Utilization of a spouted bed for the application of enteric coating in hard gelatin capsules

Apresenta-se nesse trabalho um estudo da viabilidade da aplicação de revestimento gastro-resistente em cápsulas gelatinosas duras pelo processo leito de jorro. As variáveis investigadas foram: a razão entre a vazão mássica de suspensão de revestimento alimentada pela vazão de gás introduzida ao sistema (Ws/Wg), a razão entre a vazão de ar de jorro pela vazão correspondente à condição de jorro mínimo (Q/Qjm), massa inicial de cápsulas inseridas no equipamento (M0) e o tamanho das cápsulas (Tcaps). O processo e a qualidade do produto obtido foram analisados através da taxa de aumento de massa das cápsulas (K1), da eficiência de adesão durante a operação (·), ensaios de desintegração, ensaios de compressão e por microfotografias obtidas em microscópio eletrônico de varredura. Os experimentos foram realizados em um leito de jorro com coluna cilíndrica de 15 cm de diâmetro e base cônica com ângulo incluso de 40º. A análise dos resultados obtidos levou à determinação da melhor condição para a aplicação de revestimento de cápsulas: Ws/Wg = 0,0014 e Q/Qjm = 3,0, para ambas as massas de cápsulas introduzidas no sistema e tamanhos de cápsulas estudados. Os ensaios de desintegração mostraram que massas de revestimento superiores a 0,006 g/cm² proporcionam o efeito gastro-resistente.In this work is presented a study of the viability of the use of the spouted bed for application of the gastric resistant coating on hard gelatin capsules. The parameters studied were the ratio between the mass feed flow rate of the coating suspension to the mass feed flow rate of the gas introduced to the system, (Ws/Wg), the ratio between the flow rate of the spouting gas relative to the minimum spouting, (Q/Qjm), the mass of capsules loaded to the equipment, (M0) and the capsule's size, (Tcaps). The performance of the process as well as the coating quality were evaluated through the increase rate of the particle mass, (K1), by the adhesion efficiency, (·), disintegration and compression tests and by photomicrographs obtained in a scanning electronic microscope. The experiments were carried out in a spouted bed with 15 cm of the cylindrical column and with an included angle of the conical base of the 40º. The results lead to the determination of the best condition for application of the coating on hard gelatin capsules: Ws/Wg = 0.0014 and Q/Qjm = 3.0, for both mass of capsules loaded to the system and capsule's size investigated. The disintegration tests showed that the gastric resistant properties are obtained with a coating mass higher than 0.006 g/cm²

Estudo Farmacognóstico e Screening Biológico de Solanum lycocarpum St. Hill (Solanaceae)

Devido ao negligenciamento e ao aumento de números de casos das doenças microbianas e parasitárias no Brasil, o aprimoramento da investigação científica e tecnológica na área de plantas medicinais faz-se indispensável para à busca de novos produtos antimicrobianos e antiparasitários. A Solanum lycocarpum St. Hill. (Solanaceae) é uma planta medicinal tradicionalmente utilizada na forma de polvilho de lobeira como terapia complementar para o tratamento do Diabetes Mellitus, hipocolesterolêmico e na hipertensão. Os efeitos terapêuticos são atribuídos aos dois glicoalcaloides predominantes nas espécies do gênero Solanum, a solamargina e a solasonina. Em face ao exposto o objetivo desta pesquisa foi o isolamento de solasonina e solamargina de frutos maduros de S. lycocarpum e o screening de atividades antimicrobiana, antiparasitária, antioxidante e citotóxica do extrato etanólico 96 % bruto, frações e dos glicoalcaloides. O extrato etanólico 96 % bruto foi obtido por refluxo utilizando como solvente etanol 96 ºGL e seco sobre pressão reduzida. O isolamento dos glicoalcalóides foi realizado por meio de sequência de técnicas cromatográficas. Foram analisadas as atividades, antimicrobiana (E. faecalis, S. salivarius, S. sobrinus, S. mutans, S. mitis, S. sanguinis, L. casei, B. subtilis, P. aeruginosa, Salmonella enterican, E. faecalis, S. aureus, E. coli, C. albicans, A. niger, A. flavus e Fusarium sp.), antiparasitária (Giardia lamblia, Leishmania infantum, Trypanosoma cruzi e Trypanosoma brucei), antioxidante e citotóxica. No processo de purificação foram obtidas 6 frações e nas sub-frações 2.5 e 2.7 foram isolados os glicoalcalóides solasonina (Rf = 0,46) e solamargina (Rf = 0,57), respectivamente. Apresentaram atividade parasitária para Giardia lamblia (extrato etanólico 96 % (v/v) bruto, fração etanólica 40 % (v/v) frações F1 e F2), Leishmania infantum...The neglect and increased of the numbers of cases of microbial and parasitic diseases in Brazil and the improvement of scientific and technological research in the medicinal plants has contributed for the search of new antimicrobials and antiparasitic. The Solanum lycocarpum St. Hill. (Solanaceae) is a medicinal plant traditionally used as complementary therapy for the treatment of Diabetes Mellitus, hypocholesterolemic and hypertension. The therapeutic effects are attributed to the two predominant glycoalkaloids in Solanum species, the solamargine and the solasonina. In view of the above, the objective of this research was to isolate solasonina and solamargine of ripe fruits of S. lycocarpum and screening of antimicrobial, antiparasitic, antioxidant and cytotoxicity activities of crude extract 96% ethanol, fractions and glycoalkaloids. The crude extract 96% ethanol was obtained by reflux with as solvent ethanol 96 º GL and reduced pressure dried. The isolation of glycoalkaloids was performed by chromatographic techniques. We analyzed the activity, antimicrobial (E. faecalis, S. salivarius, S. sobrinus, S. mutans, S. mitis, S. sanguinis, L. casei, B. subtilis, P. aeruginosa, Salmonella enterican, E. faecalis, S. aureus, E. coli, C. albicans, A. niger, A. flavus and Fusarium sp.), antiparasitic (Giardia lamblia, Leishmania infantum, Trypanosoma cruzi and Trypanosoma brucei), antioxidant and cytotoxicity. In the purification process were obtained six fractions and the in the sub-fractions 2.5 and 2.7 were isolated the glycoalkaloids, solasonina (Rf = 0.46) and solamargine (Rf = 0.57). Showed activity for parasite Giardia lamblia (crude extract 96% ethanol, ethanol fraction 40%, fractions F1 and F2), Leishmania infantum (crude extract 96% ethanol, ethanol fraction 40%, fractions F1, F2 and F3)... (Complete abstract click electronic access below

