Sandra Maria Warumby Zanin

Obstáculos da atenção farmacêutica no Brasil

A Atencao Farmaceutica, entendida como um modelo de pratica profissional desenvolvida no contexto da assistencia farmaceutica, de acordo com a proposta de Consenso Brasileiro de Atencao Farmaceutica, possui por finalidade aumentar a efetividade do tratamento medicamentoso, concomitante a deteccao de problemas relacionados a medicamentos (PRMs). Compoe uma pratica que vem sendo gradualmente aplicada em numero crescente de farmacias comunitarias em diversas regioes, porem ainda como projetos individuais, enfrentando diversas dificuldades na sua incorporacao, em parte devido ao desconhecimento e despreparo dos profissionais, bem como por certa rejeicao por parte de proprietarios de farmacias. Nesse contexto, realizou-se uma pesquisa com caracteristica participativa, por meio de entrevista com questoes abertas a farmaceuticos e proprietarios de farmacia no Municipio de Curitiba, na qual houve interacao das ideias, com o proposito de estabelecer permuta de informacoes sobre o referido conhecimento. Os resultados obtidos confirmam que a implantacao da Atencao Farmaceutica enfrenta obstaculos que incluem o vinculo empregaticio do profissional farmaceutico e a rejeicao do programa por gerentes e proprietarios das farmacias, alem da inseguranca e desmotivacao por parte dos farmaceuticos, decorrente de elevada carga labutaria e falta de tempo para dedicar-se ao atendimento, alem da concorrencia dos balconistas em busca de comissoes sobre vendas. Constata-se a necessidade de estimular a atuacao profissional, principalmente de academicos e egressos profissionais, o que pode representar um primeiro passo ao sucesso da Atencao Farmaceutica e a abertura por parte dos empresarios, uma vez que a sociedade comeca a reconhecer a importância do atendimento realizado pelo farmaceutico.

Isolation and characterization of β-d-glucan, heteropolysaccharide, and trehalose components of the basidiomycetous lichen Cora pavonia

Abstract Cora pavonia, a lichen having a basidiomycetous mycobiont, is rich in protein (36%), of which 10% is tyrosine. α,α-Trehalose is present and was isolated in 4.4% yield. The lichen was found to contain polysaccharides typical of basidiomycetes and different from those of ascomycetes and ascomycetous lichens. Isolated and characterized were a β- d -glucan and a heteropolysaccharide containing l -rhamnose, l -fucose, d -xylose, d -mannose, d -glucose, and d -galactose. The β- d -glucan was highly branched with 21% of nonreducing end-groups, contained 3-O-, 6-O-, and 3,6-di-O-substituted β- d -glucopyranosyl units, and had a main chain consisting of (1→3)- and (1→6)-links. The heteropolysaccharide component contained mainly mannose and xylose, having a mannose-containing nucleus and a main chain with preponderant (1→3)-linked α- d -mannopyranosyl residues. These were unsubstituted (10%), and 4-O- (10%) and 2,4-di-O-substituted (10%) with residues of β- d -xylopyranose. On methylation analysis of the heteropolysaccharide, a capillary column of DB-210 proved to be particularly useful for gas-liquid chromatographic resolution of partially O-methylated alditol acetates.

Phytochemical constituents and preliminary toxicity evaluation of leaves from Rourea induta Planch. (Connaraceae)

Most active plants are toxic at high doses and it is therefore important to investigate the preliminary toxicity of plant extracts. The Rourea induta species is a potential drug with no phytochemical or biological studies registered in the literature. Thus, a phytochemical study and a toxicity analysis of the ethanolic extract obtained from the leaves of Rourea induta Planch., Connaraceae, was run. A long chain hydrocarbon, n-tetracosane, and four flavonoids were identified: quercetin, and three glycosylated derivates, quercetin-3-O-α-arabinofuranoside, quercetin-3-O-β-xyloside and quercetin-3-O-β-galactoside. This is the first time these have been isolated in this species. The structures were elucidated by 13C NMR, 1H NMR, UV and IR spectroscopy. The toxicity evaluation of extracts was performed by the brine shrimp method and determination of hemolytic activity. The samples demonstrated no toxic potential by the analyzed methods.

