Abstract in English:This review concerns the definitions and appropriate analytical characterisations of herbal reference standards within the framework of regulatory requirements. It describes currently applicable rules and regulations, as well as future issues relating to the European Pharmacopoeia and United States Pharmacopoeia. It provides an update on the use and availability of pharmacopoeial (EP and USP) herbal reference standards since our last review was published in 2009. The continuing challenges facing manufacturers, suppliers and analysts are discussed on the basis of exemplary reference substances for herbal products in medicinal and food products. The article also reviews the special aspects of Brazilian stipulations (Brazilian Pharmacopoeia, Anvisa) by comparison with European regulations. The term herbal products as used throughout this article refers to herbal drugs, herbal preparations and finished herbal medicinal products unless a different meaning is obvious from the context. More specific terms are used where necessary.
Abstract in English:This article shows the evolution of the Brazilian legislation in recent years in the area of herbal products and discusses the concept of phytotherapy in Brazil, bringing information about how it works in Europe.
Abstract in English:The total flavonoid content (TFC), total polyphenols content (TPC), and in vitro antioxidant activity (AA) of six Bidens pilosa L., Asteraceae, populations harvested from different localities were evaluated in this work. The plants were separated in roots, stems, and leaves/flowers, and the influence of extraction methods was investigated.Areversed-phase high-performance liquid chromatography method (HPLC) was developed and employed to obtain characteristic HPLC fingerprints of the bioactive compounds present in the extractive solutions, which were correlated with the TFC, TPC, and AA. Extractive solutions of leaves/flowers presented a higher AA when compared with those obtained from other parts of the plant (IC50 of 35.35±0.10 µg/mL). The stem extracts presented the lowest AA (IC50 117.2±1.96 µg/mL). A direct correlation of AA with TFC and TPC was evidenced. The highest AA was obtained by dynamic maceration and was statistically different from the AA presented by the extractive solutions obtained by other extraction methods. The results of this work evidenced differences that can be found at different stages of development of phytopharmaceutical preparations from B. pilosa and highlighted the importance of using the concentration of marker compounds as well as HPLC fingerprints as quality control parameters.
Abstract in English: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.
Abstract in English:In the present work we carried out a comparative study of total phenolic contents and antioxidant capacity of aqueous leaf extracts of Ugni molinae Turcz., Myrtaceae (infusion and Soxhlet extracted) prepared from continent and Juan Fernández Island samples. The results revealed that total phenol content (TPC), tannins (TTC) and flavonoids (TFC) for U. molinae extracts (infusion and Soxhlet extracts) from island leaves were 38.5, 56.7 and 37.5% higher than those obtained with leaves from the continent, respectively. Also, HPLC profiles showed important differences between U. molinae populations. In vitro antioxidant capacity (scavenging of DPPH radical) for 1% infusion and aqueous extract (Soxhlet method) of U. molinae from island samples, was 15% greater than from continent samples. Further, in vivo impact of U. molinae intake (1% infusion) was studied in plasma samples obtained from healthy volunteers. Participants that consumed tea prepared with leaves from island population showed higher TBARS reduction and plasma antioxidant capacity (TEAC-CUPRAC) than those who consumed tea prepared with leaves from continental population. The conditions of the territory in which U. molinae populations growth could explain the differences in their composition and activity. According to results, island U. molinae populations could be an important source of study for the development of an antioxidant supplement, and thereby contribute to the use of this species that has becoming an ecological problem in the island.
Abstract in English:Spectrophotometric determinations (direct dilution or after acid hydrolysis) of flavonoid content in leaves of Bauhinia forficata Link, Fabaceae, from two different regions from Brazil were compared with contents of kaempferitrin quantified by HPLC analysis. The absence of kaempferitrin peak in one sample denotes the risk of LC-method failure. On the other hand, the both spectrophotometric assays showed satisfactory performance and do not underwent influence from absence of kaempferitrin. Since several flavonoids are present in the herbal material, different content of flavonoids were observed for each analytical procedure. However, a strong positive association could be detected among methods (R²>0.99). Although a conversion factor should be adopted to compare procedures, the data showed that the spectrophotometric methods remain as an important tool for analysis of complex matrices such herbal drugs, notably when there aren't any pharmacological or chemical marker established for the species. Moreover, it's possible to suggest that the techniques studied in this work exhibit similar performance under the conditions employed. Nevertheless, before the adoption of kaempferitrin as an analytical marker by HPLC for Bauhinia species, the pharmacological knowledge should be better developed. In this cases, the use of spectrophotometric assay provide higher assurance of the reproducibility of the efficacy and safety.
