Cleildo P. Santana

Evaluation of the Interaction between the Poincianella pyramidalis (Tul.) LP Queiroz Extract and Antimicrobials Using Biological and Analytical Models.

Poincianella pyramidalis (Tul.) LP Queiroz (Fabaceae) is an endemic tree of northeastern Brazil, occurring mainly in the Caatinga. Its medicinal use is widespread and is an important therapeutic option against diarrhea, dysentery, and respiratory and urinary infections, among other diseases. In this study we determined the chemical marker and evaluated the interaction between P. pyramidalis extract and a commercial antimicrobial through the use of biological and analytical models. To obtain the extract, an ethanol-water mixture (50:50 v/v) was used as solvent. It was nebulized in a spray dryer using colloidal silicon dioxide as a drying adjuvant. The extract (ENPp) was subjected to HPLC analysis to verify the presence of certain secondary metabolites. The Minimum Inhibitory Concentration (MIC) of the extract against Gram-negative bacteria was determined by broth microdilution and the MIC of synthetic antimicrobial drugs in the presence and absence of the extract. The antioxidant activity of ENPp was evaluated by the DPPH method. The compatibility between the antimicrobial and the extract was evaluated by thermal analysis (TG/DTA). The acute toxicity of the extract was evaluated in vivo in rodents. The results indicate significant additive action of the extract on synthetic antibiotics, considerable antioxidant activity and absence of toxicity. This extract shows high potential for the development of formulations for antimicrobial therapy when used with a vegetable-active ingredient.

Sideroxylon obtusifolium herbal medicine characterization using pyrolysis GC/MS, SEM and different thermoanalytical techniques

This study aimed to characterize by analytical techniques Sideroxylon obtusifolium herbal medicine raw material derived from the leaves in different particle sizes, using scanning electron microscopy (SEM), thermoanalytical techniques [thermogravimetry (TG) and analysis differential thermal (DTA)] and pyrolysis coupled to gas chromatography/mass spectrometry (PYR-GC/MS). The different particle surface area among the samples was differentiated by the techniques. SEM distinguished the particles by its volumetric size, DTA and TG by the thermal and kinetic parameters and the PYR-GC/MS by degradation products chromatographic identification through the pyrograms.

Thermal decomposition profile of chitosan microparticles produced with Schinopsis brasiliensis Engler extract

Schinopsis brasiliensis Engler is a plant of Anacardiaceae family, used in the treatment of various diseases. Dried extracts have been used as intermediate product to obtain different pharmaceutical forms. Microparticles are a controlled-release system that protects unstable materials, and assist in increasing bioavailability parameters, while still allowing release to the specific site. This study aimed to trace the profile of microparticles of thermal degradation produced with S. brasiliensis Engl. extract in a chitosan matrix, evaluating some microparticles parameters (encapsulation efficiency, zeta potential, polydispersity index and SPAN factor). Thermal behavior of microparticles showed chitosan is able to protect the S. brasiliensis extract. Encapsulation efficiency and zeta potential are not directly proportional to flow rate, differently to polydispersity index and SPAN factor. This study showed the chitosan potential to protect S. brasiliensis extract of thermal degradation, allowing future applications.

Compatibility study between lipoic acid with polymers used in controlled drug release systems

Lipoic acid is derived from octanoic acid and is considered a universal antioxidant for combating free radicals and regeneration of endogenous antioxidant, as well as acting like an essential cofactor in multienzyme mitochondrial complex. In the pharmaceutical field, the polymers are among used excipients in pharmaceutical technology, especially in therapies controlled release of drugs. The aim of this study was to evaluate the drug–excipient compatibility between the AL and excipients used in controlled release drug delivery systems. To investigate the possible interactions between substances, was initially performed one screening with differential scanning calorimetry (DSC) to detect possible interactions, and analyses were performed by infrared spectroscopy (FTIR) to confirm the possible interactions. Based on the results of DSC and FTIR was found to be incompatible only with PVP-K30. Based on these results, we can conclude that the analytical tools used in this study are effective for defining incompatibilities between drugs and pharmaceutical excipients in order to ensure a new formulation with well-defined parameters of quality control and stability.

Compatibility study of dry extract of Ximenia americana L. and pharmaceutical excipients used in solid state

Ximenia americana L. is a plant of the Olacaceae family, used in the treatment of infectious diseases. Dry extracts are API’s of great interest for the pharmaceutical industry and have been used as final and intermediate products, resulting in different pharmaceutical forms. The aim of this study is to evaluate the compatibility of dry extract of X. americana with pharmaceutical excipients used in the solid forms. The extract was obtained by spray dryer, and binary mixtures of the dry extract and pharmaceutical excipients were analyzed. The studies were obtained using thermal analysis, X-ray powder diffraction and optical microscopy. With the data obtained from DSC curves, matrices for hierarchical cluster analysis (HCA) were made. The X-ray diffraction analysis showed changes in the mixtures’ profile with corn starch, lactose and magnesium stearate. Thermal behavior of the mixtures showed incompatibilities between the extract and lactose, corn starch and magnesium stearate. This study shows the importance of using instrumental analytical techniques in the early stages of development of herbal medicine to ensure the effectiveness, safety and quality of the final product.

Dissolution and uniformity of content of tablets developed with extract of Ximenia americana L.

Herbal medicines currently represent an important part of the world pharmaceutical market, which shows growing interest in the use of herbal medicines. However, the production of such medicines involves a complex series of steps, which determine the production viability and the quality of the final product. Ximenia americana L. is a plant occurring in several regions of the world, with well-known and applied medicinal properties. Thus, the aim of this work was to develop and evaluate the physical and physical-chemical quality of tablets produced with X. americana L. extract. The extract was spray-dried from a hydroethanolic extractive solution and characterized as to its phytochemical composition. The chemical marker was determined and quantified using validated chromatographic methods. These methods indicated the presence of gallic acid at a concentration of 1.61 mg g-1. Formulations were proposed and analyzed for their flow and compaction properties. The best formulation was used to obtain a batch of tablets, which was evaluated for its quality characteristics and showed to be within the pharmacopoeial specifications for average weight, hardness, friability, and disintegration time. The dissolution profile of the tablets produced was obtained, showing the release of about 70% of the vegetable extract content within 30 minutes. Results showed that it was possible to obtain herbal tablets containing a high content of vegetal extract by direct compression, developing a rapid process of formulation and production and guaranteeing the quality characteristics of the final product.