There is a shortage of solid oral dosage forms developed from standardized extracts of this plant specie. This study is aimed to obtain pellets with a standardized liquid extract of B. The standardized liquid extract of B. Pellets were obtained through a mixture of extract of g of B. These pellets were coated with a suspension composed of titanium dioxide, aluminum red lacquer, ethyl cellulose, talc and magnesium stearate.

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There is a shortage of solid oral dosage forms developed from standardized extracts of this plant specie. This study is aimed to obtain pellets with a standardized liquid extract of B. The standardized liquid extract of B. Pellets were obtained through a mixture of extract of g of B. These pellets were coated with a suspension composed of titanium dioxide, aluminum red lacquer, ethyl cellulose, talc and magnesium stearate.

Before the photostability test, the uncoated pellets showed psoralen content equal to 0. After exposure to one level 3 J. After exposure to three levels 10, 20 and 30 J. The coated pellets where unaffected after photostability test. Pellets were obtained with the standardized liquid extract of B. Brosimum gaudichaudii Trecul. Moraceae roots, is tradionally used in Brazil for the treatment of patients with vitiligo, this effectiveness is attributed to the psoralens, psoralen and 5-methoxypsoralen 5-MOP.

Neurohumoral imbalances and states of oxidative stress are also associated with the expression of vitligo. Varanda et al. They conclude that the extract with higher levels of psoralens is more toxic. However, Cunha et al. Until now the therapeutics dosage for this plant, extract has not been stated based on the contents of the psoralens.

Despite being promising the authors did not find reports available on studies related to the technological aspects regarding the preparation of solid dosage forms containing the extract obtained from the roots of B. The use of pellets obtained by extrusion-spheronization is an interesting approach to the incorporation of this plant extract into solid dosage forms. Pellets are classified as a multiparticulate drug delivery system with many related biological advantages.

In this study, the standardized extract of B. The roundest pellets with a large amount of the extract were selected for the coating process. The characteristics of the pellets and photostability of psoralen and 5-MOP have been determined and compared. The macerated material underwent percolation with free flow of the extract. The extract was collected and re-percolated, this process was repeated five times. Empower 2. The detection wavelength was set at nm for psoralen and nm for 5-MOP.

The chromatographic analysis of the extract of B. The wet mass was obtained by two different ways. In the first moment the powdered material were manually shaken during 15 min and then transferred to a bowl to wet granulation process. The powder and the granulation liquid were homogenates after 15 min of hand kneading.

This process was performed until the optimal formula was obtained for scale-up process. The amount of each component was determined experimentally. The wet masses was manually fed into the extrusion chamber and compressed against the extrusion plate at a speed of 35 rpm. The extrudates were spheronized in a cross-hatched plate with g of load, at rpm for 5 min or at rpm for 6 min. The coating suspension was obtained sitirring in mL of water, 6. Separately, while continuously stirred until completely dispersed, 3.

The pellets were placed as a monolayer. The identification and quantification of psoralen and 5-MOP were performed with chromatographic methods previously described. The extraction procedure of psoralen and 5-MOP were performed with 15 mg of coated or uncoated pellets, crushed with mortar and pestle.

The crushed material was standardized by size separation with a mesh sieve. This powder was transferred to an Erlenmeyer flask with 10 mL of methanol and subjected to ultrasonic bath during 20 min.

After that, the contents inside of the flask were centrifuged at rpm for 10 min. The precipitated material was separated from the supernatant, and the extraction process was repeated. From the samples obtained aliquots of 1 mL were collected, filtered through a 0. For the photostability test, the values of the reaction rate constant k was determined by the straight linear equation, attributing the angular coefficient a corresponding to the k value. All analyzes were performed in triplicate.

The aspect ratio, Feret diameter, and shape factor e R were determined using the freeware ImageJ to process the images. The SEM- EDS Energy-dispersive spectroscopy were used to identify cations of aluminum, titanium and magnesium in the coated pellets surface. The chromatographic method was precise and accurate. The percentage recovered of the psoralen was equivalent to The method has a limit of detection and quantification for psoralen equal to 0.

The values obtained with the system suitability test are in accordance with international official parameters. The hydroalcoholic extract possessed a pH of 5. The content of psoralen and 5-MOP in the hydroalcoholic extract of B.