Abstract in English:A method for separation and quantification of three flavonoids by reverse-phase high performance liquid chromatography (HPLC) was developed and validated. Flavonoids present in a crude methanolic extract of the inner bark of Dimorphandra gardneriana Tul., Fabaceae, were analyzed. Rutin, isoquercitrin and quercetin were used as calibration standards. The analysis was performed using a Thermo Scientific Hypersil C18 column (250 x 4.0 mm i.d., 5 μm particle size), as stationary phase, with a flow rate of 0.8 mL/min and detection at a wavelength of 356 nm. The proposed method was validated by resolution RE No. 899/2003 of the National Health Surveillance Agency. In this study, an excellent linearity was obtained with r higher than 0.99. Besides, the chromatographic peaks showed good resolution. With other validation data, including precision, specificity, accuracy and robustness, this method demonstrated good reliability and sensitivity, and can be conveniently used for the quantification of rutin, isoquercitrin and quercetin in crude methanolic extract of D. gardneriana pods. Furthermore, there are the advantages of easy sample preparation and short time between each injection.
Abstract in English:Brazil has one of the world's largest biodiversity in flora and a plant that has attracted attention is the Endopleura uchi (Huber) Cuatrec., Humiriaceae, which is native of the Brazilian Amazon. Among the many popular uses, this species is utilized in the treatment of woman's genito urinary tract affections and also as anti-inflammatory. It is believed that their actions derive from the major constituent, bergenin. The objective of this work was to study the Endopleura uchi barks extraction using the dynamic maceration method and the effects of the extraction time, drug to solvent ratio and temperature. A Box-Behnken design was applied to study the influence of these factors and the respective response surfaces. The extract characterization was made by determination of its antioxidant activity by DPPH; total polyphenol content and bergenin content. In general, the extracts showed good antioxidant activity, with the IC50 ranging from 4.02 to 5.87 µg/mL. The polyphenol content ranged from 31.89 to 47.82%. High levels of chemical markers are observed in all extracts, with average bergenin content of 35.58%. The result showed that the multivariate study of extraction is key step in the development and standardization of extracts Endopleura uchi.
Abstract in English:Ipomoea pes-caprae (L.) R. Br., Convolvulaceae, is a medicinal plant that grows abundantly as a pan-tropical stand plant. The 3² (two factors and three levels) factorial design, was applied to determine the best time and drug/solvent proportion to maximize the flavonoid content in the hydroethanolic extract by maceration process. The antinociceptive and anti-inflammatory effects were studied at 5-20 mg/kg, i.p., using the writhing test and carrageenan-induced pleurisy models in mice. The optimized extract was able to inhibit more than 50% of abdominal writhing at 20 mg/kg, with 55.88%±2.4 of maximum inhibition. Indomethacin, used as positive control, inhibited 64.86% at 10 mg/kg. In the pleurisy model, the extract produced dose-dependent inhibition of the first phase of inflammation (4 h) in the pleural cavity induced by injection of carrageenan (1%) in mice. It inhibited 50%±0.82 (p<0.01) of exudation induced by carrageenan, and 60.88%±0.14 (p<0.01) of leukocyte migration to the pleural cavity. In conclusion, the results validate the technological conditions of the maceration process to produce an optimized bioactive herb extract for the development of analgesic and anti-inflammatory phytopharmaceuticals using 70 ºGL ethanol, a plant to solvent ratio of 12.5% (w/v), and ten days of maceration.
Abstract in English:The Copaifera langsdorffii Desf., Fabaceae, is a Brazilian native tree, known as copaiba, which oil is commonly used in folk medicine as muscle relaxant, wound healing, antiseptic and anti-inflammatory to respiratory and urinary tracts. Despite of the wide use of the oil of Copaifera species, scientific works related to the study of its leaves are rarely found. In fact, processes for flavonoid extraction from C. langsdorffii leaves have not been studied yet leaving a wide field to be investigated. In this work, the 2(5-2) fractional factorial design was selected in order to study how the factors of a dynamic maceration process influence the responses of total flavonoids, total phenols, quercetrin and afzelin contents, and antioxidant activity in extracts from C. langsdorffii leaves. The results demonstrated that the significant factors studied were the drug load in extractor, the ethanol/water ratio and the stirring speed whereas the temperature and the extraction time were not significant. In conclusion, this study allowed visualizing which factors were considered the most important in copaiba leaves dynamic maceration and their effect in extract antioxidant activity. Furthermore, this technological study gives directions to optimize future extraction experiments from C. langsdorffii.
