoralis Jacq. (Acanthaceae), is a medicinal species native to the American tropics. In Cuba it is used in folk medicine in the treatment of nervous disorders. The Cuban Pharmaceutical Industry is working on the development of technological processes for the obtention of pharmaceutical quality raw materials from natural products.Objectives: develop a technological process to obtain dry extract from aqueous extracts of J. pectoralis.Methods: a process to obtain dry extract by spray drying from aqueous extract of J. pectoralis was developed. The influence of solid-liquid r ratio and extraction time on coumarin content was evaluated by applying a response surface methodology (RSM). The drying process and later pharmacological evaluation of the dry powder were studied. Results: results show that solid-liquid ratio was the statistically significant main effect, having a strong positive influence on coumarin extraction in our working conditions. Extraction time and interaction between both factors were not significant for regression models. On the other hand, evaluation of the influence of inert additives on drying s showed that the best results were obtained with the use of 30 percent soluble starch, which did not affect sedative activity. Conclusions: a solid-liquid ratio of 1:20 and an extraction time of 15 minutes were suggested as optimum parameters for coumarin extraction
Subject(s)
Coumarins , Drug Evaluation , Plant Extracts , Tranquilizing AgentsABSTRACT
Introducción: el ensayo de disolución es una técnica analítica de empleo común en un laboratorio farmacéutico. Un proceso tecnológico para la elaboración de tabletas fue desarrollado. El ingrediente farmacéutico activo usado fue Tilo ® extracto seco. Objetivo: el objetivo de este trabajo fue desarrollar y validar un ensayo de disolución para evaluar la estabilidad y la calidad de dicho producto. Método: se utilizaron muestras de un lote experimental, un lote placebo y lotes pilotos de tabletas de Tilo ® de 100 mg. Se evaluaron como medios de disolución agua destilada y solución de ácido clorhídrico 0,1 mol/L, realizándose perfiles de disolución a 50, 75 y 100 rpm, empleándose los dos tipos de aparatos establecidos en la literatura para este ensayo (cesta y paleta). El contenido de cumarina fue analizado por HPLC. El ensayo fue validado según la USP. Resultados: los resultados mostraron que el agua destilada fue un medio de disolución adecuado, alcanzándose porcientos de disolución de la droga por encima del 85 por ciento a los 30 minutos, no existiendo diferencias significativas entre los tipos de aparatos recomendados por la USP. Mientras que, los perfiles de disolución a diferentes tiempos y velocidades de agitación mostraron una liberación gradual del principio activo en el tiempo, donde a medida que se incrementa la velocidad de agitación, se incrementa el porcentaje de disolución de la droga en el medio. La validación del ensayo demostró que el mismo era específico y preciso. Conclusiones: se estableció como ensayo de disolución las siguientes condiciones de trabajo: Aparato: paleta, 100 rpm; medio: agua destilada, 500 mL; tiempo: 60 minutos y Temperatura: 37 ± 0,5 ºC
Introduction: dissolution testing is one of the most common analytical techniques performed in a pharmaceutical analytical laboratory. A technological process for the production of tablets was developed. The active pharmaceutical ingredient used was Tilo ® dry extract. Objective: to develop and to validate the dissolution assay aimed at evaluating the stability study and the quality of this product. Methods: some samples from the experimental batch, the placebo batch and the pilot batches were used in this study. Distilled water and 0,1 mol/L chlorhidric acid were evaluated as dissolution media. The dissolution profiles at 50, 75 and 100 rpm and two types of dissolution devices (basket and paddle) recommended for the USP were evaluated. Coumarin content was analyzed by HPLC method. The dissolution assay was validated according to the United States Pharmacopeia. Results: the results showed that the distilled water was an appropriate dissolution medium, where percentages of released drug higher to 85 percent in 30 minutes were obtained; there were no significant differences among the types of dissolution devices recommended by the USP. The dissolution profiles at different shaking times and speeds showed gradual release of the active principle. As the shaking speed increases, the percentage of the drug dissolution increases in the medium. The assay was considered specific and precise. Conclusions: a type II (paddle) dissolution device, 500 ml of distilled water at 37 ± 0,5 ºC and 100 rpm, were established as parameters of the dissolution assay
Subject(s)
Dissolution , Drug Evaluation , Tilia , Laboratory and Fieldwork Analytical MethodsABSTRACT
Este trabalho teve por objetivo avaliar a resposta a dinamizações do isoterápico Justicia no crescimento e na produção de cumarina em Justicia pectoralis. O experimento foi conduzido na Universidade Federal de Viçosa. O delineamento estatístico foi inteiramente casualizado, com quatro repetições e seis tratamentos, totalizando 24 parcelas experimentais, sendo cada parcela constituída de uma planta por vaso. Os tratamentos foram constituídos das dinamizações 3CH, 6CH, 12CH, 18CH, 24CH e 30CH, do isoterápico Justicia. A aplicação dos tratamentos iniciou após o plantio das mudas, sendo pulverizada a parte aérea, em intervalos semanais. Após quatro meses do plantio as plantas foram colhidas. Foram avaliadas a matéria fresca e seca das folhas e caules a matéria fresca e seca da inflorescência, e a matéria fresca e seca total. Foram pesadas amostras de 200 mg das folhas e caules das plantas secas. As amostras foram devidamente armazenadas até a realização das análises químicas. A quantificação da cumarina (1-2 benzopirona) nas amostras foi feita em Cromatógrafo Líquido de Alta Eficiência. A matéria fresca de folhas e caules, a matéria fresca total e o rendimento de cumarina variaram em função das dinamizações do isoterápico. Os resultados confirmam o efeito de preparações homeopáticas na planta demonstrando que a homeopatia nos vegetais, mesmo na Lei da Igualdade tem efeitos potenciais.
