Fernanda Nervo Raffin

Traditional Uses, Chemical Constituents, and Biological Activities of Bixa orellana L.: A Review

Bixa orellana L., popularly known as “urucum,” has been used by indigenous communities in Brazil and other tropical countries for several biological applications, which indicates its potential use as an active ingredient in pharmaceutical products. The aim of this work was to report the main evidence found in the literature, concerning the ethnopharmacology, the biological activity, and the phytochemistry studies related to Bixa orellana L. Therefore, this work comprises a systematic review about the use of Bixa orellana in the American continent and analysis of the data collected. This study shows the well-characterized pharmacological actions that may be considered relevant for the future development of an innovative therapeutic agent.

Application of thermal analysis to the study of antituberculosis drugs-excipient compatibility

First-line drugs (rifampicin, RIF; isoniazid, INH; ethambutol, ETA; and pyrazinamide, PZA) recommended in conventional treatment of tuberculosis were analyzed in 1:1 w/w binary mixtures with microcrystalline cellulose MC 101 (CEL) and lactose supertab® (LAC) by differential scanning calorimetry (DSC), thermogravimetry (TG), differential thermal analysis (DTA), and Fourier transformed infrared analysis (FTIR) as part of development of fixed dose combination (FDC) tablets. Evidence of interaction between drug and pharmaceutical excipients was supposed when peaks disappearance or shifting were observed on DTA and DSC curves, as well as decreasing of decomposition temperature onset and TG profiles, comparing to pure species data submitted to the same conditions. LAC was showed to interact with RIF (absence of drug fusion and recrystallization events on DSC/DTA curves); INH (thermal events of the mixtures different from those observed for drug and excipient pure in DSC/DTA curves); PZA (decrease on drug fusion peak in DSC/DTA curves), and ETA (shift on drug onset fusion and absence of pure LAC events on DSC/DTA curves). In all cases, an important decrease on the temperature of drug decomposition was verified for the mixtures (TG analysis). However, FTIR analysis showed good correlation between theoretical and experimental drug-LAC spectra except for INH–LAC mixture, evidencing high incompatibility between these two species and suggesting that those interactions with PZA and RIF were thermally induced. No evidence of incompatibilities in CEL mixtures was observed to any of the four-studied drugs.

Application of thermal analysis to the study of anti-tuberculosis drug compatibility. Part 1

Worldwide Brazil is among one of the 22 countries with high rates of tuberculosis placing this disease as a priority for the Government Health Policies in this country. Studies with the main tuberculostatic drugs rifampicin, isoniazid, pyrazinamide, and ethambutol, aiming the development of fixed-dose combination formulations (FDCs) have been performed. The aim of this study was to evaluate the thermal behavior of these drugs by DSC, TG/DTG, and DTA in order to predict possible physical and chemical interactions between tuberculostatics. DSC and DTA curves suggested incompatibility and/or interactions among drug preparations resulting from new thermal events, as well as the disappearance and shift of the melting point of the drugs. TG/DTG curves of drug mixtures presented different profiles from those observed for the individually tested drugs, supporting the evidence of drug incompatibility and indicating that mixtures are less stable when compared to the drugs alone.

Permeability to hydrogen ions of an enteric coating polymer and interaction of film formulation factors

The influence of cellulose acetate phthalate film formulation on permeability to hydrogen ions was studied by measuring the permeability coefficients of free films in a diffusion cell. The effect of the studied factors and the interaction among them have been found to be significant. Aqueous and organic films have distinct behaviour; the former are considerably more permeable. Swelling experiments, X-ray diffraction and differential scanning calorimetry studies were carried out to clarify the differences observed in the permeability of the films.

Compatibility studies of trioxsalen with excipients by DSC, DTA, and FTIR

Psoralens are widely used for the treatment of psoriasis. Trioxsalen is a drug prescribed low-dose, belonging to the group of substituted psoralen. The aim of this study was to evaluate the compatibility of trioxsalen with pharmaceutical excipients used in the solid forms by analytical techniques. Binary mixtures between the trioxsalen and pharmaceutical excipients (namely, magnesium stearate, α-lactose, microcrystalline cellulose 102, pregelatinized starch, mannitol, sodium lauryl sulfate, sodium starch glycolate, and croscarmellose sodium) were examined. The trioxsalen–sodium lauryl sulfate mixture displayed some physical interaction based on the DTA and DSC results, but the FTIR study ruled out any chemical change.