Abstract in English:Although soybean isoflavones naturally accumulate in their conjugated forms, the beneficial effects on human health of soybean-containing foods have been credited to their aglycone forms. In the present study we analyzed the effects of a chemical agent, sodium nitroprusside (SNP), in eliciting the exudation of non-conjugated isoflavones from intact soybean seeds, embrionary axes and cotyledons. The isoflavones in the exudates were determined by high performance liquid chromatography and mass spectrometry. The effect of the exudates on the emission of nitric oxide (NO) and on the proliferation of breast carcinoma cells (MCF-7) was also evaluated. SNP elicitation increased the production of the aglycone forms dose- and time-dependently. Exudates of embrionary axes and cotyledons stimulated NO emission and showed biphasic effects on viability of MCF-7 cells. At lower concentrations both extracts presented proliferative effects (10-25%), and at higher concentrations inhibited (15%) cell proliferation. The biphasic effect might be due to the action of isoflavone aglycones in activating estrogen receptors which in turn stimulate the production of NO. Overall, the results suggest that soybean extracts enriched in isoflavone aglycones by elicitation with SNP could be exploited as a functional ingredient in the food industry.
Abstract in English:The aim of this work was to study the effect of dynamic maceration factors upon the curcumin content of Curcuma longa L., Zingiberaceae, extracts and to determine the optimum set of parameters for the extraction of curcumin using a 2(5) full factorial design and the response surface methodology. Under the established conditions, the content of soluble solids and curcumin in the extracts ranged from 0.8 to 3.4%, and from 0.1 to 1.8%, respectively. The most inï¬‚uential variable observed for the extraction was the ethanolic strength of the solvent. The optimized condition involves an extraction time of 12 h, agitation speed of 30 rpm, drug to solvent ratio of 1/6, extraction temperature of 80 ºC and the solvent with ethanolic strength of 70%. The data reported herein are useful for further developments of curcuma phytopharmaceutical intermediate products with optimized characteristics.
Abstract in English:Some species of plants are notable for the wide range of biologically active constituents in their tissues. Chemical and pharmacological studies of Vellozia squamata Pohl, Velloziaceae, popularly known in Brasil as "canela-de-ema" are scarce, but showed the presence of di-and triterpenoid that may be of scientific interest. In the present study the hydroalcoholic extracts from leafs and stems of V. squamata were submitted to phytochemical prospection to identify the principal groups of constituents, and the antioxidant activity was determined by DPPH method. The hydroethanolic extracts presented higher antioxidant activity. Thus, nanoemulsion formulations were prepared using the method of phase inversion. Accelerated stability tests, such as heat stress and centrifugation were made, and physical and chemical properties of the nanoemulsions were established. Stable formulations were obtained from both extracts from leafs and stems. By the results was possible to establish the potential application of hydroalcoholic extracts from V. squamata in development of products with antioxidant properties and demonstrate a promising pharmaceutical product.
Abstract in English:Essential oils are used primarily as natural preservatives, flavourants and fragrances in cosmetic products. Several pharmacopeias possess monographs of plants which are good sources of essential oils, such as Brazilian Pharmacopeia, including Illicium verum Hook. f., Schisandraceae and Rosmarinus offi cinalis. Since determination of Hydrophile-Lipophile Balance (HLB) value of essential oils appears as a critical step for development of emulsions and other semi-solid formulations, evaluation of required HLB values for I. verum and R. offi cinalis essential oils is the aim of this study. They were obtained by hydrodistillation and several emulsions were prepared by changing emulsifiers. The couple sorbitan oleate/polysorbate 20 provided best emulsions and was used at different ratios, at a total blend concentration of 5% w/w. The lowest mean droplet diameters for R. offi cinalis and I. verum emulsions were obtained at HLB 16.5 (97.12 nm) and 16.7 (246.6 nm), respectively. Moreover, emulsions with R. offi cinalis were finer and presented some bluish reflection, characteristic of nanoemulsions. The lowest turbidity value for R. offi cinalis emulsion was also obtained at HLB 16.5 (0.33). Thus, the present study describes for the first time HLB values for R. offi cinalis (16.5) and I. verum (16.7) essential oils, contributing to their physicochemical characterization and technology development of phytopharmaceuticals.