The studied aimed to evaluate the responses to dynamizations of Justicia isoterapic in growth and coumarin production in Justicia pectoralis. The studies were carried out at the Universidade Federal de Viçosa. The statistical design was completely randomized, with four replicates and six treatments, 24 experimental plots, one plant per pot. The treatment were dynamizations 3CH, 6CH, 12CH, 18CH, 24CH and 30CH Justicia isoterapic. The applications of the treatments begun are planting seedlings, the aerial part being sprayed, at weekly intervals. After four months of planting, the plants were harvested. Were evaluated fresh and dry matter of stem and leaves, fresh and dry matter of inflorecense, and fresh and dry matter total. Were weighed samples on 200 mg of leaves and stems of dried plants. The samples were properly stored at quimical analyses. The quantification of coumarin (1-2 benzopyrone) in the samples was done in High Resolution Liquid Chromatography. The fresh matter of leaves and stems, the fresh matter total and a production of coumarin varied as a function of dynamization of isoterapic. The results confirm the effect of homeopathics preparations in the plants demonstrating that homeopathy in vegetables even in the Equality Law has potential effect.
Subject(s)
Dynamization , Coumarins , Social Justice/physiology , Homeopathy/trendsABSTRACT
Este estudo objetivou avaliar a resposta do crescimento e do metabolismo secundário de Justicia pectoralis, expresso em produção de cumarina, a crescentes dinamizações de A. montana. O experimento foi conduzido na Universidade Federal de Viçosa. O delineamento estatístico foi inteiramente casualizado, com seis repetições e cinco tratamentos, totalizando 30 parcelas experimentais, sendo cada parcela constituída de uma planta por vaso. Os tratamentos foram as dinamizações 3CH, 30CH, 60CH, 100CH e 200CH do preparado homeopático A. montana. Os tratamentos foram aplicados às plantas via pulverização, em intervalos semanais, iniciando logo após o plantio. Após quatro meses do plantio as plantas foram colhidas. As características de crescimento avaliadas foram matérias fresca e seca de folhas e caules, matérias fresca e seca de inflorescências e matérias fresca e seca total. No estudo fitoquímico foi avaliada a produção da cumarina (1-2 benzopirona). Não houve resposta nas variáveis de crescimento aos tratamentos. As dinamizações de A. montana causaram alterações no metabolismo secundário das plantas. Os conteúdos de cumarina das plantas com A. montana 3CH e 30CH foram próximos e mais baixos, aumentando progressivamente a partir de 60CH, chegando ao máximo em 100CH, seguido de redução em 200CH. A preparação homeopática A. montana causa alterações no metabolismo secundário de chambá, sendo as repostas dependentes da dinamização.
Were evaluated the responses to dynamizations of Arnica montana in the growth and in the secondary metabolism of Justicia pectoralis expressed as coumarin production. The studies were carried out at the Universidade Federal de Viçosa. The statistical design was completely randomized, with six replicates and five treatments, 30 experimental plots, one plant per pot. The treatments were dynamizations 3CH, 30CH, 60CH, 100CH and 200CH homeopathic preparation of A. montana. The application the treatments begun are planting seedlings, the aerial part being sprayed, at weekly intervals. After four months of planting, the plants were harvested. The evaluated growth characteristics were: fresh and dry matter of leaves and stems, fresh and dry matter of inflorecenses, and fresh and dry matter total. In the phytochemistry study, the production of the coumarin 1,2-benzopyrone was evaluated. Were no responses of growth characteristics. The dynamizations of A. montana caused changes in secondary metabolism of plants. The coumarin production with A. montana plants 3CH and 30CH were lower, increasing progressively from 60CH, and coming to increased in 100CH, followed by a large reduction in the 200CH. The homeopathic preparation A. montana cause change in secondary metabolism of chambá, and the responses depend on dynamizations.