Assessment of Phenolic Compounds and Anti-Inflammatory Activity of Ethyl Acetate Phase of Anacardium occidentale L. Bark

The bark of A. occidentale L. is rich in tannins. Studies have described various biological activities of the plant, including antimicrobial, antioxidant, antiulcerogenic and antiinflammatory actions. The objective of this study was to assess the activity of the ethyl acetate phase (EtOAc) of A. occidentale on acute inflammation and to identify and quantify its phenolic compounds by HPLC. The method was validated and shown to be linear, precise and accurate for catechin, epicatechin, epigallocatechin and gallic acid. Swiss albino mice (Mus musculus) were treated with saline, Carrageenan (2.5%), Indomethacin (10 mg/kg), Bradykinin (6 nmol) and Prostaglandine E2 (5 µg) at different concentrations of EtOAc - A. occidentale (12.5; 25; 50; and 100 mg/kg/weight p.o.) for the paw edema test. Challenge was performed with carrageenan (500 µg/mL i.p.) for the doses 50 and 100 mg/kg of EtOAc. Levels of cytokines IL-1, TNF-α, IL-6 and IL-10 were also measured. All EtOAc - A. occidentale concentrations reduced the edema. At 50 and 100 mg/kg, an anti-inflammatory response of the EtOAc was observed. Carrageenan stimulus produced a neutrophil count of 28.6% while 50 and 100 mg/kg of the phase reduced this to 14.5% and 9.1%, respectively. The EtOAc extract reduced levels of IL-1 and TNF-α. These results suggest that the EtOAc plays a modulatory role in the inflammatory response. The chromatographic method can be used for the analysis of the phenolic compounds of the EtOAc phase.

Characterization of palygorskite clay from Piauí, Brazil and its potential use as excipient for solid dosage forms containing anti-tuberculosis drugs

Clays play an important role in health products as it has been used as excipients for solid dosage forms and as active ingredients. Usually, excipients are pharmacologically inert, but they can interact with drugs in the solid dosage form and affect their bioavailability. Thus, the aim of this work was to determinate the physicochemical properties of palygorskite clay from Piauí, Brazil, and to investigate the potential use of this mineral as excipient for solid dosage forms containing rifampicin and isoniazid, which are drugs currently used to treat tuberculosis. Palygorskite was analyzed by X-ray fluorescence, X-ray diffraction, transmission electron microscopy, and particle size analyzer. According to the results, the main component found was SiO2, and its mineral composition contains palygorskite, dolomite, and quartz. The particles appear as fibers with bundle-like aspect that cluster together to form aggregates. The results from thermal analysis indicate that there is no interaction between both rifampicin and isoniazid with palygorskite. Moreover, the presence of palygorskite did not interfere on the dissolution of these drugs, which suggests that this material can be potentially used as an excipient for these drugs.

Representações sociais do medicamento genérico por usuários

The paper aimed to apprehend the social representations of the generic drug by drug users, establishing mechanisms that could be used to improve the policy of this type of medicines in Brazil. The Theory of Social Representations was employed as theoretic-methodological support. The research was done from April, 2002 through February, 2003 in the city of Natal/RN with 116 drug users approached at pharmacies and/or drugstores. The instrument of data collection was a semistructured interview with a tape recorder. The data analysis was performed with the aid of both the ALCESTE 4.5 program and the content analysis recommended by Laurence Bardin. The ALCESTE isolated 5 semantic classes and the content analysis identified 10 categories. For users the generic drug stands for a medicine sold at a lower price, a no-mark product equivalent to a more expensive one, but which supplies the immediate consumption demand, in addition to the fact that the word generic comprises a wider representation, absorbing and incorporating any products having the characteristics of generic drugs, but with questionable quality.

Development and validation of a simultaneous RP-HPLC-UV/DAD method for determination of polyphenols in gels containing S. terebinthifolius raddi (Anacardiaceae)

Topical gels containing extracts of Schinus terebinthifolius have been used to treat bacterial vaginosis. It has been reported that this species has anti-microbial, anti-inflammatory and anti-ulcerogenic properties, which can be attributed to the presence of phenolic compounds. In this work, a sensitive and selective reversed-phase HPLC-UV/DAD method for the simultaneous assay of six polyphenols that could be present in S. terebinthifolius was developed. The method was shown to be accurate and precise. Peak purity and similarity index both exceeded 0.99. Calibration curves were linear over the concentration range studied, with correlation coefficients between 0.9931 and 0.9974. This method was used to determine the polyphenol content of a hydroalcoholic extract and pharmacy-compounded vaginal gel. Although the method is useful to assess the 6 phenolic compounds, some compounds could not be detected in the products. Abbreviations used: RP-HPLC-UV/DAD: Reverse Phase High Performance Liquid Chromatograph with Ultraviolet and Diode Array Detector, HPLC: High Performance Liquid Chromatograph, HPLC-UV: High Performance Liquid Chromatograph with Ultraviolet Detector, ANVISA: Brazilian National Health Surveillance Agency, LOD: Limit of detection, LOQ: Limit of quantitation

Avaliação de géis obtidos a partir da acetilação da quitosana em meio heterogêneo

Chitosan was acetylated during 2, 5 and 10h and physical gels were obtained at different polymer concentrations in N,N-dimethylacetamide containing 5% of LiCl. Acetylation was confirmed by infrared spectroscopy and 13C NMR, and degrees of acetylation in the range of 0.82-0.91 were determined by NMR. The O-acetylation degree (0.12-0.15) was exclusively determined by a volumetric method. Rheological studies showed that the storage modulus values were smaller for the more acetylated samples and increased with the temperature and the polymer concentration. All the gels presented storage modulus superior to loss modulus, evidencing more elastic than viscous characteristics. The results obtained in this work suggest a gelation process based on a balance between O and N-acetylation and intermolecular bonds.