Abstract in English:A 2³ full factorial design was used to assess the impact of spraying air flow rate (30-50 L/min), drying air inlet temperature (90-150 ºC) and extract feed rate (4-6 g/min) on the quality of Eugenia dysenterica DC., Myrtaceae, spray-dried extracts. Response surface methodology (RSM) was applied to analyze the significance of the effects of process factors on product quality and to obtain fitted equations to predict dry powder properties. Powder yields were satisfactory, ranging from 34.64 to 63.92%. The dried products showed moisture contents and water activities below 5% and 0.5, respectively. The recuperation ratios of total polyphenols, tannins and flavonoids ranged from 88.66 to 99.07%, 70.38 to 81.87% and 74.51 to 98.68%, respectively. Additionally, in some conditions the parameters related to dry product’s flowability and compressibility varied over a range acceptable for pharmaceutical purposes. RSM proved that studied factors significantly affected most of the quality indicators at different levels. The spray drying technology is an attractive and promising alternative for the development of intermediate phytopharmaceutical products of E. dysenterica.
Abstract in English:The anti-inflammatory and antiallodynic effects of spray dried powders starting from leaves, stems, roots, the mixture of leaves and stems, as well as the whole plant aqueous solutions of Phyllanthus niruri L., Phyllanthaceae, were assessed. Gallic acid, used as chemical marker, was quantified by HPLC in the spray dried powders. Carrageenan-induced inflammatory and allodynic responses in the mouse paw were used as pharmacological models. Quantitative and qualitative differences among chemical composition of different herb parts were observed. The oral administration of leaves or leaves plus stems spray dried powders (100 mg/kg) significantly inhibited the carrageenan-induced allodynic effect (42±5 and 54±3%, respectively). Additionally, the spray dried powders of leaves significantly reduced carrageenan-induced paw oedema (35±6%). The spray dried powders of roots, stems, or the mixture of leaves, stems and roots (100 mg/kg, p.o.) did not exhibit antiallodynic or antioedematogenic effect in the same model. In conclusion, differences in the chemical composition of spray dried powders from P. niruri are reflected in their in vivo pharmacological actions. Despite of a direct relationship of anti-inflammatory and antiallodynic effects with the gallic acid content had been observed, especially in the spray dried powders of leaves, the use of spray dried powders of leaves plus stems showed to be more effective, suggesting a synergic effect between their constituents.
Abstract in English:The aim of the work was to study the spray-drying of ethanolic extract from Amburana cearensis (Allemão) A.C. Sm., Fabaceae, in order to obtain powders with better pharmacological and technological properties for herbal medicine. A 2³ fractional factorial statistical design was used to find adequate spray-drying operating conditions (inlet air temperature; feed flow rate and air flow rate) to produce A. cearensis powder with adequate concentration of active principles (amburoside and coumarin), low moisture content and high process yield. The HPLC analyses showed that the spray-drying powder of A. cearensis production did not cause alterations in the chromatographic profile when related to the fluid extract. The most significant factor that affected the amburoside concentration was air flow rate, while the concentration of coumarin, a thermolabile molecule, was influenced mainly by inlet air temperature. The moisture content of the spray-drying powder of A. cearensis varied from 3.72 to 5.85% (w/w), while the maximal process yield was 41.1% (w/w). The present study demonstrates for the first time the best operating conditions to produce A. cearensis extract powder that were adequate when related to the coumarin and amburoside concentrations and moisture content. However, additional studies are still needed to improve mainly it technological characteristics.
Abstract in English: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.
Abstract in English:Aqueous extract from seeds of Syzygium cumini (L.) Skeels, Myrtaceae, obtained by dynamic maceration was spray-dried and characterized by its physico-chemical and antihyperglycaemic action. The extract showed to possess high amount of polyphenols, significant in vitro free radical scavenger activity using the DPPH method and an antihyperglycaemic effect in alloxan-induced experimental diabetes. S. cumini spray-dried extracts were obtained using silicon dioxide and cassava starch as adjuvants. The powders showed acceptable flowability, compactability, and low hygroscopicity at 43% relative humidity. Besides, the spray-dried extracts showed in vivo antihyperglycaemic and in vitro scavenger activity comparable to the lyophilized extract. Thus, experimental data indicates that the extract from S. cumini has a relevant activity and that spray-drying could be adequately used to perform the technological processing of S. cumini fluid extracts.