Subject(s)
Social Justice/metabolism , Secondary Metabolism/physiology , Arnica/growth & development , Coumarins/adverse effects , HomeopathyABSTRACT
Introducción: el empleo de las materias primas de origen natural, como ingrediente farmacéutico activo, se difunde cada vez más en la industria farmacéutica para la elaboración de medicamentos. Justicia pectoralis Jacq (Acantaceae) es una planta herbácea que se emplea como sedante tradicionalmente por la población cubana, conocida como tilo. Objetivo: desarrollar un medicamento, en forma de jarabe, que contenga como sustancia activa el extracto seco de J pectoralis 0,6 por ciento m/v. Métodos: se efectuó el estudio de formulación, microbiológico y de estabilidad químico-física, almacenado a temperatura ambiente en frascos de vidrio ámbar por 125 mL. Resultados: se obtuvo un jarabe con adecuadas características organolépticas, estable desde el punto de vista microbiológico, físico y químico, durante 36 meses en las condiciones estudiadas. Conclusiones: el medicamento desarrollado fue correctamente formulado desde el punto de vista galénico y cumple con los requisitos de calidad establecidos para este tipo de forma farmacéutica
Introduction: the use of natural raw materials as active ingredient is increasingly spreading in the drug industry for the manufacture of pharmaceuticals. Justicia pectoralis Jacq(Acantaceae) is a herbaceous plant traditionally used as sedative by the Cuban population which knows it as lime tea. Objective: to develop syrup containing the dry extract from J. pectoralis 0,6 percent m/v as active principle. Methods: the formulation, microbiological and chemical/physical stability studies were performed on the product stored at room temperature in 125 mL amber-coloured glass containers. Results: the syrup had adequate organoleptic characteristics and was stable from the microbiological, physical and chemical viewpoints for 36 months under the studied conditions. Conclusions: this pharmaceutical was properly formulated from the galenic viewpoint and met all the set quality requirements for this type of pharmaceutical form
Subject(s)
Hypnotics and Sedatives , Phytotherapeutic Drugs , Plants, MedicinalABSTRACT
In this paper, the influence of the altitude in the phenols and flavonoids contents and the antioxidant activity of the extracts of different polarities of Justicia pectoralis Jacq(Acanthaceae) was evaluated. There was found that the plants cultivated under the Ibagué-Tolima's climate and soil conditions, can be a source of antioxidant compounds, especially in water preparations. The chromatographic analysis revealed that J. pectoralis extracts have mainly flavonoids of the flavonone type, as apigenine. A greater (or The greatest) content of flavonoids was detected in the ethanolic extract of the plant samples grown at 1 265 m.a.s.l. (meters above sea level) (2 748,03 mg/L). The altitude level does not seem to have any influence on the functional properties, neither on the phytophenols content. The J. pectoralis Jacq can be considered one species with a high therapeutic potential and with good commercial opportunities.
En este trabajo se evaluó la influencia de la altitud en el contenido de fenoles y flavonoides y la actividad antioxidante de los extractos de diferentes polaridades provenientes de Justicia pectorales (Acanthaceae). Se halló que las plantas cultivadas en las condiciones del suelo y el clima de la zona Ibagué-Tolima pueden constituirse en compuestos antioxidantes, especialmente en preparados acuosos. El análisis cromatográfico reveló que los extractos de J. pectorales poseen en lo fundamental flavonoides del tipo flavona como es la apigenina. Un mayor contenido (sino el mayor) de flavonoides se detectó en el extracto etanol obtenido de las muestras de la planta cultivadas a 1 265 metros por encima del nivel del mar (2 748,03 mg/L). La altitud no parece influir en las propiedades funcionales, ni en el contenido de fitofenoles del extracto. La J. pectorales puede considerarse una especie de gran potencial terapéutico y buenas posibilidades de comercialización.
ABSTRACT
Justicia pectoralis Jacq., Acanthaceae, é uma erva conhecida popularmente no Nordeste como chambá e, utilizada tradicionalmente no tratamento de doenças do trato respiratório, como a asma, tosse e bronquite. Essa espécie encontra-se na Relação Nacional de Plantas Medicinais de Interesse para o SUS. O objetivo do presente estudo foi elaborar protocolo para a preparação da droga vegetal a partir de J. pectoralis e realizar a sua caracterização visando seu emprego como matéria-prima farmacêutica. A parte aérea de J. pectoralis, após secagem em estufa com circulação e renovação de ar (35 °C) durante diferentes períodos de tempo (1-5 dias) mostrou a partir de 24 h de secagem um teor de umidade abaixo do valor máximo permitido para drogas vegetais. O pó da droga vegetal foi classificado como pó moderadamente grosso e, caracterizado quanto aos teores de cinzas totais, extrativos solúveis em água e etanol. Análise do extrato hidroalcoólico (etanol 20 por cento) de J. pectoralis por Cromatografia Líquida de Alta Eficiência (CLAE-DAD) determinou um teor de cumarina e umbeliferona de 16,2 e 0,81 mg/g da droga vegetal, respectivamente. As condições de preparação da droga vegetal e os parâmetros de controle de qualidade determinados para J. pectoralis no presente estudo são de interesse no desenvolvimento de fitoterápicos que empreguem esse matéria-prima ativa.