Composition and Activity against Oral Pathogens of the Essential Oil of Melampodium divaricatum (Rich.) DC.

The chemical composition of the essential oil isolated from the aerial parts of Melampodium divaricatum (Rich.) DC. (Asteraceae) was characterized by GC-FID and GC/MS analyses. (E)-Caryophyllene (56.0%), germacrene D (12.7%), and bicyclogermacrene (9.2%) were identified as the major oil components. The antimicrobial activity of the oil against seven standard strains of oral pathogens from the American Type Culture Collection (ATCC) was evaluated by determining minimum inhibitory concentrations (MICs) using the microdilution method. MIC Values below 100 mu g/ml were obtained against Streptococcus sobrinus (90 mu g/ml), Lactobacillus casei (30 mu g/ml), S. mutans (20 mu g/ml), and S. mitis (18 mu g/ml). In contrast, the MIC values of the major oil compound (E)-caryophyllene were higher than 400 mu g/ml against all pathogens, suggesting that the activity of the oil might depend on minor oil components and/or on synergistic effects. The M. divaricatum essential oil is a promising agent to include in anticariogenic oral rinse formulations for the control of oral pathogens

Optimization of extraction conditions and antioxidant activity of Solanum lycocarpum fruits

Antioxidants are substances that may protect cells from the damage caused by unstable molecules known as free radicals. The capacity of natural antioxidant from phytochemical has increase attention from researchers and public. However, the extraction process is affecting the activity and the bioavailability of bioactive compounds. The Solanum lycocarpum is a plant of the Brazilian “cerrado”, popularly used as a hypoglycemic, hypocholesterolemic and control of metabolic diseases. Its effects are attributed to the presence of several glycoalkaloids (solamargine, solasonina) and solasodine. Therefore, the purpose of this communication was, investigate the optimization of extraction condition and evaluation of antioxidant activity from fruits of Solanum lycocarpum. The extracts were obtained using different solvent systems, i.e., water, 50% ethanol, ethanol absolute and ethyl ether (1:10 and 1:20) and different extraction processes: maceration with constant agitation at room temperature, maceration with constant agitation and heating at 30°C and ultrasound. The extracts were characterized by the amount of material extracted (1, 6 and 24 h) and the action of antioxidant activity by DPPH method. The results showed that the polar solvent (50% ethanol) and extractive process maceration with agitation to ambient temperature showed higher contents of extractable of fruits of S. lycocarpum (3.4 g %) and also showed higher antioxidant activity (88.57±2.41% de inhibition). This action whether the presence of glycoalkaloids (solamargine, solasonine and solasodine) in fruits S. lycocarpum which are polar compounds and may explain this increased antioxidant action of this extract

Paepalanthus spp: antimycobacterial activity of extracts, methoxylated flavonoids and naphthopyranone fractions

Paepalanthus spp., Eriocaulaceae, are native plants from Brazil known as “sempre-vivas” (everlasting flowers). In this work, we evaluated the potential anti-mycobacterial activity of two methoxylated flavonoids (flavonoid 7-methylquercetagetin and 7-methylquercetagetin-4′-O-β-D-glucopyranoside) isolated and identified from P. latipes and the naphthopyranone fractions from P. bromeliodes ethanolic extracts. The MIC value of 500 μg/mL was verified for all compounds tested against M. tuberculosis H37Rv. For M. avium, the MIC value ranged from 1000–2000 μg/mL excepting to naphthopyranone fractions with MIC of 500 μg/mL. This is the first report of activity determination of Paepalanthus spp. flavonoids activity against Mycobacterium tuberculosis and M. avium.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq

Composition and leishmanicidal activity of the essential oil of <i>Vernonia polyanthes</i> Less (Asteraceae)

<p>The composition of the essential oil (EO) from leaves of <i>Vernonia polyanthes</i> and the evaluation of its leishmanicidal potential are reported here for the first time. The oil obtained by hydrodistillation was analysed by combination of GC and GC/MS. Thirty-five compounds were identified, representing 91.8% of the oil composition. The oil consists primarily of monoterpenes (37.1%), sesquiterpenes (26.3%) and oxygenated sesquiterpenes (23.9%), myrcene (34.3%), zerumbone (15.8%), bicyclogermacrene (8.9%), α-humulene (4.8%) and germacrene D (4.3%) being the major constituents. Activity against <i>Leishmania infantum</i> was determined using the tetrazolium dye (MTT) colorimetric method. The oil, as well as zerumbone, one of its major constituents, showed significant leishmanicidal activity, with IC₅₀ values of 19.4 and 9.0 μg/ml, respectively. Cytotoxicity in macrophages cells was evaluated using the MTT colorimetric assay. The EO showed the CC₅₀ < 10 μg/ml to macrophages cells.</p