Anti-inflammatory and antinociceptive activities of Phyllanthus niruri spray-dried standardized extract

Phyllanthus niruri L., Euphorbiaceae, spray-dried standardized extract was studied for its anti-inflammatory and antinociceptive activities in adult albino rats and mice. The anti-inflammatory effect of spray-dried standardized extract was observed in carrageenan-induced paw edema and thioglycolate-induced leukocyte migration, while antinociceptive effects were observed using Randall & Selitto, tail flick, and hot plate tests. This study showed that intraperitoneal spray-dried standardized extract at 100, 200, 800, or 1600 mg/kg reduced the vascular response in the inflammatory process of paw edema induced by 1% carrageenan. Oral spray-dried standardized extract at 100 or 200 mg/kg inhibited leukocyte migration to the site of inflammation induced by 3% thioglycolate. In rats, at 100 and 200 mg/kg intraperitoneally, the extract exhibited a marked peripheral analgesic effect in a Randall & Selitto assay and showed significant central analgesic activity in a hot plate and tail flick assay. In conclusion, this study suggested that Phyllanthus niruri spray-dried standardized extract has potent inflammatory and antinociceptive activities and that these activities are not modified by standard drying process, making it feasible to use the dry extract standardized to obtain a phytotherapic preparation and thus validating its use for the treatment of pain and inflammation disorders.

Chemical and technological evaluation of the Phyllanthus niruri aerial parts as a function of cultivation and harvesting conditions

Tea from Phyllanthus niruri L., Phyllanthaceae, aerial parts is commonly used by Brazilian folk medicine for its benefits on the treatment of genitourinary disorders, for what the polyphenolic compounds are mainly responsible. The yield of such compounds may be influenced by several variables related with the plant growth. The effects of planting periods and harvesting conditions are investigated in this work, including four different seasons. The cultivation was characterized by dry mass yield of aerial parts, and the effect of pruning was analyzed. Leaves, stems and their mixtures were analyzed after drying and milling. Loss on drying and water soluble extractives were used as physical parameters for quality control. Flavonoid content and gallic acid were chosen as chemical markers for this work. The spectrophotometric trial based on the aluminum chloride complexes was applied to evaluate the total flavonoids content. Gallic acid contents were measured from the water extractive solutions by high-performance liquid chromatography. The pruning caused a positive influence on the amount of leaves and stems. The highest flavonoids and gallic acid contents were found in the leaves, which were developed over the summer and the winter, respectively, both from the second harvesting (after pruning). Chomatographic profile by HPLC was characterizes by the presence of gallic acid and two other major peaks (not identified substances), which relation was peculiar to each aerial part. In conclusion, these results suggest that even under less favorable climatic conditions, in winter, the pruning seems to cause a strong influence over the P. niruri polyphenolics production. Indeed, the total flavonoids content, as well as the HPLC profile, can be used as indicative parameters of the ratio of leaves and stem in the vegetal raw material.

Achyrocline satureioides (Lam.) DC., Asteraceae: development of granules from spray dried powder

Achyrocline satureioides (Lam.) DC., Asteraceae, is a herbal specie widely used in folk medicine in the south of Brazil, Uruguay, Argentina and Paraguay. The technological characteristics of an Achyrocline satureioides spray dried extract powder, produced in semi-industrial scale, as well as the feasibility of the granules are reported in the present work. The spray dried powder was characterized as a fine powder consisting of small spherical particles with rough and porous surface. The Hausner's factor, Carr's index, and densification index of the spray dried powder were, respectively, 1,23, 18,9 percent, and 27,2 mL, characterizing it as a poor flow and low density powder. The preparation of granules from this spray dried powder, through dry disaggregation method, yielded irregularly shaped granules, with a rough surface, but with better flow and compactability characteristics. These granules presented a Hausner's factor, a Carr's index, and a densification index of, respectively, 1,09, 8,16 percent, and 12,33 mL. The LC assay of the main polyphenols, quercetin, luteolin, and 3-O-methylquercetin revealed that the granulation process did not changed the quantitative and qualitative profile of these constituents originally present in the spray dried powder. The comparative evaluation of the physical stability of both the spray dried powder and the granules, under relative humidity conditions of 65 percent and 99 percent, showed an expressive reduction in the humidity sorption on the granules as compared to the spray dried powders.