Justicia pectoralis Jacq., Acanthaceae, is a herb popularly known in Brazilian northeast as "chambá" and used in folk medicine for the treatment of respiratory tract conditions such as asthma, cough and bronchitis. This species is included in the National Register of Plants of Interest to the National Health System. The aim of the present study was to develop a protocol for the preparation of the plant drug from J. pectoralis and to characterise the plant drug for its use as a pharmaceutical raw material. The aerial parts of J. pectoralis, after drying chamber with forced air circulation (35 °C) for different periods of time (1-5 days), presented after one day a moisture content below the maximum allowed for plant drugs. The powder of the plant drug was classified as moderately coarse, and the total ashes content and the water- or ethanol-soluble extractives were determined. Analysis of hydroalcoholic (ethanol 20 percent) extract of J. pectoralis by high performance liquid chromatography-photo diode array (HPLC-PDA) determined the content of coumarin and umbelliferone (16.2 and 0.81 mg/g plant drug, respectively). The preparation conditions of the plant drug and the quality control parameters established for J. pectoralis in this study are of interest for the development of phytomedicines which use this active raw material.
ABSTRACT
Fundamentos: Justicia pectoralis Jacq., especie de la familia Acantaceae, es una planta herbácea que se emplea como sedante tradicionalmente por la población cubana. Objetivos: desarrollar y validar un método de análisis por cromatografía líquida de alta resolución para la determinación de cumarina en el extracto seco obtenido a partir de extractos de J. pectoralis. Métodos: se desarrolla y valida un método de análisis por cromatografía líquida de alta resolución para la determinación de cumarina. Resultados: el método desarrollado es específico, preciso, exacto y lineal. Conclusiones: el método puede ser empleado para cuantificar cumarina, en muestras de polvo seco obtenidas mediante secado por aspersión a partir de extractos de J. pectoralis.
Rationale: Justicia pectoralis Jacq., an Acantaceae family species, is an herbaceous plant that is used as a traditional sedative by the Cuban population. Objectives: to develop and to validate a high performance liquid chromatography to determine coumarin in dry extract from J. pectoralis extracts. Methods: A high performance liquid chromatography method to determine coumarin was developed and validated. Results: The method was specific, accurate, precise and linear. Conclusions: This method may be used to quantify coumarin in dry power samples obtained through spraying drying from J. pectoralis extracts.
Subject(s)
Analytic Sample Preparation Methods , Chromatography, High Pressure Liquid/methods , Quality Control , Tilia/chemistryABSTRACT
Justicia pectoralis and J. gendarussa are species of medicinal interest employed in several countries of Central and South America as analgesics and antiinflamatories. The leaves of J. pectoralis are also utilized by indigenous of the Brazilian Amazon and Venezuela as hallucinogenic snuffs. J. pectoralis and J. gendarussa were morphologically characterized under standardized experimental cultivation and investigated to any evidence of hallucinogenic principle. Two varieties of J. pectoralis, J. pectoralis var. stenophylla Leonard and J. pectoralis var. A. (undetermined), were differentiated by the habit, form and number of leaves; J. gendarussa differs by the habit, form of the leaves and color of the veins. The use of J. pectoralis as hallucinogenic is also discussed.
Justicia pectoralis e J. gendarussa são espécies de interesse medicinal utilizadas popularmente em vários países da América do Sul e Central como analgésicas e antiinflamatórias. As folhas de J. pectoralis também são utilizadas por indígenas da Amazônia brasileira e da Venezuela em rapés alucinógenos. J. pectoralis e J. gendarussa foram caracterizadas morfologicamente sob condições padronizadas de cultivo e investigadas quanto a presença de algum princípio alucinógeno. Duas variedades de J. pectoralis, J. pectoralis var. stenophylla Leonard e J. pectoralis var. A. (indeterminada), foram diferenciadas pelo hábito, forma e número de folhas; J. gendarussa difere destas pelo hábito, forma das folhas e coloração das nervuras. O uso de J. pectoralis como alucinógena também é discutido.