Production and characterization of alginate-starch-chitosan microparticles containing stigmasterol through the external ionic gelation technique

O estigmasterol, um fitoesterol com diversas atividades farmacologicas, e suscetivel a oxidacao quando exposto ao ar, calor e umidade. Neste contexto, a microencapsulacao e uma forma de protecao contra oxidacao, permitindo a incorporacao do estigmasterol em diversas formas farmaceuticas e aumentar sua absorcao. As microparticulas foram obtidas por gelificacao ionica externa, em uma etapa, utilizando como revestimento polimeros naturais de alginato de sodio, amido de milho e quitosana. As microparticulas apresentaram formato esferico com tamanho aproximado de 1,4 mm. O rendimento foi de 94,87% e a eficiencia media de encapsulacao de 90,42%. A quantidade de estigmasterol no oleo recuperado das microparticulas foi de 9,97 mg/g. O metodo mostrou-se viavel para a microencapsulacao do estigmasterol.

Alcalóides aporfinóides do gênero Ocotea (Lauraceae)

During the last decades several aporphinoid alkaloids of the Ocotea species have been isolated. This review describes the occurrence of the fifty four aporphinoids in seventeen different species of Ocotea: thirty nine (39) aporphine sensu stricto, four (4) oxoaporphine, five (5) 6a,7-dehydroaporphine, one (1) didehydroaporphine, one (1) C-3-O-aporphine, one (1) C-4-O-aporphine, two (2) phenanthrene, one (1) proaporphine and their 13C NMR spectral data.

Spray-dried Eudragit® L100 microparticles containing ferulic acid: Formulation, in vitro cytoprotection and in vivo anti-platelet effect

This paper aimed to obtain new spray-dried microparticles containing ferulic acid (FA) prepared by using a methacrylic polymer (Eudragit® L100). Microparticles were intended for oral use in order to provide a controlled release, and improved in vitro and in vivo biological effects. FA-loaded Eudragit® L100 microparticles were obtained by spray-drying. Physicochemical properties, in vitro cell-based effects, and in vivo platelet aggregation were investigated. FA-loaded Eudragit® L100 microparticles were successfully prepared by spray-drying. Formulations showed suitable encapsulation efficiency, i.e. close to 100%. Microparticles were of spherical and almost-spherical shape with a smooth surface and a mean diameter between 2 and 3μm. Fourier-transformed infrared spectra demonstrated no chemical bond between FA and polymer. X-ray diffraction and differential scanning calorimetry analyses indicated that microencapsulation led to drug amorphization. FA-loaded microparticles showed a slower dissolution rate than pure drug. The chosen formulation demonstrated higher in vitro cytoprotection, anti-inflammatory and immunomodulatory potential and also improved in vivo anti-platelet effect. These results support an experimental basis for the use of FA spray-dried microparticles as a feasible oral drug delivery carrier for the controlled release of FA and improved cytoprotective and anti-platelet effects.

Identificação de δ tocotrienol e de ácidos graxos no óleo fixo de urucum (Bixa orellana Linné)

Bixa orellana is a native plant of Brazil, popularly known as annatto. The purpose of this study was to isolate the oil from the seeds of B. orellana and from it, identify the antioxidant tocotrienol and quantify its fatty acids. The extraction of the oil was performed in a Soxhlet apparatus using hexane as solvent. The tocotrienol was isolated by chromatographic methods and identified by spectrometric methods NMR 1H and 13C. The fatty acids present in the oil were quantified by gas chromatography coupled with mass spectrometry. Results demonstrated the presence of δ-tocotrienol and among the fatty acids, the arachidonic acid was present, a substance which so far had not been previously reported.