Achyrocline satureioides (Lam.) DC., Asteraceae, é uma planta amplamente utilizada na medicina popular no sul do Brasil, Uruguai, Argentina e Paraguai. As características tecnológicas do extrato seco por aspersão de Achyrocline satureioides, produzido em escala semi-industrial, assim como a viabilidade da produção de granulados são relatadas no presente trabalho. O extrato seco por aspersão foi caracterizado como um pó fino, composto por pequenas partículas esféricas com superfície rugosa e porosa. O fator de Hausner, índice de Carr e o índice de densificação das partículas foram, respectivamente, 1,23, 18,9 por cento e 27,2 mL, caracterizando-o como um pó com fluxo pobre e de baixa densidade. A preparação dos granulados a partir deste extrato seco por aspersão, através do método de desagregação por via seca, originou grânulos com forma irregular, superfície rugosa, mas com melhor fluxo e melhores características de compactabilidade. Estes grânulos apresentaram fator de Hausner, índice de Carr e índice de densificação de 1,09, 8,16 por cento e 12,33 mL, respectivamente. A análise por de CLAE dos polifenóis principais quercetina, luteolina e 3-O-metilquercetina revelou que o processo de granulação não altera o perfil quantitativo e qualitativo dos constituintes inicialmente presentes no extrato seco. A avaliação da estabilidade física do extrato seco por aspersão e do granulado, em condições de unidade relativa de 65 e 99 por cento, mostrou uma expressiva redução na absorção de umidade dos grânulos quando comparados com o extrato seco.

Avaliação da redução da carga microbiana de droga vegetal através do processamento tecnológico: decocção e secagem por aspersão / Evaluation of microbial contamination reduction on plants through technological process of decoction and spray dry

As plantas medicinais podem representar importantes alternativas terapêuticas. No entanto, para elaboração de um fitoterápico a contaminação microbiana constitui um problema a ser vencido. O processamento tecnológico da matéria-prima envolve etapas, geralmente, desfavoráveis à sobrevivência de microrganismos, sendo sua eliminação dependente da carga microbiana inicial e das condições de trabalho utilizadas. Assim, este estudo teve como objetivo verificar a contaminação microbiana presente nas partes aéreas de Phyllanthus niruri e produtos derivados, solução extrativa (SE) e produto seco por aspersão (PSA), a fim de avaliar a redução da contaminação após a decocção e a secagem por aspersão. A determinação dos microrganismos viáveis nos produtos foi realizada através do método de contagem em placas, e a quantificação de coliformes totais pela técnica do número mais provável. Os resultados demonstraram que carga microbiana dos produtos analisados encontrava-se abaixo do limite máximo permitido. Em relação à droga vegetal, a solução extrativa apresentou carga microbiana consideravelmente menor, sugerindo que a decocção tenha sido responsável pela redução de 98,3 por cento da contaminação inicial. Por outro lado, a carga microbiana do PSA foi semelhante a da SE, indicando que os microrganismos não são afetados pela operação de secagem por aspersão.

Medicinal plants can be important therapeutic alternative, however microbiological contamination of plants represent a problem to be solved before the production. The technologic process of raw material has many stages, generally, adverse to microbial growth, but its complete elimination depends on the initial and work condition utilized. The aim of this work was to verify the microbial contamination of Phyllanthus niruri aerial parts and derivatives products, such as extractive solution (SE) and spray dried extract (PSA) with the purpose of evaluating the decrease of the contamination after the decoction and the spray dry. The microbiological analysis of the products was performed by total plate count and MPN coliform. The results showed that the contamination of the products was below the limit maxim. The contamination in the SE was significantly lower than in the plant and this fact suggest that the decoction was responsible for a reduction of 98,3 percent of the initial contamination. On the other hand, the PSA contamination was similar the SE thus suggesting that the spray dry did not affect the microorganisms present in the initial product.

From a medicinal plant to a pharmaceutical dosage form. A (still) long way for Brazilian medicinal plants

Phytopharmaceutical drugs play an important role in the Brazilian health system considering both economic and cultural perspectives. Pondering the richness of the Brazilian flora and the wide use of medicinal plants by the population, there should be sufficient knowledge to apply that information as a suitable starting point to transform medicinal plants into adequate industrial pharmaceutical dosage forms. Problems involving lack of organized knowledge and scientific information are not sufficiently solved to accomplish the modern drug concept, which has to consider efficacy, safety and constant quality. On basis of one of the most used medicinal plants in southern Brazil, Achyrocline satureioides, this paper presents and discusses the problems involving the transformation of medicinal plants into phytopharmaceutical drugs, showing some steps carried out by the academic milieu in order to provide answers to solve this question.