Abstract in English:The most studied phyto constituent isolated from Virola surinamensis (Rol. ex Rottb.) Warb., Myristicaceae, is the tetrahydrofuran neolignan grandisin, which exhibits a series of biological activities, including trypanocidal, larvicidal and antitumoral. Due to its extremely low solubility, additional studies, including in vivo investigations are challenged by the difficulties in the development of an effective drug delivery system for grandisin. The encapsulation in polymeric nanoparticles is a very attractive alternative for overcoming some of these limitations. In this work, PLGA nanocapsules loaded with grandisin were developed in an attempt to optimize the efficacy of grandisin as an antitumoral drug, with high drug loading and efficiency, prolonged drug release and increased physical-chemical stability. Mean diameter of the nanocapsules was lower than 200 nm, with very low polydispersity. Encapsulation efficiency was above 90%. A sustained in vitro drug release was achieved for up to twenty days and cytotoxicity was markedly increased (IC50 for grandisin-NC and grandisin were 0.005 µM and 0.078 µM, respectively), indicating that polymeric nanocapsules are a potential drug delivery system for grandisin allowing the preparation of formulations viable for further in vivo studies.
Abstract in English:Cecropia glaziovi Snethl., Urticaceae, is commonly used in South America and is one of the species included in the Brazilian Medicinal Plants Research Program. Pharmacological studies have led to reports of the potential of C. glaziovi as a hypotensive, antiasthmatic and anxiolytic agent. The strict requirements regarding the quality, safety and effectiveness of phytopharmaceutical products represent an enormous challenge in the search for products with a high level of uniformity, reproducibility and stability. The incorporation of dry extracts into multiparticulate dosage forms, such as pellets produced by extrusion/spheronization technology, is a suitable alternative to overcome the lack of technological properties of dry extracts, since they are associated with low flowability and high hygroscopicity. In this study, an optimized dry extract (ODE) of C. glaziovi was incorporated into pellets seeking to decrease the moisture sorption and increase the stability, safety and percentage of the extract in the final product. Pellets containing around 50% of ODE were considered the most technologically viable, offering a narrow particle size distribution, significant improvement in the flowability and compressibility properties, and decrease in the moisture compared with the ODE. In conclusion, pellets containing a high dose of the C. glaviovi extract were successfully prepared, achieving degrees of quality, physical stability and feasibility compatible with the desirable characteristics of a phytopharmaceutical.
Abstract in English:Pothomorphe umbellata (L.) Miq., Piperaceae, has been extensively used in Brazilian folk medicine and it is well known for its strong antioxidant properties. However, its main active constituent, 4-nerolydilcatechol (4-NC), is sensitive to ultraviolet and visible light, which can limit the use of intermediate and final herbal preparations of this species. In the present work, coated multiparticulate solid dosage forms of P. umbellata were obtained with the purpose of increasing the stability of 4-NC. P. umbellata extract was used as a wetting liquid for the preparation of pellets by extrusion-spheronization. Pellets were coated in a fluidized bed by three different polymers (hydroxypropylmethylcellulose (HPMC), polyvynilpirrolidone K-30 (PVP-K30), and polyvinyl alcohol-polyethylene glycol graft-copolymer (PVAPEG)). 4-NC photostability was evaluated by an accelerated photostability protocol. Pellets showed a narrow size distribution and low friability. 4-NC photodegradation followed a second order degradation kinetics with similar k values for the percolate, uncoated pellets and HPMC coated pellets. Photoprotection was higher in pellets coated with PVP-K30 and PVA-PEG. PVA-PEG coated pellets with 6 and 9% weight gain resulted in a final concentration of 4-NC approximately cinco times higher than uncoated pellets or liquid extracts, suggesting the potential of this formulation as a multiparticulate solid dosage form for P. umbellata extracts.