Effect of Donepezil, Tacrine, Galantamine and Rivastigmine on Acetylcholinesterase Inhibition in Dugesia tigrina

Dugesia tigrina is a non-parasitic platyhelminth, which has been recently utilized in pharmacological models, regarding the nervous system, as it presents a wide sensitivity to drugs. Our trials aimed to propose a model for an in vivo screening of substances with inhibitory activity of the enzyme acetylcholinesterase. Trials were performed with four drugs commercialized in Brazil: donepezil, tacrine, galantamine and rivastigmine, utilized in the control of Alzheimer’s disease, to inhibit the activity of acetylcholinesterase. We tested five concentrations of the drugs, with an exposure of 24 h, and the mortality and the inhibition of acetylcholinesterase planarian seizure-like activity (pSLA) and planarian locomotor velocity (pLMV) were measured. Galantamine showed high anticholinesterasic activity when compared to the other drugs, with a reduction of 0.05 μmol·min−1 and 63% of convulsant activity, presenting screw-like movement and hypokinesia, with pLMV of 65 crossed lines during 5 min. Our results showed for the first time the anticholinesterasic and convulsant effect, in addition to the decrease in locomotion induced by those drugs in a model of invertebrates. The experimental model proposed is simple and low cost and could be utilized in the screening of substances with anticholinesterasic action.

Spray-dried solid dispersions containing ferulic acid: comparative analysis of three carriers, in vitro dissolution, antioxidant potential and in vivo anti-platelet effect

Abstract This article aimed to improve the relative solubility and dissolution rate of ferulic acid (FA) by the use of spray-dried solid dispersions (SDs) in order to ensure its in vitro antioxidant potential and to enhance its in vivo anti-platelet effect. These SDs were prepared by spray-drying at 10 and 20% of drug concentration using polyvinylpyrrolidone K30 (PVP-K30), polyethylene glycol 6000 (PEG 6000) and poloxamer-188 (PLX-188) as carriers. SDs and physical mixtures (PM) were characterized by SEM, XRPD, FTIR spectroscopy and TGA analysis. Spray-dried SDs containing FA were successfully obtained. Relative solubility of FA was improved with increasing carrier concentration. PVP-K30 and PEG 6000 formulations showed suitable drug content values close to 100%, whereas PLX-188 presented mean values between 70 and 90%. Agglomerates were observed depending on the carrier used. XRPD patterns and thermograms indicated that spray-drying led to drug amorphization and provided appropriate thermal stability, respectively. FTIR spectra demonstrated no remarkable interaction between carrier and drug for PEG 6000 and PLX-188 SDs. PVP-K30 formulations had changes in FTIR spectra, which denoted intermolecular O–H•••O = C bonds. Spray-dried SDs played an important role in enhancing dissolution rate of FA when compared to pure drug. The free radical-scavenging assay confirmed that the antioxidant activity of PEG 6000 10% SDs was kept. This formulation also provided a statistically increased in vivo anti-platelet effect compared to pure drug. In summary, these formulations enhanced relative solubility and dissolution rate of FA and chosen formulation demonstrated suitable in vitro antioxidant activity and improved in vivo anti-platelet effect.

A Stability-Indicating HPLC-DAD Method for Determination of Ferulic Acid into Microparticles: Development, Validation, Forced Degradation, and Encapsulation Efficiency

A simple stability-indicating HPLC-DAD method was validated for the determination of ferulic acid (FA) in polymeric microparticles. Chromatographic conditions consisted of a RP C18 column (250 mm × 4.60 mm, 5 μm, 110 Å) using a mixture of methanol and water pH 3.0 (48 : 52 v/v) as mobile phase at a flow rate of 1.0 mL/min with UV detection at 320 nm. The developed method was validated as per ICH guidelines with respect to specificity, linearity, limit of quantification, limit of detection, accuracy, precision, and robustness provided suitable results regarding all parameters investigated. The calibration curve was linear in the concentration range of 10.0–70.0 μg/mL with a correlation coefficient >0.999. Precision (intraday and interday) was demonstrated by a relative standard deviation lower than 2.0%. Accuracy was assessed by the recovery test of FA from polymeric microparticles (99.02% to 100.73%). Specificity showed no interference from the components of polymeric microparticles or from the degradation products derived from acidic, basic, and photolytic conditions. In conclusion, the method is suitable to be applied to assay FA as bulk drug and into polymeric microparticles and can be used for studying its stability and degradation kinetics.