During the stages of development of new pharmaceutical product, the first trials are conducted parsimoniously to ensure that the material used is not wasted and more information about it is generated. As a result, the BG1 formula [ Figure 1 ] was obtained only with microcrystalline cellulose and hydroalcoholic extract of B. The microcrystalline cellulose is the most popular excipient used in the production of pellets because it increases plasticity contributing for the formation of spherical shape in pellets and exhibited a weak natural adhesiveness.

According to Shah et al. Composition of the tested formulations obtained with the hydroalcoholic extract of Brosimum gaudichaudii. According to Beringhs et al. The use of HPMC is justified because this excipient provides a greater formation of hydrogen bridges.

The addition of HPMC and the reduction in the amount of plant extract increased the mechanical strength and decreased the moisture of its wet mass. According to Lukkonen et al. To reduce the adhesiveness the proportion of the plant extract was increased [ Table 1 ], obtaing BG3 formula. The modification to this formula was not enough to reduce mechanical strength, because dumbbell pellets [ Figure 1 ] were obtained.

For the first time pellets were produced, despite their low sphericity e R and elongated shape AR [ Table 2 ]. Results of the shape parameters from the pellets obtained with with the hydroalcoholic extract of Brosimum gaudichaudii. To reduce the formation of elongated pellets the spheronization process was changed according to the the studies proposed by Hellen, Yliruusi and Kristofferson.

In this new formula the time and the speed of revolutions of the spheronizer plate had been increased [ Table 1 ]. Although, compared with the BG4 the pellets obtained with BG5 formula were One last attempt to increase the proportion of hydroalcoholic extract of B. Therefore the ideal composition was established [ Table 1 ] for pellets with good sphericity and homogeneity [ Table 2 ].

Thus, we proceeded with the scale-up of BG6 for the BG7 formula, the pilot batch. The pilot batch BG7 showed an increase in r equal to 1. Despite the results achieved further studies are needed to evaluate the influence of production parameters or composition of the formula in the sphericity of pellets, prepared with the standardized extract of B.

Half the pellets obtained from the formula BG7 were coated [ Figure 1 ] to determine the importance of the coating in the photostability of psoralen and 5-methoxypsoralen. Both pellets coated and uncoated were subjected to photostability test. Prior to quantify the amount of psoralen and 5-MOP in pellets subjected to the test of photostability, the extraction process by ultrasound was conducted as described above.

Thus, after the second extraction the supernatant obtained showed only traces of the presence of psoralen and 5-MOP, which were below the limits of detection and quantification. Therefore, for the extraction of psoralen and 5-MOP of coated or uncoated pellets was necessary realizer only a first extraction.

Before the photostability test the uncoated pellets showed psoralen psoralen content equal to 0. The photodegradation of psoralen and 5-MOP happened in two phases.

The linear correlation coefficient r in k 1 or k2 , for both analytes, were equal to 1 [ Figure 2 ]. Photostability of psoralen and 5-methoxypsoralen from uncoated pellets obtained with Brosimum gaudichaudii hydroalcoholic extract. Standard deviation is indicated by bars. The conditions in which the photodegradation of these furocoumarins occurs is not yet clear. In other words, 5-MOP assumes reactive states more easily than the psoralen. The results obtained with UVA irradiation in the uncoated pellets shows that the photodegradation of 5-MOP in k 1 occurred faster than the psoralen [ Figure 2 ].

Based on this argument we can infer that the degradation rate decreases in k 2 because of this effect would become observed in the 5-MOP molecules that are in the deeper layers of the pellets. According to Balasaraswathy et al. Based on our previous results this sun exposure would be sufficient for the degradation of The application of the photoprotective suspension creates a film that protects the pellets individually.

Pellets were successfully obtained using The coating of pellets prevented psoralen and 5-MOP were degraded during the photostability assay. For the first time a formulation is proposed for obtaining pellets from this plant extract is also identified a technological alternative for maintaining the stability of its chemical markers.

Source of Support: Nil. Conflict of Interest: None declared. National Center for Biotechnology Information , U.


Brosimum gaudichaudii

Small fruit becoming grizzled and orange when ripe. Its juice is sweet and sticky and can be chewed much like gum. Seeds are not available for the Mama-Cadela. Please visit our seed store to view current selections. Description Small to medium sized tree with a crooked trunk, growing up to 25ft in height.


Alicastrum P. Browne Brosimopsis S. Moore Galactodendron Kunth Piratinera Aubl. Brosimum is a genus of plants in the family Moraceae , native to tropical regions of the Americas.


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