Abstract in English:Soy isoflavones have been extensively used for menopausal symptoms and prevention of hormone-related cancer, osteoporosis and cardiovascular diseases. Commercially available forms of isoflavones include supplements, capsules and tablets. However, the non-standardization of soy isoflavones extracts and different dissolution profiles of these solid dosage forms highlight the need of additional studies on the development of well characterized pharmaceutical dosage forms of isoflavones. In this work, immediate release oral tablets of soy isoflavones were obtained and evaluated. Genistein and daidzein, were the main constituents of the dried soy extract. Preparation of the tables was accomplished in a rotary tableting machine following either a dry mixture for direct compression or wet granulation with different excipients. Powder, granules and tablets were evaluated for several parameters, including flow properties, Carr and Hausner indexes, hardness, friability, disintegration time and drug release profile. Also, a fast and validated HPLC analytical method for both genistein and daidzein was developed. Formulations containing sodium croscarmellose and sodium dodecyl sulfate resulted in better flowability as indicated by the flow rate and angle of repose, faster disintegration time and immediate release dissolution profile.
Abstract in English:With this study we evaluated the effects of the herb rosemary (Rosmarinus officinalis L. Lamiaceae) extract on the labeling of blood constituents with technetium-99m (99mTc) labeled sulphur colloid and on the biodistribution of 99mTc-Sulphur Colloid in Wistar albino rats. For this purpose, two groups of animals (male wistar rats, 130-140 g) were treated (1 mL) with a rosemary extract (750 mg/kg body wt.,n=9) and water (control, n=9) separately by gavage for five days. 99mTc-Sulphur Colloid was administrated by intravenous injection; organs/tissues were withdrawn and weighted. Blood was centrifuged, plasma and blood cells were isolated. The radioactivity was counted to calculate the percentage of activity per gram for each organ/tissue and percentage of activity in blood cells and plasma. A significant increase (p<0.05) in the uptake of 99mTc-Sulphur Colloid in the liver after the treatment with rosemary extract was observed. These results indicate that the substances or metabolites of the rosemary extract would change the biodistribution of99mTc-Sulphur Colloid.
Abstract in English:This study evaluated the technological feasibility of producing a semipurified extract of guaraná (Paullinia cupana Kunth, Sapindaceae) in tablet form, using a direct-compression process. Maltodextrin and gum arabic were used to produce the extract microparticles, in order to protect the microparticles against such factors as temperature, oxidation, and humidity. Using pharmacopoeial methodologies, technological and physicochemistry tests (determination of residual moisture, of bulk and tapped density, Hausner ratio, compressibility and compactibility index, appearance, mean weight, hardness, friability, disintegration time, determination of EPA amount in tablets and in vitro release profile) were conducted. The formulation containing 200 mg of microparticles, 170 mg microcrystalline cellulose, and 10 mg lactose gave the best results in terms of hardness (116 N), friabilility (0.28%), mean weight (0.3821 g), and disintegration time (25 min) for a tablet designed for oral administration. The results met pharmacopoeial specifications, and the tablets are suitable for oral administration.
Abstract in English:Calophyllum brasiliense Cambess, Calophyllaceae, is of great interest in folk medicine and is used in the treatment of various diseases such as diabetes. Granules containing the hydroethanolic extract from the stem bark of C. brasiliense were obtained. The polyphenol content was standardized, and the average weight, disintegration, and the dissolution profiles of the capsules were determined after encapsulation. The capsules had an average weight of 574.5±8.0 mg. In vitro tests showed that the most efficient disintegration profile was in hydrochloric acid buffer (pH 1.2), with a capsule disintegration time within 9 min. The dissolution analysis showed a better uniformity of capsule content release when the test was performed in a hydrochloric acid buffer (pH 1.2), with a maximal release rate at 15 min (giving a polyphenol content of 4.38%, which corresponds to a concentration of 0.0080 mg/mL). In distilled water, the maximal release was reached at 20 min (giving a polyphenol content of 5.41%, which is equivalent to 0.0105 mg/mL). In phosphate buffer, the maximal release of capsule contents was reached at the end of the dissolution assay (30 min), with the lowest amount of released polyphenols (3.61%, which corresponds to a concentration of 0.0070 mg/mL). The encapsulated form of the hydroethanolic extract of C. brasiliense was shown to have the necessary traits of a desirable delivery agent, and the dissolution test was an effective analysis of this material's polyphenol release profile for the specific dosage form.